Advantage : LIDE PHARMACEUTICALS LTD. is a mid-small manufacturing-type enterprise, engaged in pharmaceutical intermediates of R&D, custom-made and production, and also involving trading chemicals for export. We have established the R&
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inquiryThe product is the key intermediate for producing the Olaparib. and we have produced it for several times from 1-50kg per batch with high quality of above 99% purity . At the same time, the related impurities have been studied in detail. For the
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inquiry100% owned factory, regulatory compliance and be audited.Appearance:Off- white powder Application:Commercial
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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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inquiryProduct description: Product name 2-Fluoro-5-(4-oxo-3,4-dihydrophthalazin-1-ylmethyl)benzoic acid CAS number 763114-26-7 Assay ≥99% Appearance White powder Capacity 200mt/year A
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inquiry2-Fluoro-5-(4-oxo-3,4-dihydrophthalazin-1-ylmethyl)benzoic acid CAS No.:763114-26-7 Name: 2-Fluoro-5-(4-oxo-3,4-dihydrophthalazin-1-ylmethyl)benzoic acid Molecular Structure
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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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inquiryCangzhou Enke Pharma Tech Co.,ltd. is located in Cangzhou City, Hebei province ,where is a famous petroleum chemical industry city in China. Enke Pharma a high-tech enterprise ,and we are dedicated to developing and manufacturing new ap
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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
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inquiryOur 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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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
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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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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 crystalline powder Storage:Store in sealed containers
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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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inquiry2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)Methyl)benzoic acid CAS:763114-26-7 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermedi
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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
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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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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:As
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Min.Order:100 Gram
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inquiry2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)Methyl)benzoic acid is one of the most competitive products in our company, we can supply it with good quality and best price. Appearance:White to pink solid Storage:Room temperature, Keep in Dark Place.
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inquiryOur 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-
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inquiry1,we produce and sell good chemicals around the world. 2,our success rate is about 95%. this means, if customer order is accepted, the probability that the customer will obtain the ordered substances, is 95%. 3,our staff consists of highly qualifie
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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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inquiryA substitute for perfluorooctanoic acid, mainly used as a surfactant, dispersant, additive, etc Appearance:White solid or Colorless liquid Purity:99.3 % We will ship the goods in a timely manner as required We can provide relevant documents acc
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inquiryHigh purity 763114-26-7 low price 2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)Methyl)benzoic acid good supplier 5-[(3, 4-dihydro-4-oxo-1-phthalazinyl) methyl]-2-fluorobenzoic acid is an intermediate in organic synthesis and pharmaceutical interme
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inquiryMassive Chemical is certified with ISO9001 and ISO14001 manufacturer for this product. We will offer all documents as requirement for the materials which includes, Certificate of Analysis, Material Safety Data Sheet, and Method of Analysis and
Cas:763114-26-7
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inquiryZibo 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:763114-26-7
Min.Order:10 Gram
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inquiryWe are one of a few suppliers that can offer custom synthesis service of this product We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research. We are committed to prov
Cas:763114-26-7
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inquiryProduct name: 2-Fluoro-5-((4-Oxo-3,4-Dihydrophthalazin-1-yl)Methyl)Benzoic Acid CAS No.:763114-26-7 Molecule Formula:C16H11FN2O3 Molecule Weight:298.27 Purity: 99.0% Package: 25kg/drum Description:White crystalline powder Manufacture Standards
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Min.Order:1 Kilogram
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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,
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inquiry4-(3-bromo-4-fluorobenzyl)phthalazin-1(2H)-one
carbon dioxide
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: 4-(3-bromo-4-fluorobenzyl)phthalazin-1(2H)-one With n-butyllithium In diethyl ether; hexane at -40 - -30℃; for 0.5h; Stage #2: carbon dioxide In diethyl ether; hexane for 0.333333h; Stage #3: With hydrogenchloride In water at 20℃; for 0.5h; Temperature; | 95.1% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: methyl 2-fluoro-5-(3-oxo-3H-isobenzofuran-1-ylmethylene)benzoate With hydrazine hydrate In tetrahydrofuran; water at 8 - 25℃; for 4h; Stage #2: With sodium hydroxide In tetrahydrofuran; water; acetone at 40℃; for 3.3h; | 95% |
2-fluoro-5-(3-oxo-1,3-dihydroisobenzofuranylidene methyl)benzonitrile
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: 2-fluoro-5-(3-oxo-1,3-dihydroisobenzofuranylidene methyl)benzonitrile With water; sodium hydroxide at 90℃; for 1h; Stage #2: With hydrazine hydrate at 70℃; for 18h; | 93.7% |
Stage #1: 2-fluoro-5-(3-oxo-1,3-dihydroisobenzofuranylidene methyl)benzonitrile With sodium hydroxide In water at 90℃; for 1h; Stage #2: With hydrazine hydrate In water at 70℃; for 18h; | 93.69% |
Stage #1: 2-fluoro-5-(3-oxo-1,3-dihydroisobenzofuranylidene methyl)benzonitrile With hydrazine hydrate at 8 - 25℃; for 4h; Stage #2: With water; sodium hydroxide In acetone at 20 - 90℃; for 1h; | 91% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With sodium hydroxide In tetrahydrofuran; water at 20℃; | 93% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With potassium hydroxide In methanol for 6h; Reflux; | 90.5% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With sodium hydroxide; hydrazinium sulfate In water; isopropyl alcohol Reflux; | 85.1% |
dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphonate
2-fluoro-5-formyl-benzoic acid
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphonate; 2-fluoro-5-formyl-benzoic acid With triethylamine In tetrahydrofuran at 0 - 20℃; for 5h; Stage #2: With hydrazine hydrate In tetrahydrofuran at 70℃; for 3h; | 83% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: (Z)-2-fluoro-5-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrle; 2-fluoro-5-[(E)-(3-oxo-2-benzofuran-1-ylidene)methyl]benzonitrile With sodium hydroxide In water at 90℃; for 0.5h; Stage #2: With hydrazine In water at 70℃; for 18h; Stage #3: With hydrogenchloride at 20℃; for 0.166667h; pH=4; | 77% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With sodium hydroxide; hydrazine hydrate In water | 77% |
Stage #1: (Z)-2-fluoro-5-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrle With water; sodium hydroxide at 90℃; for 16h; Inert atmosphere; Stage #2: With hydrazine hydrate at 70℃; for 16h; Inert atmosphere; |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: 2-fluoro-4-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrile With water; sodium hydroxide at 90℃; for 1h; Stage #2: With hydrazine hydrate at 70℃; for 18h; | 77% |
4-(3-bromo-4-fluorobenzyl)phthalazin-1(2H)-one
carbon monoxide
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With bis-triphenylphosphine-palladium(II) chloride; ethanol at 110℃; under 9120.61 Torr; for 6h; Autoclave; | 71.1% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With hydrazine hydrate In tetrahydrofuran Heating; |
methyl phosphite
o-carboxybenzaldehyde
A
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
B
dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphonate
Conditions | Yield |
---|---|
With methanesulfonic acid; sodium methylate In methanol | A 95%, 95% B n/a |
2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzonitrile
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: 2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzonitrile With sodium hydroxide; water at 20 - 90℃; Stage #2: With hydrogenchloride; water at 60℃; for 0.666667h; | |
With hydrogenchloride; water at 20℃; | |
With sodium hydroxide In water |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With hydrazine hydrate at 70℃; for 18h; Inert atmosphere; | 30.1 g |
With hydrazine hydrate at 70℃; for 72h; Inert atmosphere; | 2 g |
o-carboxybenzaldehyde
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: sodium; methanol / 0.5 h / 0 - 20 °C / Inert atmosphere 2.1: triethylamine / tetrahydrofuran / 15 - 20 °C 3.1: sodium hydroxide; water / 1 h / 90 °C 3.2: 70 °C 3.3: 20 °C / pH 3 - 4 View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium methylate / methanol / 0.08 h / 0 °C / Inert atmosphere 1.2: 1 h / 20 °C 1.3: 10 °C / Cooling with ice 2.1: triethylamine / tetrahydrofuran / 1 h / 15 - 20 °C 3.1: sodium hydroxide / water / 1 h / 100 °C 3.2: 24 h / 70 °C 3.3: pH 4 View Scheme | |
Multi-step reaction with 5 steps 1: sodium / methanol / 0.5 h / 0 - 20 °C / Inert atmosphere 2: triethylamine / tetrahydrofuran / 15 - 20 °C 3: sodium hydroxide; water / 1 h / 90 °C 4: hydrazine hydrate / water / 70 °C 5: water; hydrogenchloride / 20 °C View Scheme |
2-fluoro-5-formylbenzonitrile
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: triethylamine / tetrahydrofuran / 15 - 20 °C 2.1: sodium hydroxide; water / 1 h / 90 °C 2.2: 70 °C 2.3: 20 °C / pH 3 - 4 View Scheme | |
Multi-step reaction with 4 steps 1: triethylamine / tetrahydrofuran / 15 - 20 °C 2: sodium hydroxide; water / 1 h / 90 °C 3: hydrazine hydrate / water / 70 °C 4: water; hydrogenchloride / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: Dimethyl phosphite; hydrogenchloride / water / 20 °C 1.2: 20 °C 2.1: sodium hydroxide / water / 20 - 70 °C 2.2: 20 - 70 °C / pH 4 - 6 View Scheme |
3-bromo-4-fluorobenzaldehyde
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: 1-methyl-pyrrolidin-2-one / 24 h / 170 °C 1.2: celite / 1 h / 80 °C 2.1: triethylamine / tetrahydrofuran / 15 - 20 °C 3.1: sodium hydroxide; water / 1 h / 90 °C 3.2: 70 °C 3.3: 20 °C / pH 3 - 4 View Scheme | |
Multi-step reaction with 5 steps 1: 1-methyl-pyrrolidin-2-one / 24 h / 170 °C 2: triethylamine / tetrahydrofuran / 15 - 20 °C 3: sodium hydroxide; water / 1 h / 90 °C 4: hydrazine hydrate / water / 70 °C 5: water; hydrogenchloride / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: triethylamine / tetrahydrofuran / 6 h / 30 °C 2.1: hydrazine hydrate / tetrahydrofuran / 1 h / 30 °C 2.2: 7 h / Reflux 3.1: n-butyllithium / diethyl ether; hexane / 0.5 h / -40 - -30 °C 3.2: 0.33 h 3.3: 0.5 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: triethylamine / tetrahydrofuran / 6 h / 30 °C 2.1: hydrazine hydrate / tetrahydrofuran / 1 h / 30 °C 2.2: 7 h / Reflux 3.1: bis-triphenylphosphine-palladium(II) chloride; ethanol / 6 h / 110 °C / 9120.61 Torr / Autoclave View Scheme |
dimethyl (3-oxo-1,3-dihydroisobenzofuran-1-yl)phosphonate
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: triethylamine / tetrahydrofuran / 15 - 20 °C 2.1: sodium hydroxide; water / 1 h / 90 °C 2.2: 70 °C 2.3: 20 °C / pH 3 - 4 View Scheme | |
Multi-step reaction with 2 steps 1.1: triethylamine / tetrahydrofuran / 1 h / 15 - 20 °C 2.1: sodium hydroxide / water / 1 h / 100 °C 2.2: 24 h / 70 °C 2.3: pH 4 View Scheme | |
Multi-step reaction with 4 steps 1: triethylamine / tetrahydrofuran / 15 - 20 °C 2: sodium hydroxide; water / 1 h / 90 °C 3: hydrazine hydrate / water / 70 °C 4: water; hydrogenchloride / 20 °C View Scheme |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: hydrazine hydrate / water / 70 °C 2: water; hydrogenchloride / 20 °C View Scheme |
2-fluoro-5-bromomethyl benzoic acid methyl ester
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: magnesium; triethylamine / acetonitrile / 2 h / 65 °C 2: sodium carbonate; [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II) / methanol; water / 4 h / Inert atmosphere; Reflux 3: sodium hydroxide / water; tetrahydrofuran / 20 °C View Scheme |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: sodium carbonate; [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II) / methanol; water / 4 h / Inert atmosphere; Reflux 2: sodium hydroxide / water; tetrahydrofuran / 20 °C View Scheme |
2,3-dihydrophthalazine-1,4-dione
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: trichlorophosphate / 4 h / 110 °C 2.1: zinc; ethylene dibromide; chloro-trimethyl-silane / tetrahydrofuran / 2 h / 0 °C 2.2: 2 h / 80 °C / Inert atmosphere 3.1: potassium hydroxide / methanol / 6 h / Reflux View Scheme |
1-chloro-4-phthalazinone
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: zinc; ethylene dibromide; chloro-trimethyl-silane / tetrahydrofuran / 2 h / 0 °C 1.2: 2 h / 80 °C / Inert atmosphere 2.1: potassium hydroxide / methanol / 6 h / Reflux View Scheme |
3-hydroxy-1(3H)-isobenzofuranone
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: dichloromethane / 0.42 h / 100 °C 2: triethylamine / dichloromethane / 0.33 h / 15 °C 3: sodium hydroxide; hydrazine hydrate / ethanol / 0.17 h / 70 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium methylate / methanol / 0.17 h / 0 °C 1.2: 1 h / 0 - 25 °C 2.1: triethylamine / tetrahydrofuran / 10 - 20 °C 3.1: sodium hydroxide; water / 1 h / 90 °C / Inert atmosphere 3.2: 18 h / 70 °C / Inert atmosphere 3.3: 0.17 h / 25 °C / pH 4 / Inert atmosphere View Scheme | |
Multi-step reaction with 4 steps 1.1: triethylamine; methanesulfonic acid / dichloromethane / 0.5 h 2.1: triethylamine / dichloromethane / 4 h / 6 - 20 °C 3.1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; carbon monoxide / methanol / 8 h / 80 °C / 2585.81 Torr / Inert atmosphere 4.1: hydrazine hydrate / water; tetrahydrofuran / 4 h / 8 - 25 °C 4.2: 3.3 h / 40 °C View Scheme |
phthalonitrile
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: potassium tert-butylate / toluene / 5 h / 50 - 80 °C 1.2: 5 h / 90 - 95 °C 2.1: hydrazine hydrate; hydrogenchloride / water / 10 h / 65 - 70 °C / pH 2.5 - 3 View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium tert-butylate / toluene / 5 h / 50 - 80 °C 1.2: 5 h / 90 - 95 °C 2.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 3.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 3.2: 1 h / 20 - 25 °C View Scheme |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: sodium methylate / toluene / 3 h / 55 - 85 °C 1.2: 4 h / 50 - 95 °C 2.1: hydrazine hydrate; hydrogenchloride / water / 10 h / 65 - 70 °C / pH 2.5 - 3 View Scheme | |
Multi-step reaction with 2 steps 1.1: sodium methylate / toluene / 4 h / 50 - 85 °C 1.2: 4 h / 50 - 85 °C 2.1: hydrazine hydrate; hydrogenchloride / water / 10 h / 65 - 70 °C / pH 2.5 - 3 View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium methylate / toluene / 3 h / 55 - 85 °C 1.2: 4 h / 50 - 95 °C 2.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 3.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 3.2: 1 h / 20 - 25 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium methylate / toluene / 4 h / 50 - 85 °C 1.2: 4 h / 50 - 85 °C 2.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 3.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 3.2: 1 h / 20 - 25 °C View Scheme |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With hydrogenchloride; hydrazine hydrate In water at 65 - 70℃; for 10h; pH=2.5 - 3; Temperature; Reagent/catalyst; | 27.8 g |
Multi-step reaction with 2 steps 1.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 2.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 2.2: 1 h / 20 - 25 °C View Scheme |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: sodium ethanolate / 1,2-dichloro-ethane / 6 h / 50 - 83 °C 1.2: 4 h / 50 - 83 °C 2.1: hydrazine hydrate; hydrogenchloride / water / 10 h / 65 - 70 °C / pH 2.5 - 3 View Scheme | |
Multi-step reaction with 3 steps 1.1: sodium ethanolate / 1,2-dichloro-ethane / 6 h / 50 - 83 °C 1.2: 4 h / 50 - 83 °C 2.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 3.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 3.2: 1 h / 20 - 25 °C View Scheme |
5-(cyanomethyl)-2-fluorobenzonitrile
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: potassium tert-butylate / toluene / 5 h / 50 - 80 °C 1.2: 5 h / 90 - 95 °C 2.1: hydrazine hydrate; hydrogenchloride / water / 10 h / 65 - 70 °C / pH 2.5 - 3 View Scheme | |
Multi-step reaction with 2 steps 1.1: potassium tert-butylate / tetrahydrofuran / 8 h / 50 - 64 °C 1.2: 5 h / 50 - 95 °C 2.1: hydrazine hydrate; hydrogenchloride / water / 10 h / 65 - 70 °C / pH 2.5 - 3 View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium tert-butylate / toluene / 5 h / 50 - 80 °C 1.2: 5 h / 90 - 95 °C 2.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 3.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 3.2: 1 h / 20 - 25 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: potassium tert-butylate / tetrahydrofuran / 8 h / 50 - 64 °C 1.2: 5 h / 50 - 95 °C 2.1: toluene-4-sulfonic acid / toluene; water / 7 h / 74 - 80 °C 3.1: hydrazine hydrate / toluene; water / 4 h / 30 - 45 °C 3.2: 1 h / 20 - 25 °C View Scheme |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
tert-butyl 1,6-diazaspiro[3.3]heptane-6-carboxylate
Conditions | Yield |
---|---|
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In tetrahydrofuran at 60℃; for 12h; | 98% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
tert-butyl 1,4-diazepine-1-carboxylate
tert-butyl 4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)-1,4-diazepane-1-carboxylate
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine In N,N-dimethyl-formamide at 20℃; for 2h; Inert atmosphere; | 97% |
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl acetamide | |
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 24h; | |
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 24h; |
4-HYDROXYPIPERIDINE
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
4-(4-fluoro-3-(4-hydroxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine In N,N-dimethyl acetamide at 20℃; for 17h; Product distribution / selectivity; | 97% |
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In ISOPROPYLAMIDE at 20℃; for 16h; Product distribution / selectivity; |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
1-t-Butoxycarbonylpiperazine
tert-butyl 4-[2’-fluoro-5’-[(4’’-oxo-3’’H-phthalazin-1’’-yl)methyl]benzoyl]piperazine-1-carboxylate
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine In N,N-dimethyl-formamide at 20℃; for 2h; Inert atmosphere; | 96% |
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine In N,N-dimethyl-formamide at 20℃; for 2h; | 96% |
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl acetamide at 15 - 25℃; for 2h; Product distribution / selectivity; | 78% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
methyl 2-(2-(pyrrolidin-1-yl)ethylamino)propanoate
3-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)phenyl)-5-methyl-1-(2-(pyrrolidin-1-yl)ethyl)imidazolidine-2,4-dione
Conditions | Yield |
---|---|
With diphenyl phosphoryl azide; triethylamine In acetonitrile at 85℃; for 1.25h; | 95% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
1-(cyclopropylcarbonyl)piperazine
Conditions | Yield |
---|---|
Stage #1: 2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid With 1,1'-carbonyldiimidazole In tetrahydrofuran for 0.5h; Stage #2: 1-(cyclopropylcarbonyl)piperazine In tetrahydrofuran at 20℃; for 3h; | 95% |
With pivaloyl chloride; triethylamine In ethanol; dichloromethane at 20℃; for 4h; | 91.5% |
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 30 - 50℃; | 81.9% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
cyclopropyl (piperazin-1-yl)methanone hydrochloride
Conditions | Yield |
---|---|
Stage #1: 2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In tetrahydrofuran at 25℃; for 1h; Stage #2: cyclopropyl (piperazin-1-yl)methanone hydrochloride With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20 - 25℃; for 5.5h; Reagent/catalyst; Temperature; Solvent; | 94.5% |
With triethylamine In dichloromethane at -10 - 20℃; for 4h; Solvent; | 92.2% |
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In acetonitrile at 5 - 20℃; Product distribution / selectivity; | |
With triethylamine; dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 8h; Solvent; Temperature; Reagent/catalyst; | 18.92 g |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
Stage #1: 2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid With pivaloyl chloride; N-ethyl-N,N-diisopropylamine In acetone at 0 - 20℃; for 3h; Stage #2: N-cyclopropanoylpiperazinium p-toluenesulfonate With N-ethyl-N,N-diisopropylamine In acetone at 0 - 20℃; for 3h; | 89.5% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
4-(2-(pyrrolidin-1-yl)ethoxy)piperidine
4-(4-fluoro-3-(4-(2-(pyrrolidin-1-yl)ethoxy)piperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide for 2h; | 89% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
1-(piperidin-1-yl)-2-(piperidin-4-yloxy)ethanone
4-(4-fluoro-3-(4-(2-oxo-2-(piperidin-1-yl)ethoxy)piperidine-1-carbonyl)benzyl)phthalazin-1 (2H)-one
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In ISOPROPYLAMIDE for 2h; | 89% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 25℃; for 6h; | 88% |
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 25℃; | 87.7% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; | 84.6% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 25℃; for 8h; | 84.6% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; | 83% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
4-(piperidin-4-yl)butan-1-ol
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; triethylamine In N,N-dimethyl-formamide at 25℃; Inert atmosphere; | 83% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide for 6h; | 82.5% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; | 81.3% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
1,2,3-Benzotriazole
Conditions | Yield |
---|---|
With thionyl chloride; triethylamine In dichloromethane at 0 - 20℃; Reagent/catalyst; | 81% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
2,7-diaza-spiro[3.5]nonane-7-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In tetrahydrofuran at 60℃; for 12h; | 81% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
4-(2-propenoxy)piperidine
C24H24FN3O3
Conditions | Yield |
---|---|
With O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide for 2h; | 80% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In tetrahydrofuran at 60℃; for 12h; | 79% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
2,8-diazaspiro[4,5]decane-8-carboxylic acid tert-butyl ester
Conditions | Yield |
---|---|
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In tetrahydrofuran at 60℃; for 12h; | 79% |
2-fluoro-5-[(4’-oxo-3’H-phthalazin-1’-yl)methyl]benzoic acid
Conditions | Yield |
---|---|
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 25℃; for 4h; | 79% |
With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 25℃; | 78.9% |
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