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:US-2024279179-A1 优先权日:2020-12-22 标题 :Synthesis and use of 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine derivative
专利号:CN-112645866-B 优先权日:2020-12-22 标 题:Synthesis and application of 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine derivatives
专利号:EP-4269391-A1 优先权日:2020-12-22 标 题 :Synthesis and use of 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine derivative
专利号:CN-112645866-A 优先权日:2020-12-22 标题 :Synthesis and application of 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine derivatives
参考文献:10.1007/s40843-025-3248-y 摘要:Zhang Q, Huang T, Liu Z, Feng Y, Yu Y, Li L. Hydrogen bonding evolution and efficient blue light emission in a series of Zn-based organic–inorganic hybrid metal halide crystals. Sci. China Mater. 2025 Feb 17;68(4):1004–11. doi: 10.1007/s40843-025-3248-y.