Chemvon Biotechnology is one of the leading high-technology manufacturer in the field of pharmaceutical and fine chemical industry. From origins as a research group in technology service, chemvon has progressed into an integrated company with a k
Dayangchem'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
Cas:170729-80-3
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inquiryItems Standard Result Assay 98%min ---------------------------------------------------------------------------------------------
Cas:170729-80-3
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inquiryWelcome to Simagchem, your partner in China as a premier supply of bulk specialty chemicals for industry and life science. We introduce experienced quality product and exceptional JIT service with instant market intelligence in China to benefit our
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inquiryWe Puhopharma supply high quality of good pharmaceutical product. We specialize in controling the quality and reducing the impurities of Aprepitant . Our Aprepitant is with the best quality and the most competitive price in China. Our Aprepitant
LIDE PHARMACEUTICALS LIMITED is a professional chemicals and APIs leading manufacturer in China. Our core business line covers APIs, Intermediates, Herb extract, etc.
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inquiry1. Guaranteed purity; 2. Large quantity in stock; 3. Largest manufacturer; 4. Best service after shipment with email; 5. High quality & competitive price; ...... Appearance:White to off-white powder Storage:-20°C Freezer Package:100g/
Cas:170729-80-3
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inquiryAprepitant API and intermediates 170729-80-3 3-Chloromethyl-1,2,4-triazolin-5-one[CAS:252742-72-6] (2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine 4-methylbenzenesulfonate[CAS:200000-59-5] HANGZH
The above product is Ality Chemical's strong item with best price, good quality and fast supply. Ality Chemical has been focusing on the research and production of this field for over 14 years. At the same time, we are always committed to providi
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
Cas:170729-80-3
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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
Cas:170729-80-3
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inquiryShanghai Seasonsgreen Chemical is a high-tech research and development, production, sale and custom synthesis set in one high-tech chemical products enterprises. Our sales and marketing division is located in Shanghai, serving international pharmaceu
Cas:170729-80-3
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Name:Aprepitant CAS:170729-80-3 Grade:For chemical industry, scientific research and export Product Quality 12 years of chemical raw materials Mature operation of the industry System stability Data storage Security without vulnerability P
Cas:170729-80-3
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inquiryOur company was built in 2009 with an ISO certificate.In the past 5 years, we have grown up as a famous fine chemicals supplier in China and we had established stable business relationships with Samsung,LG,Merck,Thermo Fisher Scientific and so on.O
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
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Cas:170729-80-3
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inquiryChemical Name: Aprepitant Cas No.: 170729-80-3 Molecular Formula: C23H21F7N4O3 Molecular Weight: 534.43 Molecular Structure: Appearance:White powder Storage:Store in cool and dry
Advantages: Hubei XinRunde Chemical Co., Ltd is a renowned pharmaceutical manufacturer. We can offer high quality products at competitive price in quick delivery with 100% custom pass guaranteed. Never stop striving to offer our best serv
Cas:170729-80-3
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Cas:170729-80-3
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inquiryAprepitant CAS: 170729-80-3 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
Cas:170729-80-3
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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
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Cas:170729-80-3
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inquiryHebei Mojin Biotechnology Co., Ltd, Our company is a professional chemical raw materials and chemical reagents research and development production enterprises. We have several production line,So we can control the lowest price. We also have several
Cas:170729-80-3
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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
Shanghai SOYOUNG onsite assessment conducted by Bureau Veritas commissioned at June 2018. Assessed Supplier of Shanghai SOYOUNG is a faithful and professional supplier of health raw materials in pharmacy, food, cosmetic and other fields for many ye
Cas:170729-80-3
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inquiryAppearance:white or light yellow crystalline powder Storage:Store in a cool,dry place and keep away from direct strong light Package:As customer request Application:Used for research and industrial manufacture. Transportation:By
Cas:170729-80-3
Min.Order:100 Gram
Negotiable
Type:Lab/Research institutions
inquiryConditions | Yield |
---|---|
With potassium carbonate In water; N,N-dimethyl-formamide at 0℃; for 3h; | 99% |
2-[2-[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]-1-iminoethyl]hydrazinecarboxylic acid methyl ester
aprepitant
Conditions | Yield |
---|---|
In 5,5-dimethyl-1,3-cyclohexadiene for 3h; Reflux; | 98.4% |
In 5,5-dimethyl-1,3-cyclohexadiene at 130 - 139℃; for 4h; Temperature; | 97.7% |
In acetonitrile at 120 - 125℃; | 60.4% |
aprepitant
Conditions | Yield |
---|---|
With diethyl sulfate; triethylamine; lithium diisopropyl amide In dimethylsulfoxide-d6; 5,5-dimethyl-1,3-cyclohexadiene at 33℃; for 14h; Temperature; Inert atmosphere; | 97.9% |
aprepitant
Conditions | Yield |
---|---|
With triethylsilane; boron trifluoride diethyl etherate In acetonitrile at 0 - 35℃; for 5h; | 94% |
Conditions | Yield |
---|---|
With potassium carbonate In N,N-dimethyl-formamide at 0 - 10℃; for 4h; | 92% |
3-(chloromethyl)-1H-1,2,4-triazol-5(4H)-one
[2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine
aprepitant
Conditions | Yield |
---|---|
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 0.5h; | 68% |
[2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine
aprepitant
Conditions | Yield |
---|---|
Stage #1: N'-(1-amino-2-chloroethylidene)hydrazinecarboxylic acid methyl ester; [2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine With N-ethyl-N,N-diisopropylamine In acetonitrile at 20℃; for 3h; Stage #2: In acetonitrile at 110℃; under 1125.11 Torr; for 55h; Product distribution / selectivity; | 53% |
2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-4-fluorophenyl-4-2-(N-methylcarboxyactamidrazono)morpholine
aprepitant
Conditions | Yield |
---|---|
With pyrographite In methanol at 60℃; for 1h; | 0.96 kg |
In toluene at 140℃; for 3h; | |
at 135 - 137℃; for 2h; |
aprepitant
Conditions | Yield |
---|---|
With potassium carbonate In dimethyl sulfoxide at 20 - 23℃; for 1.5h; Product distribution / selectivity; |
3,5-bis(trifluoromethyl)phenyl methyl ketone
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 97 percent / borane-methyl sulfide complex; (S)-Me-CBS / various solvent(s); toluene / 1 h / -5 °C 2: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 5 steps 1: 97 percent / borane-methyl sulfide complex; (S)-Me-CBS / various solvent(s); toluene / 1 h / -5 °C 2: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 4: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 5: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 4 steps 1: 97 percent / borane-methyl sulfide complex; (S)-Me-CBS / various solvent(s); toluene / 1 h / -5 °C 2: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme |
(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 4 steps 1: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 3: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 4: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 3 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme |
4-benzyl-morpholine-2,3-dione
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 80 percent / lithium tri(sec-butyl)borohydride; sodium hydroxide; hydrogen peroxide / tetrahydrofuran; H2O / 1 h / 10 °C 2: acetonitrile / 5 - 34 °C 3: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 4: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 6 steps 1: 80 percent / lithium tri(sec-butyl)borohydride; sodium hydroxide; hydrogen peroxide / tetrahydrofuran; H2O / 1 h / 10 °C 2: acetonitrile / 5 - 34 °C 3: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 4: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 5: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 6: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 5 steps 1: 80 percent / lithium tri(sec-butyl)borohydride; sodium hydroxide; hydrogen peroxide / tetrahydrofuran; H2O / 1 h / 10 °C 2: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 3: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 4: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme |
N-Benzylethanolamine
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 76 percent / tetrahydrofuran; H2O / 21 h / Heating 2: acetonitrile / 5 - 34 °C 3: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 4: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 6 steps 1: 76 percent / tetrahydrofuran; H2O / 21 h / Heating 2: acetonitrile / 5 - 34 °C 3: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 4: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 5: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 6: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 5 steps 1: 76 percent / tetrahydrofuran; H2O / 21 h / Heating 2: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 3: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 4: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme |
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 2: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 2 steps 1: potassium carbonate / N,N-dimethyl-formamide / 10 - 20 °C 2: potassium hydroxide / ethanol; water / 0.2 h / 90 - 100 °C View Scheme | |
Multi-step reaction with 2 steps 1: potassium carbonate / N,N-dimethyl-formamide / 10 - 20 °C 2: potassium hydroxide / ethanol; water / 0.2 h / 90 - 100 °C View Scheme | |
Multi-step reaction with 2 steps 1: potassium carbonate; N-benzyl-N,N,N-triethylammonium chloride / 5,5-dimethyl-1,3-cyclohexadiene; dimethyl sulfoxide / 20 - 25 °C / Inert atmosphere 2: 5,5-dimethyl-1,3-cyclohexadiene / 2 h / 135 - 141 °C / Inert atmosphere View Scheme |
4-benzyl-2-hydroxy-morpholin-3-one
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: acetonitrile / 5 - 34 °C 2: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 5 steps 1: acetonitrile / 5 - 34 °C 2: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 4: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 5: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 4 steps 1: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 2: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme |
trifluoro-acetic acid 4-benzyl-3-oxo-morpholin-2-yl ester
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 4 steps 1: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 3: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 4: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme |
2,2,2-trichloro-acetimidic acid 4-benzyl-3-oxo-morpholin-2-yl ester
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 3 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 4 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 3: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 4: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 5 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C 3: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 4: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 5: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme |
(2S,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 4 steps 1: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C 2: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 3: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 4: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 3 steps 1: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 2: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 3: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: 5%-palladium/activated carbon; hydrogen / methanol; water / 4.5 h / 50 - 60 °C / 26252.6 Torr 2.1: sodium hydroxide / acetonitrile / 2.5 h / 30 - 40 °C 3.1: tetrahydrofuran / 1 h / 15 - 25 °C 3.2: 1 h / 20 - 65 °C 4.1: triethylsilane; boron trifluoride diethyl etherate / acetonitrile / 5 h / 0 - 35 °C View Scheme |
(2S,3R)-3-(4-fluorophenyl)-4-[(1R)-1-phenylethyl]-2-morpholinol
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: K2CO3 / toluene / 5 h / 20 °C 2: 14.3 g / BF3*Et2O / tetrahydrofuran / 1 h / -20 °C 3: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 4: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 5: DBU / dimethylformamide / 3 h / 0 - 20 °C 6: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme |
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1: DIBALH / toluene; tetrahydrofuran / 0.5 h / -20 °C 2: K2CO3 / toluene / 5 h / 20 °C 3: 14.3 g / BF3*Et2O / tetrahydrofuran / 1 h / -20 °C 4: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 5: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 6: DBU / dimethylformamide / 3 h / 0 - 20 °C 7: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme |
2,2,2-Trichloro-acetimidic acid (2R,3R)-3-(4-fluoro-phenyl)-4-((R)-1-phenyl-ethyl)-morpholin-2-yl ester
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: 14.3 g / BF3*Et2O / tetrahydrofuran / 1 h / -20 °C 2: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 3: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 4: DBU / dimethylformamide / 3 h / 0 - 20 °C 5: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme |
(2R)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-5,6-dihydro-2H-1,4-oxazine
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme | |
Multi-step reaction with 2 steps 1.1: potassium formate / palladium on carbon / ethanol; water / 2 h / 20 °C 2.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 3 h / 20 °C 2.2: 55 h / 110 °C / 1125.11 Torr View Scheme |
(2R,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 2: DBU / dimethylformamide / 3 h / 0 - 20 °C 3: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium hypochlorite; potassium carbonate / acetonitrile / 0.25 h 1.2: 14 h / 20 °C 2.1: potassium formate / palladium on carbon / ethanol; water / 2 h / 20 °C 3.1: potassium carbonate / N,N-dimethyl-formamide / 0.5 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium hypochlorite; potassium carbonate / acetonitrile / 0.25 h 1.2: 14 h / 20 °C 2.1: potassium formate / palladium on carbon / ethanol; water / 2 h / 20 °C 3.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 3 h / 20 °C 3.2: 55 h / 110 °C / 1125.11 Torr View Scheme |
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: DBU / dimethylformamide / 3 h / 0 - 20 °C 2: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme |
(2R,3R)-2-[(R)-1-(3,5-Bis-trifluoromethyl-phenyl)-ethoxy]-3-(4-fluoro-phenyl)-4-((R)-1-phenyl-ethyl)-morpholine
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: TsOH*H2O; hydrogen / 5percent Pd/C / ethanol; toluene / 3 h / 30 °C / 2068.65 Torr 2: NCS; K2CO3 / dimethylformamide / 0.5 h / 0 °C 3: DBU / dimethylformamide / 3 h / 0 - 20 °C 4: hydrogen / 5percent Pd/C / dimethylformamide; ethanol / 2 h / 20 °C / 2068.65 Torr View Scheme |
C27H31F7N4O4
aprepitant
Conditions | Yield |
---|---|
With potassium hydroxide In ethanol; water at 90 - 100℃; for 1h; Reagent/catalyst; Solvent; Large scale; |
aprepitant
Conditions | Yield |
---|---|
With potassium hydroxide In ethanol; water at 90 - 100℃; for 0.2h; |
(2S,3R)-4-benzyl-3-(4-fluorophenyl)morpholin-2-ol
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: boron trifluoride diethyl etherate / toluene / 1 h / -10 °C 2.1: hydrogen; toluene-4-sulfonic acid / palladium 10% on activated carbon / methanol / 16 h / 20 °C 3.1: sodium hypochlorite; potassium carbonate / acetonitrile / 0.25 h 3.2: 14 h / 20 °C 4.1: potassium formate / palladium on carbon / ethanol; water / 2 h / 20 °C 5.1: potassium carbonate / N,N-dimethyl-formamide / 0.5 h / 20 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: boron trifluoride diethyl etherate / toluene / 1 h / -10 °C 2.1: hydrogen; toluene-4-sulfonic acid / palladium 10% on activated carbon / methanol / 16 h / 20 °C 3.1: sodium hypochlorite; potassium carbonate / acetonitrile / 0.25 h 3.2: 14 h / 20 °C 4.1: potassium formate / palladium on carbon / ethanol; water / 2 h / 20 °C 5.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 3 h / 20 °C 5.2: 55 h / 110 °C / 1125.11 Torr View Scheme |
Conditions | Yield |
---|---|
Stage #1: aprepitant With dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate; sodium hexamethyldisilazane In tetrahydrofuran at -3℃; for 2h; Stage #2: 1-deoxy-1-(methylamino)-D-glucitol With palladium 10% on activated carbon; hydrogen In methanol; water for 4h; | 98% |
dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate
aprepitant
[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonic acid bis(phenylmethyl)ester
Conditions | Yield |
---|---|
With sodium hexamethyldisilazane In tetrahydrofuran at 0℃; for 1h; Temperature; Inert atmosphere; | 93.6% |
With sodium hexamethyldisilazane In tetrahydrofuran at 0℃; for 1h; Temperature; Inert atmosphere; | 93.6% |
With sodium hexamethyldisilazane In tetrahydrofuran at 0℃; for 0.25h; phosphorylation; | 90% |
Dibenzyl phosphite
aprepitant
[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonic acid bis(phenylmethyl)ester
Conditions | Yield |
---|---|
With triethylamine In tetrachloromethane; dichloromethane at 0 - 10℃; Reagent/catalyst; Solvent; | 92.4% |
Conditions | Yield |
---|---|
With N-ethyl-N,N-diisopropylamine In tert-butyl methyl ether at 0 - 30℃; | 90.6% |
Conditions | Yield |
---|---|
With dmap In chloroform at 0 - 20℃; | 90.4% |
dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate
aprepitant
Conditions | Yield |
---|---|
Stage #1: aprepitant With lithium hydroxide monohydrate In 1-methyl-pyrrolidin-2-one at 20℃; for 0.5h; Stage #2: dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate In 1-methyl-pyrrolidin-2-one at 25 - 30℃; for 0.5h; Quantum yield; | 87.4% |
aprepitant
Conditions | Yield |
---|---|
With dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate; sodium hexamethyldisilazane In tetrahydrofuran at -3℃; for 2h; | 86.7% |
Multi-step reaction with 3 steps 1: sodium hexamethyldisilazane / tetrahydrofuran / 3.5 h / -20 °C 2: hydrogen / palladium 10% on activated carbon / methanol / 1 h / 5171.62 Torr 3: hydrogenchloride / water; methanol / 0.08 h / 0 - 5 °C / pH 1 View Scheme | |
Multi-step reaction with 2 steps 1: sodium hexamethyldisilazane / tetrahydrofuran / 1 h / 0 °C / Inert atmosphere 2: borane pyridine; methanol / 2 h / 20 °C / Inert atmosphere View Scheme |
Conditions | Yield |
---|---|
Stage #1: aprepitant With sodium hexamethyldisilazane In tetrahydrofuran at -5 - 5℃; for 0.5h; Inert atmosphere; Cooling with ice; Stage #2: C26H22ClO3P In tetrahydrofuran at 5 - 20℃; for 1h; Solvent; | 82% |
Conditions | Yield |
---|---|
With triethylamine In tetrachloromethane; dichloromethane at 0 - 10℃; Reagent/catalyst; Solvent; | 81.1% |
aprepitant
Conditions | Yield |
---|---|
With deuteroacetic acid; magnesium In dimethylsulfoxide-d6; d(4)-methanol; water-d2 at 20℃; for 2h; regioselective reaction; | 43% |
aprepitant
Conditions | Yield |
---|---|
With magnesium; acetic acid In water; dimethyl sulfoxide at 20℃; for 2h; regioselective reaction; | 41% |
dibenzyl [[bis(benzyloxy)phosphoryl]oxy]phosphonate
aprepitant
A
[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonic acid bis(phenylmethyl)ester
Conditions | Yield |
---|---|
With n-butyllithium In tetrahydrofuran; hexane at 20℃; for 0.75h; phosphorylation; | A 39% B 5 % Chromat. |
aprepitant
Conditions | Yield |
---|---|
With magnesium; acetic acid In water; dimethyl sulfoxide at 20℃; for 5h; regioselective reaction; | A 16% B 22% |
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