2,2,2-三氟乙醇置于吡啶,三氟甲磺酸酐体系中,用 二氯甲烷,水 作为反应溶剂,化学反应生成 2,2,2-三氟乙基三氟甲烷磺酸酯 参考文献:Novel Substituted 4-(1H-Benzimidazol-2-yl) [1,4]Diazepanes Useful For The Treatment Of Allergic Diseases 标题:Novel Substituted 4-(1H-Benzimidazol-2-yl) [1,4]Diazepanes Useful For The Treatment Of Allergic Diseases 摘要:本发明涉及一种新颖的4-(1H-苯并咪唑-2-基)[1,4]二氮杂环庚烷衍生物及其立体异构体,以及其药学上可接受的盐,其作为组胺受体拮抗剂和速激肽受体拮抗剂具有用途.这些拮抗剂在过敏性鼻炎的治疗中有用,包括季节性鼻炎和鼻窦炎;炎症性肠病,包括克罗恩病和溃疡性结肠炎;哮喘;支气管炎;以及呕吐.
专利号:WO-2011101864-A1 优先权日:2010-02-17 标题 :Novel process for the synthesis of phenoxyethyl derivatives 发明人:JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 权利人:PANACEA BIOTEC LTD; JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 摘要:The present invention provides an improved process for the synthesis of 2-[2- (2,2,2-trifluoroethoxy)phenoxy]ethanol intermediate, its derivatives and/or its pharmaceutically acceptable salts, useful in the synthesis of α-1 adrenoceptor blockers such as silodosin.
专利号:US-12275733-B2 优先权日:2016-11-07 标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders 发明人:GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN 权利人:SANOFI SA 摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
专利号:WO-2010144293-A1 优先权日:2009-06-08 标 题 :Synthesis of telcagepant and intermediates thereof 发明人:XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J 权利人:MERCK SHARP & DOHME; XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J 摘要:Disclosed is an efficient synthesis for the manufacture of the caprolactam intermediate (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one: Formula and salts thereof, and an efficient preparation of telcagepant using the caprolactam intermediate.
专利号:US-2025115551-A1 优先权日:2023-10-03 标 题:Synthesis of ras inhibitors 发明人:LI YI; MENDOZA BENJAMIN; NAGANATHAN SRIRAM; WANG ROSS; YI YI; BALLMER STEVEN G; DAVIDSON JAMES; HUANG XIAOJUN 权利人:REVOLUTION MEDICINES INC 摘要:The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.
专利号:US-7196197-B2 优先权日:2003-09-17 标题:Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof 发明人:WANG ZHI-XIAN; LI YUANQIANG; GUNTOORI BHASKAR REDDY 权利人:APOTEX PHARMACHEM INC 摘要:Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof that involves the use of the 2-halobenzoic acid and its derivatives as a starting material. The use of this process also allows for the synthesis of a novel intermediate useful in the production of Flecainide. This new process is an inexpensive and efficient process for the manufacture of these compounds.
专利号:US-10457640-B2 优先权日:2016-10-19 标 题:Synthesis of inhibitors of EZH2 发明人:VASWANI RISHI G; HEWITT MICHAEL CHARLES 权利人:CONSTELLATION PHARMACEUTICALS INC 摘要:Provided herein are synthetic methods for the preparation of EZH2 inhibitors.
[参考文献]: Laura A Mcallister, Et Al. A General Strategy For The Synthesis Of Cyclic N-Aryl Hydroxamic Acids Via Partial Nitro Group Reduction. J Org Chem. 2011 May 6;76(9):3484-97.
合成参考文献
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