专利号:US-2012215002-A1 优先权日:2009-10-09 标 题:Synthesis of optically active intermediate for the preparation of montelukast 发明人:LEFORT LAURENT 权利人:LEFORT LAURENT 摘要:The present invention relates to the synthesis of optically active alcohols by means of enantioselective hydrogenation of ketones in biphasic systems. In particular the present invention relates to the synthesis of an optically active alcohol of general formula (1).
专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-8263784-B2 优先权日:2008-10-30 标 题 :Method for the synthesis of a ramipril intermediate 发明人:DE LANGE BEN; HEEMSKERK DENNIS 权利人:DE LANGE BEN; HEEMSKERK DENNIS; DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-11518780-B2 优先权日:2019-07-31 标 题:Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers 发明人:FANG SHIYUE 权利人:FANG SHIYUE 摘要:Embodiments for the synthesis of sensitive oligonucleotides as well as insensitive oligonucleotides are provided. Sulfur-based groups are used for the protection of exo-amino groups of nucleobases, phosphate groups and 2′—OH groups, and as cleavable linker for linking oligonucleotides to a support. Oligonucleotide syntheses are achieved under typical conditions using phosphoramidite chemistry with important modifications. To prevent replacing sulfur-based protecting groups by acyl groups via cap-exchange, special capping agents are used. To retain hydrophobic tag to assist RP HPLC purification, special phosphoramidites are used in the last synthetic cycle. With the sulfur-based groups for protection and linking, oligonucleotide deprotection and cleavage are achieved via oxidation followed by beta-elimination under mild conditions. Therefore, besides for insensitive oligonucleotide synthesis, the embodiments of the invention are capable for the synthesis of oligonucleotide analogs containing sensitive functional groups that cannot survive the harsh conditions used in prior art oligonucleotide synthesis technologies.
参考标题:Synthesis Of 3‐amino‐4‐iodothiophenes Through Iodocyclization Of 1‐(1,3‐dithian‐2‐yl)Propargylamines 作者:Eda Ismailoglu,Zeynep Mert,Mert Dinc,Kerem Kaya,Baris Yucel |发布日期:2021.8.6 摘要:3-Amino-4-Iodothiophenes Are Obtained By Iodocyclization Of 1,3-Dithianyl Substituted Propargylamine Derivatives Through Iodine Induced Cleavage Of Dithiane Ring In A Bicyclic Sulfonium Intermediate. 1-(1,3-Dithian-2-Yl)Propargylamines Are Readily Available By Au-Catalyzed Reaction Of 1,3-Dithiane-2-Carbaldehydes, Amines, And Alkynes In A One-Pot.
合成参考文献
摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 119. 摘要:Saikawa, Y.; Nakata, M., Science of Synthesis Knowledge Updates, (2018) 3, 370. 摘要:European Journal of Medicinal Chemistry--Chimie Therapeutique., 19(461), 1984