专利号:US-2025236897-A1 优先权日:2022-02-16 标 题 :Processes for preparation of avacopan and intermediates thereof 发明人:GYUJTO IMRE; PAAL TIHAMER; JUHASZ ZSUZSA POTARINE; ESZENYI DANIEL; ZAHUCZKY GABOR JOZSEF; KONDOR ZOLTAN; RENGASAMY VADIVELAN; PRAJAPATI RAMKARAN; DAUND VAIBHAV SURESH; SAINGER SHACHI; KADU RUSHIKESH; SHARMA VISHAL 权利人:TEVA PHARMACEUTICALS INT GMBH 摘要:The present disclosure encompasses a process for chiral resolution of racemic amines, particularly ethyl 2-(4-((tert-butoxycarbonyl)amino)phenyl)piperidine-3-carboxylate, into its desired isomer, ethyl (2R,3S)-2-(4-((tert-butoxycarbonyl)amino)phenyl)-piperidine-3-carboxylate, which is an intermediate useful in the synthesis of Avacopan.
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参考标题:Rh(III)-Catalyzed Regio- And Chemoselective [4 + 1]-Annulation Of Azoxy Compounds With Diazoesters For The Synthesis Of 2H-Indazoles: Roles Of The Azoxy Oxygen Atom 作者:Zhen Long,Zhigang Wang,Danni Zhou,Danyang Wan,Jingsong You |发布日期:2017.6.2 摘要:Tandem C-H Alkylation/intramolecular Decarboxylative Cyclization Of Azoxy Compounds With Diazoesters For The Synthesis Of 3-Acyl-2H-Indazoles Is Disclosed. The Azoxy Instead Of The Azo Group Enables A Distinct Approach For Cyclative Capture, Leading To A [4 + 1]-Annulation Rather Than A Classic [4 + 2] Manner. The Azoxy Oxygen Atom Is Traceless After Annulation, And Further Removal From The Product Is
合成参考文献
摘要:Nahra, F.; Cazin, C. S. J., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 305.