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:1187594-09-7
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inquiry1. DMF is available. Hangzhou Huarong Pharm Co., Ltd. established since 2009 , has been always focusing on supplying products and services to our clients in the field of small molecule drug. Huarong Pharm has built platforms for the research, d
Jinlan Pharm-Drugs Technology Co.,Limited (with its export company Hangzhou Royall Import & Export Co.,Ltd.)is located in Hangzhou, Zhejiang Province. Neighboring Ningbo port, Shanghai port, Hangzhou Xiaoshan Int’l Airport and Shanghai Pu
Luhan Pharmachem Co., Ltd. owns strong elite professional quality sales force, has the customer base from the US, Europe, Japan, Southeast Asia, Korea, Hong Kong, Taiwan and other countries and regions, the company operates in accordance with the mod
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:1187594-09-7
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inquiryItems Standard Result Assay 98%min ----------------------------------------------------------------------------------------------
Cas:1187594-09-7
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inquiryProduct Description: Name Baricitinib CAS NO. 1187594-09-7 Mol. formula
Cas:1187594-09-7
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inquiryUnique advantages for Baricitinib Cas 1187594-09-7 Guaranteed purity High quality & competitive price Quality control Fast feedback Prompt shipment Appearance:White or off-white crystalline powder Storage:N/A Package:10g,100g,1kg/foil
Cas:1187594-09-7
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inquiryBaricitinib CAS:1187594-09-7 Name Baricitinib Synonyms INCB 028050; LY 3009104; 1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl
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&D b
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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
Shanghai 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
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inquiry
Cas:1187594-09-7
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inquiryBaricitinib The production of high yield Baricitinib Chinese Name: Baricitinib English Name: Baricitinib CAS: 1187594-09-7 Molecular formula: C16H17N7O2S Molecular weight: 371.41688 EINECS: 1592732-453-0 Character: white
Cas:1187594-09-7
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inquiryProduct Name: Baricitinib Synonyms: aricitinib (LY3009104, INCB028050);Baricitinib Chemical Structure;Barrickini;1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile;Baricitinib;INCB 028050;LY 3009104;B
Cas:1187594-09-7
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inquiryBaricitinib Basic information Overview Indication and administration Pharmacodynamics Safety References Product Name: Baricitinib Synonyms: 1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile;Bari
Our Advantage Rich Experience Our products are sold all over Europe,North&South America, Sino-East, Asia and pacific area as well as Africa,we establish long term. Quality service Company cooperates with research institutes. We strictly con
Cas:1187594-09-7
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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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inquiryName: Baricitinib Synonyms: 2-(3-(4-(7H-Pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile CAS:1187594-09-7 MF: C16H17N7O2S Appearance: white powder Storage:Store in cool and dry place, away from sun
Appearance:White or off-white powder Storage:R.T Package:500g/bottle Application:Inhibitor Transportation:Express/Sea/Air Port:Any port in China
Cas:1187594-09-7
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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:powder Storage:Store in sealed containers at cool & dry pla
Cas:1187594-09-7
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inquiryHanways chempharm is a specialized company concentrating on the R&D, production, marketing and technical service of APIs and pharmaceutical intermediates. The marketing department is located in Wuhan. We have two GMP facilities in Hubei Pr
Cas:1187594-09-7
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inquiry1,In No Less five years exporting experience. 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Appearance:White powder Storage:storage in a dr
Cas:1187594-09-7
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inquiryWe are the manufacturers and suppliers of API in China, and warehouse in Germany and USA of California, which can quickly and safely deliver to your address 1.High quality and competitive price. 2.Free sample for your evaluation. 3.Promptly delivery
Cas:1187594-09-7
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Type:Trading Company
inquiryProduct Name: Baricitinib Synonyms: 1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile;Baricitinib;INCB 028050;LY 3009104;BARICITINIB;INCB28050;LY3009104;Baricitinib (LY3009104);2-(3-(4-(3H-Pyrrolo
Our company has been in existence for 10 years since its establishment. We have our own unique team. The company integrates independent research and development, production and sales. We have established famous brands at home and abroad. At present,
Baricitinib CAS:1187594-09-7 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 intermediat
Cas:1187594-09-7
Min.Order:1 Gram
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Type:Lab/Research institutions
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
Henan 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
Cas:1187594-09-7
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Type:Lab/Research institutions
inquiryConditions | Yield |
---|---|
With tetrakis(triphenylphosphine) palladium(0); potassium carbonate In 1,4-dioxane; water at 80 - 85℃; for 5h; | 99% |
With tetrakis(triphenylphosphine) palladium(0); cesium fluoride In water; toluene; tert-butyl alcohol at 100℃; for 48h; Concentration; Temperature; Solvent; Reagent/catalyst; Suzuki Coupling; Inert atmosphere; | 90% |
With potassium phosphate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 In tetrahydrofuran; water at 90℃; for 19h; Autoclave; Inert atmosphere; | 90% |
With tetrakis(triphenylphosphine) palladium(0); cesium fluoride In water; toluene; tert-butyl alcohol for 48h; Suzuki Coupling; Reflux; Inert atmosphere; | 84% |
Baricitinib
Conditions | Yield |
---|---|
With hydrogenchloride In ethanol at 40 - 45℃; | 93% |
With hydrogenchloride In ethanol at 40 - 45℃; | 93% |
In water; butan-1-ol at 90℃; | 92.7% |
2-[1-(ethanesulfonyl)azetidin-3-ylidene]acetonitrile
Baricitinib
Conditions | Yield |
---|---|
Stage #1: C14H15N5O2 With potassium carbonate In acetonitrile at 20℃; for 0.5h; Stage #2: 2-[1-(ethanesulfonyl)azetidin-3-ylidene]acetonitrile With 1,8-diazabicyclo[5.4.0]undec-7-ene In acetonitrile at 40℃; for 8h; | 91.2% |
(4-{1-[3-(cyanomethyl)-1-(ethylsulphonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate
Baricitinib
Conditions | Yield |
---|---|
Stage #1: (4-{1-[3-(cyanomethyl)-1-(ethylsulphonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate With water; sodium hydroxide In tetrahydrofuran; methanol at 20℃; for 2 - 3h; Stage #2: With hydrogenchloride In tetrahydrofuran; methanol; water at 20℃; for 0.5h; pH=7 - 7.5; Product distribution / selectivity; | 86% |
With sodium hydroxide In tetrahydrofuran; methanol at 20 - 25℃; for 3h; | 81% |
With sodium hydroxide In tetrahydrofuran; methanol; water at 20 - 30℃; |
2-(1-(ethylsulfonyl)-3-(4-(7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile
Baricitinib
Conditions | Yield |
---|---|
Stage #1: 2-[1-ethanesulfonyl-3-[4-(7-[(2-(trimethylsilyl)ethoxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl]acetonitrile With lithium tetrafluoroborate; water In acetonitrile at 75℃; Stage #2: With ammonium hydroxide; water In acetonitrile at 0 - 10℃; pH=9 - 10; Product distribution / selectivity; | 83.8% |
Baricitinib
Conditions | Yield |
---|---|
With tetrabutyl ammonium fluoride In tetrahydrofuran at 50 - 55℃; | 83% |
Baricitinib
Conditions | Yield |
---|---|
With tetrabutyl ammonium fluoride In 2-methyltetrahydrofuran Reflux; | 81.2% |
Baricitinib
Conditions | Yield |
---|---|
With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium phosphate In water; N,N-dimethyl-formamide at 85 - 90℃; Inert atmosphere; | 76% |
Conditions | Yield |
---|---|
With palladium diacetate; caesium carbonate; 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene In N,N-dimethyl acetamide; water at 95 - 100℃; Inert atmosphere; | 73% |
Conditions | Yield |
---|---|
Stage #1: 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile dihydrochloride salt; Ethanesulfonyl chloride With N-ethyl-N,N-diisopropylamine In acetonitrile at 0 - 5℃; for 6h; Stage #2: With ammonium hydroxide In acetonitrile at 20℃; for 4h; | 65% |
Conditions | Yield |
---|---|
Stage #1: 3-[4-[7-(hydroxymethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-1H-pyrazol-1-yl]-3-azetidineacetonitrile dihydrochloride; Ethanesulfonyl chloride With N-ethyl-N,N-diisopropylamine In acetonitrile at 0 - 5℃; for 6h; Stage #2: With ammonium hydroxide In acetonitrile at 20℃; for 4h; | 65% |
3-(cyanomethylene)azetidine-1-carboxylic acid tert-butyl ester
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: trifluoroacetic acid / dichloromethane / 5 h / 20 °C 2: N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 20 °C 3: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile; isopropyl alcohol / 4 h / 60 °C 4: tetrakis(triphenylphosphine) palladium(0); cesium fluoride / tert-butyl alcohol; water; toluene / 48 h / Reflux; Inert atmosphere View Scheme | |
Multi-step reaction with 4 steps 1: trifluoroacetic acid / acetonitrile / 4 h / 20 °C 2: N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 5 °C 3: 1,8-diazabicyclo[5.4.0]undec-7-ene / isopropyl alcohol / 3.5 h / 20 - 60 °C 4: cesium fluoride; tetrakis(triphenylphosphine) palladium(0) / toluene; water; tert-butyl alcohol / 48 h / 100 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 4 steps 1.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / isopropyl alcohol / Reflux 2.1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / isopropyl alcohol; water / 1 h / Reflux 3.1: hydrogenchloride / isopropyl alcohol; water; methanol / 20 - 25 °C 3.2: 20 - 25 °C 4.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 6 h / 0 - 5 °C 4.2: 4 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / isopropyl alcohol / Reflux 2.1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / isopropyl alcohol; water / 1 h / Reflux 3.1: hydrogenchloride / isopropyl alcohol; water; methanol / 20 - 25 °C 3.2: 20 - 25 °C 4.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 6 h / 0 - 5 °C 4.2: 4 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / isopropyl alcohol / Reflux 2.1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / 1,4-dioxane; water / 1 h / Reflux 3.1: hydrogenchloride / 1,4-dioxane; water / 15 - 20 °C 4.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 6 h / 0 - 5 °C 4.2: 4 h / 20 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 20 °C 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile; isopropyl alcohol / 4 h / 60 °C 3: tetrakis(triphenylphosphine) palladium(0); cesium fluoride / tert-butyl alcohol; water; toluene / 48 h / Reflux; Inert atmosphere View Scheme | |
Multi-step reaction with 3 steps 1: N-ethyl-N,N-diisopropylamine / acetonitrile / 0 - 5 °C 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / isopropyl alcohol / 3.5 h / 20 - 60 °C 3: cesium fluoride; tetrakis(triphenylphosphine) palladium(0) / toluene; water; tert-butyl alcohol / 48 h / 100 °C / Inert atmosphere View Scheme |
2-[1-(ethanesulfonyl)azetidin-3-ylidene]acetonitrile
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 1,8-diazabicyclo[5.4.0]undec-7-ene / isopropyl alcohol / 3.5 h / 20 - 60 °C 2: cesium fluoride; tetrakis(triphenylphosphine) palladium(0) / toluene; water; tert-butyl alcohol / 48 h / 100 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 2 steps 1: N,N,N′,N′-tetramethyl-N″-tert-butylguanidine / tetrahydrofuran / 3 h / 65 °C 2: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium phosphate / water; tetrahydrofuran / 19 h / 90 °C / Autoclave; Inert atmosphere View Scheme | |
Multi-step reaction with 3 steps 1: N,N,N′,N′-tetramethyl-N″-tert-butylguanidine / tetrahydrofuran / 3 h / 65 °C 2: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 / 9 h / 60 °C 3: water; butan-1-ol / 90 °C View Scheme |
4-chloro-1H-pyrrolo[2,3-d]pyrimidine
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: potassium phosphate / water; tetrahydrofuran / 17 h / 20 - 25 °C 2: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 / 9 h / 60 °C 3: water; butan-1-ol / 90 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: potassium tert-butylate / tetrahydrofuran / 0.33 h / 20 °C 1.2: 3 h 2.1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / water; N,N-dimethyl-formamide / 4 h / 20 - 85 °C 3.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / 14 h / 20 °C 4.1: hydrogenchloride / water; ethanol / 2 h / Reflux 5.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C 6.1: tetrabutyl ammonium fluoride / 2-methyltetrahydrofuran / Reflux View Scheme | |
Multi-step reaction with 3 steps 1.1: dipotassium hydrogenphosphate / tetrahydrofuran; water / 12 h / 20 °C 2.1: hydrazine hydrate / 8 h / Reflux 3.1: potassium carbonate / acetonitrile / 0.5 h / 20 °C 3.2: 8 h / 40 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: 2,2,6,6-Tetramethyl-1-piperidinyloxy free radical / ethyl acetate / 2 h 1.2: 3.5 h / 3 - 11 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / isopropyl alcohol / 20 h / 0 - 10 °C 3.1: N,N,N′,N′-tetramethyl-N″-tert-butylguanidine / tetrahydrofuran / 3 h / 65 °C 4.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium phosphate / water; tetrahydrofuran / 19 h / 90 °C / Autoclave; Inert atmosphere View Scheme | |
Multi-step reaction with 5 steps 1.1: 2,2,6,6-Tetramethyl-1-piperidinyloxy free radical / ethyl acetate / 2 h 1.2: 3.5 h / 3 - 11 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / isopropyl alcohol / 20 h / 0 - 10 °C 3.1: N,N,N′,N′-tetramethyl-N″-tert-butylguanidine / tetrahydrofuran / 3 h / 65 °C 4.1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 / 9 h / 60 °C 5.1: water; butan-1-ol / 90 °C View Scheme | |
Multi-step reaction with 4 steps 1: sulfur trioxide pyridine complex; triethylamine / dichloromethane / -5 - 20 °C 2: dichloromethane / 20 °C 3: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 4: palladium diacetate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; caesium carbonate / water; N,N-dimethyl acetamide / 95 - 100 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 5 steps 1: sulfur trioxide pyridine complex; triethylamine / dichloromethane / -5 - 20 °C 2: dichloromethane / 20 °C 3: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 4: palladium diacetate; tricyclohexylphosphine; potassium phosphate / water; 1,4-dioxane / 90 - 100 °C / Inert atmosphere 5: hydrogenchloride / ethanol / 40 - 45 °C View Scheme | |
Multi-step reaction with 5 steps 1: sulfur trioxide pyridine complex; triethylamine / dichloromethane / -5 - 20 °C 2: dichloromethane / 20 °C 3: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 4: palladium diacetate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; caesium carbonate / water; Isopropyl acetate / 95 - 100 °C 5: tetrabutyl ammonium fluoride / tetrahydrofuran / 50 - 55 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: N-ethyl-N,N-diisopropylamine / isopropyl alcohol / 20 h / 0 - 10 °C 2: N,N,N′,N′-tetramethyl-N″-tert-butylguanidine / tetrahydrofuran / 3 h / 65 °C 3: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; potassium phosphate / water; tetrahydrofuran / 19 h / 90 °C / Autoclave; Inert atmosphere View Scheme | |
Multi-step reaction with 4 steps 1: N-ethyl-N,N-diisopropylamine / isopropyl alcohol / 20 h / 0 - 10 °C 2: N,N,N′,N′-tetramethyl-N″-tert-butylguanidine / tetrahydrofuran / 3 h / 65 °C 3: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 / 9 h / 60 °C 4: water; butan-1-ol / 90 °C View Scheme | |
Multi-step reaction with 3 steps 1: piperidine / toluene / Reflux 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 3: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium phosphate / N,N-dimethyl-formamide; water / 85 - 90 °C / Inert atmosphere View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: isopropyl magnesium chloride - lithium chloride complex / tetrahydrofuran / -10 - 0 °C / Inert atmosphere 1.2: 20 °C / Inert atmosphere 2.1: palladium diacetate; caesium carbonate; CyJohnPhos / N,N-dimethyl-formamide; water / 90 - 100 °C / Inert atmosphere 3.1: hydrogenchloride / ethanol / 40 - 45 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: potassium acetate; palladium diacetate; CyJohnPhos / N,N-dimethyl-formamide / 60 - 65 °C / Inert atmosphere 1.2: 95 - 100 °C / Inert atmosphere 2.1: hydrogenchloride / ethanol / 40 - 45 °C View Scheme | |
Multi-step reaction with 3 steps 1: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / tetrahydrofuran / 60 - 65 °C / Inert atmosphere 2: palladium diacetate; caesium carbonate; CyJohnPhos / N,N-dimethyl-formamide; water / 90 - 100 °C / Inert atmosphere 3: hydrogenchloride / ethanol / 40 - 45 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: palladium diacetate; caesium carbonate; CyJohnPhos / N,N-dimethyl-formamide; water / 90 - 100 °C / Inert atmosphere 2: hydrogenchloride / ethanol / 40 - 45 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: potassium tert-butylate / N,N-dimethyl-formamide / 0 - 20 °C 2: sulfur trioxide pyridine complex; triethylamine / dichloromethane / -5 - 20 °C 3: dichloromethane / 20 °C 4: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 5: palladium diacetate; 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; caesium carbonate / water; N,N-dimethyl acetamide / 95 - 100 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 6 steps 1: potassium tert-butylate / N,N-dimethyl-formamide / 0 - 20 °C 2: sulfur trioxide pyridine complex; triethylamine / dichloromethane / -5 - 20 °C 3: dichloromethane / 20 °C 4: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 5: palladium diacetate; 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; caesium carbonate / water; Isopropyl acetate / 95 - 100 °C 6: tetrabutyl ammonium fluoride / tetrahydrofuran / 50 - 55 °C View Scheme | |
Multi-step reaction with 6 steps 1: potassium tert-butylate / N,N-dimethyl-formamide / 0 - 20 °C 2: sulfur trioxide pyridine complex; triethylamine / dichloromethane / -5 - 20 °C 3: dichloromethane / 20 °C 4: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 35 - 40 °C 5: palladium diacetate; tricyclohexylphosphine; potassium phosphate / water; 1,4-dioxane / 90 - 100 °C / Inert atmosphere 6: hydrogenchloride / ethanol / 40 - 45 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: palladium diacetate; tricyclohexylphosphine; potassium phosphate / water; 1,4-dioxane / 90 - 100 °C / Inert atmosphere 2: hydrogenchloride / ethanol / 40 - 45 °C View Scheme | |
Multi-step reaction with 2 steps 1: palladium diacetate; 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; caesium carbonate / water; Isopropyl acetate / 95 - 100 °C 2: tetrabutyl ammonium fluoride / tetrahydrofuran / 50 - 55 °C View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: hydrogenchloride / water; ethanol / 2 h / Reflux 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C 3: tetrabutyl ammonium fluoride / 2-methyltetrahydrofuran / Reflux View Scheme |
4-chloro-7-(phenylsulfonyl)-7H-pyrrolo [2,3-d]pyrimidine
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / water; N,N-dimethyl-formamide / 4 h / 20 - 85 °C 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / 14 h / 20 °C 3: hydrogenchloride / water; ethanol / 2 h / Reflux 4: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C 5: tetrabutyl ammonium fluoride / 2-methyltetrahydrofuran / Reflux View Scheme |
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 1,8-diazabicyclo[5.4.0]undec-7-ene / 14 h / 20 °C 2: hydrogenchloride / water; ethanol / 2 h / Reflux 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C 4: tetrabutyl ammonium fluoride / 2-methyltetrahydrofuran / Reflux View Scheme |
4-chloro-7H-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid tert-butyl ester
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: hydrazine hydrate / 8 h / Reflux 2.1: potassium carbonate / acetonitrile / 0.5 h / 20 °C 2.2: 8 h / 40 °C View Scheme |
methanol
(4-{1-[3-(cyanomethyl)-1-(ethylsulphonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate
A
Baricitinib
Conditions | Yield |
---|---|
With water; lithium hydroxide In acetonitrile Inert atmosphere; |
[4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl 2,2-dimethylpropanoate
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile; N,N-dimethyl-formamide / Inert atmosphere 2: lithium hydroxide; water / acetonitrile / Inert atmosphere View Scheme |
(4-(1-(1-ethoxyethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl pivalate
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: hydrogenchloride; water / tetrahydrofuran / Inert atmosphere 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile; N,N-dimethyl-formamide / Inert atmosphere 3: lithium hydroxide; water / acetonitrile / Inert atmosphere View Scheme |
(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate
Baricitinib
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: tetrakis(triphenylphosphine) palladium(0); potassium carbonate / Inert atmosphere 2: hydrogenchloride; water / tetrahydrofuran / Inert atmosphere 3: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile; N,N-dimethyl-formamide / Inert atmosphere 4: lithium hydroxide; water / acetonitrile / Inert atmosphere View Scheme |
Baricitinib
benzenesulfonic acid
Conditions | Yield |
---|---|
In ethyl acetate at 20 - 22℃; for 2h; Solvent; Temperature; | 100% |
Baricitinib
{1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d] pyrimidin-)-1H-pyrazol-1-yl] azetidin-3-yl}acetonitrile phosphate
Conditions | Yield |
---|---|
With phosphoric acid In methanol; water; acetonitrile at 68℃; for 1h; Solvent; Temperature; | 99.2% |
With phosphoric acid In ethanol; acetonitrile at 70℃; for 2h; Product distribution / selectivity; | 93% |
With phosphoric acid In ethanol; acetonitrile at 70℃; for 2h; |
ethanesulfonic acid
Baricitinib
Conditions | Yield |
---|---|
In ethyl acetate at 20 - 22℃; for 2h; Solvent; Temperature; | 98.8% |
Baricitinib
Conditions | Yield |
---|---|
With phosphoric acid In propan-1-ol; ethanol at 68℃; for 1.5h; | 97.9% |
methanesulfonic acid
Baricitinib
Conditions | Yield |
---|---|
In isopropyl alcohol at 20 - 22℃; for 2h; Solvent; | 97.8% |
Baricitinib
toluene-4-sulfonic acid
Conditions | Yield |
---|---|
In acetonitrile at 20 - 22℃; for 3h; | 96.7% |
Baricitinib
(2E)-but-2-enedioic acid
Conditions | Yield |
---|---|
In acetonitrile for 0.5h; Reflux; | 96.7% |
In tetrahydrofuran for 1h; |
2-hydroxyethanesulfonic acid
Baricitinib
Conditions | Yield |
---|---|
In acetonitrile at 20 - 22℃; for 4h; | 90.8% |
Baricitinib
(2E)-but-2-enedioic acid
Conditions | Yield |
---|---|
In water; dimethyl sulfoxide at 5 - 60℃; Solvent; Temperature; | 86% |
Baricitinib
Conditions | Yield |
---|---|
With phosphoric acid In ethanol; acetonitrile at 70℃; for 2h; | 80% |
Conditions | Yield |
---|---|
Stage #1: Baricitinib In dichloromethane; acetonitrile for 0.25h; Cooling with ice; Stage #2: isobutyryl chloride In dichloromethane; acetonitrile at 20℃; | 72% |
Conditions | Yield |
---|---|
Stage #1: Baricitinib In dichloromethane; acetonitrile for 0.25h; Cooling with ice; Stage #2: With sodium hydride In dichloromethane; acetonitrile for 0.5h; Stage #3: chloromethyl n-butyrate In dichloromethane; acetonitrile at 20℃; | 68% |
Conditions | Yield |
---|---|
Stage #1: Baricitinib In dichloromethane; acetonitrile for 0.25h; Cooling with ice; Stage #2: With sodium hydride In dichloromethane; acetonitrile for 0.5h; Stage #3: Dimethyl chlorophosphate In dichloromethane; acetonitrile at 20℃; | 68% |
Baricitinib
citric acid
Conditions | Yield |
---|---|
In acetonitrile at 0℃; for 2h; Solvent; Temperature; Reflux; | 67% |
Conditions | Yield |
---|---|
Stage #1: Baricitinib In dichloromethane; acetonitrile for 0.25h; Cooling with ice; Stage #2: acetyl chloride In dichloromethane; acetonitrile at 20℃; | 64% |
Baricitinib
citric acid
Conditions | Yield |
---|---|
In acetonitrile at 20℃; for 18h; Solvent; Temperature; | 61% |
Baricitinib
Conditions | Yield |
---|---|
With dihydrogen peroxide; sodium hydroxide In methanol; dimethyl sulfoxide at 50℃; for 3h; Temperature; Reagent/catalyst; Solvent; | 58.4% |
Baricitinib
oxalic acid
Conditions | Yield |
---|---|
In acetonitrile at 20 - 22℃; for 2h; | 56.36% |
Baricitinib
Conditions | Yield |
---|---|
With Sodium trimetaphosphate; sodium carbonate In water at 45℃; | 51% |
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