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:WO-2008148560-A1 优先权日:2007-06-07 标题 :New hybrid compounds of nucleobases and organic redox molecules and their use 发明人:ASAFTEI SIMONA CARMEN 权利人:UNIV OSNABRUECK; ASAFTEI SIMONA CARMEN 摘要:The present invention relates to new compounds as well as methods for the synthesis of the same, said compounds comprise a redox active group, e.g. a 4,4-bipyridine (viologen), a 1,2-di(4-pyridyl)ethane, a 2,7-diazapyrene or 2,9-diazaperylene group and a N-heterocyclic nucleobase (HB), also referred to as base.
专利号:US-12441733-B2 优先权日:2018-03-26 标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors 发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
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:US-6271370-B1 优先权日:1999-05-11 标 题 :Process for the synthesis of nucleoside analogs 发明人:SCOTT ROBERT W 权利人:PFIZER 摘要:The present invention relates to an improved method for synthesizing nucleosides with a low α:β anomeric ratio. The method comprises coupling a protected furanosyl halide and an appropriately protected heterocycle in the presence of a nucleophilic polar solvent and a strong base.
专利号:US-10562904-B2 优先权日:2015-12-31 标 题:Synthesis process of ruxolitinib 发明人:ZHANG XIQUAN; ZHANG AIMING; ZHOU ZHOU; YANG LEILEI; YAO HUADONG; ZHU XUEYAN; WANG HUBO 权利人:CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD 摘要:The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).