专利号:US-8309716-B2 优先权日:2005-07-29 标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis 发明人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J 权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER 摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
专利号:US-9828380-B2 优先权日:2015-04-10 标题 :Efficient method for the preparation of tofacitinib citrate 发明人:BONANOMI JACOPO; DEFIORE STELLA; NOVO BARBARA 权利人:OLON SPA 摘要:Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises:n 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)
专利号:WO-2025003177-A1 优先权日:2023-06-27 标题:Benzyl (3-(methyl(7h-pyrrolo[2,3-d]pyrimidin-4yl)amino)cyclobutyl) carbamate or a salt thereof, method for the preparation thereof, and use thereof in the synthesis of abrocitinib
专利号:CN-109608468-A 优先权日:2018-12-29 标 题 :A kind of tofacitinib citrate impurity and its synthesis method and use
专利号:US-12233062-B2 优先权日:2018-09-26 标 题 :Heterocyclic derivatives useful as SHP2 inhibitors 发明人:HAN HUIFENG; GAO PANLIANG; MA CUNBO; KANG DI 权利人:JACOBIO PHARMACEUTICALS CO LTD 摘要:This invention provides a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention provides a pharmaceutical composition comprising the said compound.
专利号:AR-056004-A1 优先权日:2005-07-29 标 题 :PIRROLO DERIVATIVES [2, 3 -D] PYRIMIDINE, SYNTHESIS METHODS OF THE SAME AND ITS PREPARATION INTERMEDIARIES