专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:US-2002103381-A1 优先权日:2000-11-30 标 题 :Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.
专利号:US-8084630-B2 优先权日:2007-05-31 标 题 :Process for the synthesis of ramelteon and its intermediates 发明人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL 权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL; TEVA PHARMA 摘要:The present invention provides processes and intermediates for the synthesis of ramelteon.
专利号:US-10059653-B2 优先权日:2015-01-20 标 题 :Process for the preparation of indanamine derivatives and new synthesis intermediates 发明人:BERTOLINI GIORGIO; CEREA PAOLANGELO; COLLI CORRADO; FELICIANI LAZZARO; GASSA FEDERICO; BIANCHI ALDO; COLOMBO FEDERICA; MAIORANA STEFANO; NISIC FILIPPO 权利人:LABORATORIO CHIMICO INT S P A; OLON SPA 摘要:Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I):
摘要:Chiba, S.; Narasaka, K., Science of Synthesis Knowledge Updates, (2011) 4, 451. 摘要:Rodríguez-Mata, M.; Gotor-Fernández, V., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 208. 摘要:Schmidberger, J. W.; Hepworth, L. J.; Green, A. P.; Flitsch, S. L., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 355. 摘要:Diéguez, M.; Bäckvall, J.-E.; Pàmies, O., Science of Synthesis, (2019) , 194. 摘要:Adriaensen, K.; De Vos, D., Science of Synthesis, (2022) , 150.