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inquiryDayangchem's R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. DayangChem can provide different quantities
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inquiry1. Factory price and high quality must be guaranteed, base on 8 years of production and R&D experience2. Free samples will be provided,ensure specifications and quality are right for customer3. Customers will receive the most professional technical s
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inquiryOur main production base is located in Xuzhou industry park. We are certified both to the ISO 9001 and ISO 14001 Standards, have a safety management system in place.Our R&D team masters core technology for process-design of target building block
Our advantages: 1. All inquiries will be replied within 12 hours. 2. Dedication to quality, supply & service. 3. Strictly on selecting raw materials. 4. Reasonable & competitive price, fast lead time. 5. Sample is available for your eva
Cas:875446-37-0
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inquiryWITH US,YOUR MONEY IN SAFE,YOUR BUSINESS IN SAFE 1)Quick Response Within 12 hours; 2)Quality Guarantee: All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France et
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inquiryOur Advantage: high quality with competitive price High quality standard: BP/USP/EP Enterprise standard All purity customized Fast and safe delivery We have reliable forwarder who can help us deliver our goods more fast and safe. We
Cas:875446-37-0
Min.Order:10 Kilogram
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inquiry1.No Less 8 years exporting experience. Clients can 100% received goods 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Upbio is Specialized
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inquiryAnacetrapib CAS:875446-37-0 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermediates, specializing in high quality organic intermediate
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inquiryHello, dear friend! I'm Hansen and Allen from China. Welcome to my lookchem mall! The following is a brief introduction of our company's products and services. If you are interested in our products, please contact us by emai
We can provide GMP validation service that complies with SFDA, FDA, WHO and EU EMPA.Excellent registration team could help us easlily to register our products in different countries.If you and your customer are interested in some products or need C
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inquiryHenan Wentao Chemical Product Co.,Ltd is Located in Zhengzhou High-tech Development Zone with import and export license, We passed ISO 9001:2008 as well, Henan Wentao has developed more than 1000 compounds, which are widely used in the fields of prod
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Our company provides one-stop services of research - development - production for a variety of special prouducts. Not only do we make effective use of our strong technological strength, but also establish of cooperative relations with several well-
Cas:875446-37-0
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inquiryHangzhou KeyingChem Co., Ltd. exported this product to many countries and regions at best price. If you are looking for the material’s manufacturer or supplier in China, KeyingChem is your best choice. Pls contact with us freely for getting det
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inquiryCompany Introduction 1. Established in 2005, with two independent business divisions: Fine chemicals division; Pharmaceutical division. 2. Main product: Optical brightener Textile auxiliary Dye stuff Pigments
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Zibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi
Cas:875446-37-0
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inquirySuperior quality, moderate price & quick delivery. Appearance:white crystal powder Storage:Stored in cool, dry and ventilation place; Away from fire and heat Package:10g/bag,or as your request Application:Used as Pharmaceutical Intermediates Tr
Product Name: Anacetrapib Synonyms: Anacetrapib;Mk0859;Mk-0859;Unii-p7T269pr6s;(4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-[[4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)biphen
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inquiryProduct Details Grade: pharmaceutical grade Purity:99%+ ProductionCapacity: 1000 Kilogram/Month Scope of use: For scientific research only(The product must be used legally) Our Advantage 1. Best quality with competitive price. 2. Quick shipping,
Cas:875446-37-0
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inquiryOur Advantages A. International Top level TechnologyOur company owned biomedicine experts are famous at home and abroad with rich experience in research and development in the field of efficient chiral functional molecules research and development an
GMP standard, high purity, competitive price, in stock 1. Quick Response: within 6 hours after receiving your email. 2. Quality Guarantee: All products are strictly tested by our QC, confirmed by QA, and approved by a third-party lab in China, USA,
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inquiryfactory?direct?saleAppearance:White Powder Storage:Store In Dry, Cool And Ventilated Place Package:25kg/drum, also according to the clients requirement Application:It is widely used as a thickener, emulsifier and stabilizer Transportation:By Sea Or B
Cas:875446-37-0
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inquiryProduct name: Anacetrpib CAS No.:875446-37-0 Molecule Formula:C30H25F10NO3 Molecule Weight:637.51 Purity: 99.0% Package: 25kg/drum Description:White powder Manufacture Standards:Enterprise Standard TESTING ITEMS
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inquiryShandong Mopai Biotechnology Co., LTD is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemicals. W
Cas:875446-37-0
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inquiry1.Applied in food field.it can improve the immune system and prolong life. 2.Appliedin cosmetic field.it can improve the skin care. 3.Applied in pharmaceutical field.it can treat various dieases. 4.Our product quality assurance will make our customer
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inquiryWuhu Nuovo Chemical Technology Co., Ltd. was established in August 2014, mainly engaged in the development, production and sales of ionic liquids, ribose, nucleosides, nucleotides and related chemicals; Products are mainly used in new energy, new ma
SAGECHEM is a chemical R&D, manufacturing and distribution company in China since 2009, including pharmaceutical intermediates, agrochemical, dyestuff intermediates, organosilicone, API and etc. We also offer a full range of services in custom synthe
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Type:Lab/Research institutions
inquiry(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one
anacetrapib
Conditions | Yield |
---|---|
With tetra-(n-butyl)ammonium iodide; potassium carbonate In N,N-dimethyl-formamide at 60℃; for 17h; | 92% |
Stage #1: (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one With sodium hexamethyldisilazane In N,N-dimethyl-formamide at -15℃; for 1h; Stage #2: 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)biphenyl In N,N-dimethyl-formamide at -15 - 12℃; | 88% |
Stage #1: (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one With sodium hexamethyldisilazane In N,N-dimethyl-formamide at -15℃; for 1h; Stage #2: 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)biphenyl In N,N-dimethyl-formamide at -10 - 12℃; | 88% |
anacetrapib
Conditions | Yield |
---|---|
With potassium hydroxide In tetrahydrofuran; methanol at 20℃; Inert atmosphere; | 89% |
anacetrapib
Conditions | Yield |
---|---|
Stage #1: (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one With sodium hexamethyldisilazane In N,N-dimethyl-formamide at -15℃; for 1.5h; Stage #2: 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)biphenyl In N,N-dimethyl-formamide at -15 - 12℃; | 88% |
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one
(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol
anacetrapib
Conditions | Yield |
---|---|
Stage #1: [4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-1,1'-biphenyl-2-yl]methanol With thionyl chloride In dichloromethane at 5 - 20℃; Stage #2: (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one With tetra-(n-butyl)ammonium iodide; potassium carbonate In dichloromethane at 60℃; | 72% |
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[2-iodo-5-(trifluoromethyl)benzyl]-4-methyl-1,3-oxazolidin-2-one
[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]boronic acid
anacetrapib
Conditions | Yield |
---|---|
With sodium carbonate; tetrakis(triphenylphosphine) palladium(0) In ethanol; water; benzene at 100℃; for 14h; Heating / reflux; | |
With potassium carbonate; palladium diacetate In water; acetone for 1h; Heating / reflux; |
anacetrapib
Conditions | Yield |
---|---|
In water-d2 at 37℃; for 3.75h; pH=7.52; Sodium phosphate buffer; |
1-bromo-2-(bromomethyl)-4-(trifluoromethyl)benzene
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: sodium hydride / tetrahydrofuran / 0 °C 1.2: 0 - 20 °C 2.1: tetrakis(triphenylphosphine) palladium(0); potassium carbonate / ethanol; water; toluene / Reflux View Scheme |
[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]boronic acid
(4S,5R)-5-(3,5-bis-trifluoromethyl-phenyl)-3-(2-bromo-5-trifluoromethyl-benzyl)-4-methyl-oxazolidin-2-one
anacetrapib
Conditions | Yield |
---|---|
With tetrakis(triphenylphosphine) palladium(0); potassium carbonate In ethanol; water; toluene Suzuki coupling; Reflux; |
1-(2-fluoro-4-methoxyphenyl)-1-ethanone
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: tetrahydrofuran / 1 h / -15 - 0 °C 2.1: hydrogenchloride; hydrogen / palladium 10% on activated carbon / ethanol; water / 1 h / 40 °C / 775.74 Torr 3.1: N-Bromosuccinimide / acetonitrile / 35 °C 4.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 4.2: Inert atmosphere 5.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 24 h / 35 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 7.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 7.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: tetrahydrofuran / 1 h / -15 - 0 °C 2.1: hydrogenchloride; hydrogen / palladium 10% on activated carbon / ethanol; water / 1 h / 40 °C / 775.74 Torr 3.1: N-Bromosuccinimide / acetonitrile / 35 °C 4.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 4.2: Inert atmosphere 5.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 30 - 45 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 7.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 7.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: tetrahydrofuran / 1 h / -15 - 0 °C 2.1: N-Bromosuccinimide / acetonitrile / 60 °C 3.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 4.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 4.2: 1 h / 15 - 20 °C / pH 2 5.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 7.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 7.2: -10 - 12 °C View Scheme |
2-(2-fluoro-4-methoxyphenyl)-2-isopropanol
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: hydrogenchloride; hydrogen / palladium 10% on activated carbon / ethanol; water / 1 h / 40 °C / 775.74 Torr 2.1: N-Bromosuccinimide / acetonitrile / 35 °C 3.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 3.2: Inert atmosphere 4.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 24 h / 35 °C / Inert atmosphere 5.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 6.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 6.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: hydrogenchloride; hydrogen / palladium 10% on activated carbon / ethanol; water / 1 h / 40 °C / 775.74 Torr 2.1: N-Bromosuccinimide / acetonitrile / 35 °C 3.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 3.2: Inert atmosphere 4.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 30 - 45 °C / Inert atmosphere 5.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 6.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 6.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: hydrogenchloride; hydrogen / palladium 10% on activated carbon / ethanol; water / 1 h / 40 °C / 775.74 Torr 2.1: N-Bromosuccinimide / acetonitrile / 35 °C 3.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 3.2: 1 h / 15 - 20 °C / pH 2 4.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 5.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 6.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 6.2: -10 - 12 °C View Scheme |
[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]boronic acid
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 24 h / 35 °C / Inert atmosphere 2.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 3.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 3.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 30 - 45 °C / Inert atmosphere 2.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 3.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 3.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 2.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 3.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 3.2: -10 - 12 °C View Scheme |
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: N-Bromosuccinimide / acetonitrile / 35 °C 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: Inert atmosphere 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 24 h / 35 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: N-Bromosuccinimide / acetonitrile / 35 °C 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: Inert atmosphere 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 30 - 45 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: N-Bromosuccinimide / acetonitrile / 35 °C 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: 1 h / 15 - 20 °C / pH 2 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 - 12 °C View Scheme |
1-bromo-4-fluoro-2-methoxy-5-(propan-2-yl)-benzene
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 1.2: Inert atmosphere 2.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 24 h / 35 °C / Inert atmosphere 3.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 1.2: Inert atmosphere 2.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 30 - 45 °C / Inert atmosphere 3.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 1.2: 1 h / 15 - 20 °C / pH 2 2.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 3.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -10 - 12 °C View Scheme |
(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 0 - 20 °C 2.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 2.2: -15 - 12 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 2.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 2.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: thionyl chloride / N,N-dimethyl-formamide / 10 - 20 °C 2.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 2.2: -10 °C View Scheme | |
Multi-step reaction with 4 steps 1: Dess-Martin periodane / dichloromethane / 2 h / 20 °C 2: isopropyl alcohol / 2 h / 35 - 40 °C 3: sodium tetrahydroborate / methanol / 2 h / 20 °C 4: tetrahydrofuran; N,N-dimethyl-formamide / 2 h / 70 - 75 °C View Scheme | |
Multi-step reaction with 2 steps 1: thionyl chloride; N,N-dimethyl-formamide / 10 - 15 °C 2: potassium carbonate; tetra-(n-butyl)ammonium iodide / N,N-dimethyl-formamide / 17 h / 60 °C View Scheme |
2,4-difluorobromobenzene
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1.1: tetrahydrofuran / 5 h / 65 - 68 °C 2.1: aluminum (III) chloride / 1,2-dichloro-ethane / 1 h / -10 - 5 °C 3.1: tetrahydrofuran / 1 h / -15 - 0 °C 4.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 5.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 5.2: 1 h / 15 - 20 °C / pH 2 6.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 7.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 8.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 8.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 8 steps 1.1: tetrahydrofuran / 5 h / 65 - 68 °C 2.1: aluminum (III) chloride / 1,2-dichloro-ethane / 1 h / -10 - 5 °C 3.1: tetrahydrofuran / 1 h / -15 - 0 °C 4.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 5.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 5.2: 1 h / 15 - 20 °C / pH 2 6.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 7.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 8.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 8.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 9 steps 1.1: tetrahydrofuran / 5 h / 65 - 68 °C 2.1: aluminum (III) chloride / 1,2-dichloro-ethane / 1 h / -10 - 5 °C 3.1: tetrahydrofuran / 1 h / -15 - 0 °C 4.1: sulfuric acid / 12 h / Reflux 5.1: hydrogen; hydrogen bromide / 5%-palladium/activated carbon / water; methanol / 0.25 h / 20 °C / 3102.97 Torr / Inert atmosphere 6.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 6.2: 1 h / 15 - 20 °C / pH 2 7.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 8.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 9.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 9.2: -10 - 12 °C View Scheme |
1-bromo-4-fluoro-2-methoxybenzene
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: aluminum (III) chloride / 1,2-dichloro-ethane / 1 h / -10 - 5 °C 2.1: tetrahydrofuran / 1 h / -15 - 0 °C 3.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 4.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 4.2: 1 h / 15 - 20 °C / pH 2 5.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 7.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 7.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: aluminum (III) chloride / 1,2-dichloro-ethane / 1 h / -10 - 5 °C 2.1: tetrahydrofuran / 1 h / -15 - 0 °C 3.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 4.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 4.2: 1 h / 15 - 20 °C / pH 2 5.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 7.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 7.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 8 steps 1.1: aluminum (III) chloride / 1,2-dichloro-ethane / 1 h / -10 - 5 °C 2.1: tetrahydrofuran / 1 h / -15 - 0 °C 3.1: sulfuric acid / 12 h / Reflux 4.1: hydrogen; hydrogen bromide / 5%-palladium/activated carbon / water; methanol / 0.25 h / 20 °C / 3102.97 Torr / Inert atmosphere 5.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 5.2: 1 h / 15 - 20 °C / pH 2 6.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 7.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 8.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 8.2: -10 - 12 °C View Scheme |
1-(5-bromo-2-fluoro-4-methoxyphenyl)ethan-1-one
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: tetrahydrofuran / 1 h / -15 - 0 °C 2.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 3.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 3.2: 1 h / 15 - 20 °C / pH 2 4.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 5.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 6.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 6.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: tetrahydrofuran / 1 h / -15 - 0 °C 2.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 3.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 3.2: 1 h / 15 - 20 °C / pH 2 4.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 5.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 6.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 6.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: tetrahydrofuran / 1 h / -15 - 0 °C 2.1: sulfuric acid / 12 h / Reflux 3.1: hydrogen; hydrogen bromide / 5%-palladium/activated carbon / water; methanol / 0.25 h / 20 °C / 3102.97 Torr / Inert atmosphere 4.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 4.2: 1 h / 15 - 20 °C / pH 2 5.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 7.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 7.2: -10 - 12 °C View Scheme |
(4'-fluoro-2'-methoxy-5'-(prop-1-en-2-yl)-4-(trifluoromethyl)biphenyl-2-yl)methanol
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: hydrogen / 5%-palladium/activated carbon / methanol / 20 °C / 1551.49 Torr / Inert atmosphere 2.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 3.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 3.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 3 steps 1: hydrogen; 5%-palladium/activated carbon / methanol / 20 °C / 1551.49 Torr 2: thionyl chloride / N,N-dimethyl-formamide / 5 h / 10 - 20 °C 3: sodium hexamethyldisilazane / N,N-dimethyl-formamide / -15 - 12 °C View Scheme |
2-(5-bromo-2-fluoro-4-methoxyphenyl)propan-2-ol
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: 1 h / 15 - 20 °C / pH 2 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: trifluoroacetic acid; 1,1,3,3-Tetramethyldisiloxane / 1,2-dichloro-ethane / 0.25 h / -20 - -10 °C 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: 1 h / 15 - 20 °C / pH 2 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: sulfuric acid / 12 h / Reflux 2.1: hydrogen; hydrogen bromide / 5%-palladium/activated carbon / water; methanol / 0.25 h / 20 °C / 3102.97 Torr / Inert atmosphere 3.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 3.2: 1 h / 15 - 20 °C / pH 2 4.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 5.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 6.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 6.2: -10 - 12 °C View Scheme |
1-bromo-4-fluoro-2-methoxy-5-(1-methylvinyl)benzene
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: hydrogen; hydrogen bromide / 5%-palladium/activated carbon / water; methanol / 0.25 h / 20 °C / 3102.97 Torr / Inert atmosphere 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: 1 h / 15 - 20 °C / pH 2 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: hydrogen; hydrogen bromide / 5%-palladium/activated carbon / water; methanol / 0.25 h / 20 °C / 3102.97 Torr / Inert atmosphere 2.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 2.2: 1 h / 15 - 20 °C / pH 2 3.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: n-butyllithium / toluene; hexane; tetrahydrofuran / -80 - -35 °C / Inert atmosphere 1.2: -35 °C 2.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 3.1: hydrogen / 5%-palladium/activated carbon / methanol / 20 °C / 1551.49 Torr / Inert atmosphere 4.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 - 12 °C View Scheme |
4-fluoro-2-methoxy-5-(2-propenyl)phenylboronic acid
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 2.1: hydrogen / 5%-palladium/activated carbon / methanol / 20 °C / 1551.49 Torr / Inert atmosphere 3.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 2.1: hydrogen / 5%-palladium/activated carbon / methanol / 20 °C / 1551.49 Torr / Inert atmosphere 3.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -10 - 12 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: hydrogen / 5%-palladium/activated carbon / methanol / 0.5 h / 20 °C / 1292.9 Torr / Inert atmosphere 2.1: potassium carbonate / (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / water; tetrahydrofuran / 32 h / 20 - 45 °C / Inert atmosphere 3.1: N,N-dimethyl-formamide; thionyl chloride / 5 h / 10 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -10 - 12 °C View Scheme |
2-fluoro-4-methoxy-1-(prop-1-en-2-yl)benzene
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: hydrogen / palladium on activated carbon / methanol / 50 °C / 2250.23 Torr / Inert atmosphere 1.2: 40 °C 2.1: n-butyllithium / toluene; hexane / -80 - -55 °C / Inert atmosphere 2.3: 1 h / 15 - 20 °C / pH 2 3.1: potassium carbonate / dichloro[1,1'-bis(di-t-butylphosphino)ferrocene]palladium(II) / water; tetrahydrofuran / 32 h / 35 - 45 °C / Inert atmosphere 4.1: thionyl chloride / N,N-dimethyl-formamide / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 5.2: -10 °C View Scheme |
C10H12BrFMgO
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: toluene; tetrahydrofuran / 5 - 10 °C 1.3: 15 - 20 °C / pH 2 2.1: potassium carbonate / dichloro[1,1'-bis(di-t-butylphosphino)ferrocene]palladium(II) / water; tetrahydrofuran / 32 h / 35 - 45 °C / Inert atmosphere 3.1: thionyl chloride / N,N-dimethyl-formamide / 10 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / 1 h / -15 °C 4.2: -10 °C View Scheme |
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C / Inert atmosphere 2.1: copper(l) chloride; potassium tert-butylate; 1,10-Phenanthroline / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere 2.2: 18 h / 50 °C / Inert atmosphere 3.1: sodium hexamethyldisilazane / tetrahydrofuran; N,N-dimethyl-formamide / 1 h / -20 °C / Inert atmosphere 3.2: 18 h / 20 °C View Scheme |
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: copper(l) chloride; potassium tert-butylate; 1,10-Phenanthroline / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere 1.2: 18 h / 50 °C / Inert atmosphere 2.1: sodium hexamethyldisilazane / tetrahydrofuran; N,N-dimethyl-formamide / 1 h / -20 °C / Inert atmosphere 2.2: 18 h / 20 °C View Scheme |
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: hydrogenchloride; zinc / 1 h / 0 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C / Inert atmosphere 3.1: copper(l) chloride; potassium tert-butylate; 1,10-Phenanthroline / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere 3.2: 18 h / 50 °C / Inert atmosphere 4.1: sodium hexamethyldisilazane / tetrahydrofuran; N,N-dimethyl-formamide / 1 h / -20 °C / Inert atmosphere 4.2: 18 h / 20 °C View Scheme |
3,5-diiodobenzaldehyde
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: / tetrahydrofuran / 20 h / -60 - 20 °C / Inert atmosphere 2.1: hydrogenchloride; zinc / 1 h / 0 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C / Inert atmosphere 4.1: copper(l) chloride; potassium tert-butylate; 1,10-Phenanthroline / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere 4.2: 18 h / 50 °C / Inert atmosphere 5.1: sodium hexamethyldisilazane / tetrahydrofuran; N,N-dimethyl-formamide / 1 h / -20 °C / Inert atmosphere 5.2: 18 h / 20 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: / tetrahydrofuran / 64 h / -60 °C 2.1: hydrogenchloride; zinc / 1 h / 0 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 12 h / 0 - 20 °C / Inert atmosphere 4.1: copper(l) chloride; potassium tert-butylate; 1,10-Phenanthroline / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere 4.2: 18 h / 50 °C / Inert atmosphere 5.1: sodium hexamethyldisilazane / tetrahydrofuran; N,N-dimethyl-formamide / 1 h / -20 °C / Inert atmosphere 5.2: 18 h / 20 °C View Scheme |
2-(3-(trifluoromethyl)phenyl)-4,5-dihydrooxazole
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: potassium phosphate; potassium acetate; triphenylphosphine; dichloro(benzene)ruthenium(II) dimer / 1-methyl-pyrrolidin-2-one / 42 h / 110 - 130 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine; methyl chloroformate / tetrahydrofuran / 0.75 h / 62 °C 2.2: 13 h / 0 - 20 °C 3.1: thionyl chloride / N,N-dimethyl-formamide / 5 h / 10 - 20 °C 4.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / -15 - 12 °C View Scheme |
3-trifluoromethylbenzonitrile
anacetrapib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: calcium chloride / 5,5-dimethyl-1,3-cyclohexadiene / 24 h / 125 °C / Inert atmosphere 2.1: potassium phosphate; potassium acetate; triphenylphosphine; dichloro(benzene)ruthenium(II) dimer / 1-methyl-pyrrolidin-2-one / 42 h / 110 - 130 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine; methyl chloroformate / tetrahydrofuran / 0.75 h / 62 °C 3.2: 13 h / 0 - 20 °C 4.1: thionyl chloride / N,N-dimethyl-formamide / 5 h / 10 - 20 °C 5.1: sodium hexamethyldisilazane / N,N-dimethyl-formamide / -15 - 12 °C View Scheme |
anacetrapib
(4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-((4'-fluoro-5'-isopropyl-2'-hydroxy-4-(trifluoromethyl)biphenyl-2-yl)methyl)-4-methyl-1,3-oxazolidin-2-one
Conditions | Yield |
---|---|
Stage #1: anacetrapib With boron tribromide In dichloromethane at 15 - 16℃; for 1h; Stage #2: With water In dichloromethane | 60% |
anacetrapib
(1R,2S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-[({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)amino]propan-1-ol
Conditions | Yield |
---|---|
With water; potassium hydroxide In isopropyl alcohol at 75℃; Sealed tube; |
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