专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:WO-2019073011-A1 优先权日:2017-10-12 标题:ENZYMATIC SYNTHESIS OF LIPOLANTHIPEPTIDES 发明人:JUNGMANN NATALIA; MAINZ ANDI; WIEBACH VINCENT; SÜSSMUTH RODERICH 权利人:DEINOVE SA 摘要:The present invention relates to methods of producing lipolanthipeptide compounds and in particular to the enzymatic activities involved in the synthesis of these compounds.
专利号:US-9221821-B2 优先权日:2012-06-05 标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds 发明人:DIEP NHUT; KALYAN YURIY B 权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD 摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
专利号:US-12410131-B2 优先权日:2021-10-21 标题:Method for preparation of trans-n-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as intermediate of halofuginone 发明人:FENG YU; XU HONG; WU JIAXUAN; SONG DANHUI; ZHONG WEIHUI; LING FEI; XU CHAO 权利人:CHENGDA PHARMACEUTICALS CO LTD 摘要:The present disclosure relates to the field of drug synthesis, and discloses a method for the preparation of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as an intermediate of halofuginone. In the preparation method according to the present disclosure, for the first time, trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as shown in Formula I is obtained from amino-substituted pentanal and a thiazolyl sulfoxide compound as raw materials by Mislow-Evans rearrangement reaction and subsequent Lewis acid catalysis. The method for the preparation of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as an intermediate of halofuginone according to the present disclosure has high yields and stable qualities, provides a new reference route for the synthesis of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone, avoids the reduction of pyridine, and overcomes the disadvantage of requiring the use of an expensive metal catalyst Rh/Al2O3.
专利号:EP-0389197-A1 优先权日:1989-03-20 标 题:Recovery of difluoro sugar 发明人:NAGARAJAN RAMAKRISHNAN 权利人:LILLY CO ELI 摘要:A process for recycling the difluoro sugar in the synthesis of 2,2-difluoronucleosides proceeds by removing the base moiety from α-difluoronucleosides by reduction and hydrolysis, followed by oxidation to put the difluoro sugar in a form conveniently recycled into the synthesis, and intermediates useful therefor.
摘要:Ipaktschi, J.; Saidi, M. R., Science of Synthesis Knowledge Updates, (2012) 4, 448. 摘要:Shen, Q.; Guo, F.; Hartwig, J. F., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 188. 摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 165. 摘要:Shang, Y.; Ren, Y.; Su, W., Science of Synthesis: Special Topics, (2022) 1, 224. 摘要:Stankevič, M.; Włodarczyk, A., Science of Synthesis: Knowledge Updates, (2024) 1, 426.