专利号:US-11708341-B2 优先权日:2016-08-05 标题:Synthesis of (S)-2-amino-4-methyl-((R)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof 发明人:Beaver Matthew; CUI SHENG; SHI XIANGQING 权利人:AMGEN INC 摘要:The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure n nCompound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.
专利号:US-8921583-B2 优先权日:2007-10-04 标题:Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides 发明人:PHIASIVONGSA PASIT; SEHL LOUIS C; FULLER WILLIAM DEAN; LAIDIG GUY J 权利人:ONYX THERAPEUTICS INC 摘要:The invention relates to crystalline peptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions. This invention also relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.
专利号:CN-109641863-B 优先权日:2016-08-05 标 题 :Synthesis of intermediates for the synthesis of carfilzomib and its pharmaceutically acceptable salts
专利号:US-2016194354-A1 优先权日:2013-09-06 标 题 :Stereoselective synthesis of diols and triols by mannich reaction and their use in the synthesis of carfilzomib 发明人:HÖFERL-PRANTZ KATHRIN; WILHELM THORSTEN 权利人:SANDOZ AG 摘要:It is provided an improved process for preparing Carfilzomib, including novel compounds that can be used as intermediates in the process for preparing Carfilzomib.
专利号:SA-519401022-B1 优先权日:2016-08-05 标题:(S)-2- Synthesis of amino-4-methyl-1- -pentane-1-on and pharmaceutically acceptable salts thereof ((R)-2-methyloxyran-2-yl)
专利号:EP-3494108-B1 优先权日:2016-08-05 标 题:Synthesis of (s)-2-amino-4-methyl-1-((r)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof
参考标题:Allenone-Mediated Racemization/epimerization-Free Peptide Bond Formation And Its Application In Peptide Synthesis 作者:Zhengning Wang,Xuewei Wang,Penghui Wang,Junfeng Zhao |发布日期:2021.7.14 摘要:Peptide Synthesis (Spps). The Robustness Of The Allenone-Mediated Peptide Bond Formation Was Showcased Incisively By The Synthesis Of Carfilzomib, Which Involved A Rare Racemization-/epimerization-Free N To C Peptide Elongation Strategy. Furthermore, The Successful Synthesis Of The Model Difficult Peptide Acp (65-74) On A Solid Support Suggested That This Method Was Compatible With Spps. This Method Combines