CAS: 247068-84-4; (2S)-2-Amino-4-Methyl-1-[(2R)-2-Methyloxiran-2-Yl]Pentan-1-One

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    上下游产品

    N-[(2S)-4-甲基-1-[(2R)-2-甲基环氧乙烷-2-基]-1-氧代-2-戊基]氨基甲酸叔丁酯 Tert-Butyl ((S)-4-Methyl-1-((R)-2-Methyloxiran-2-yl)-1-Oxopentan-2-yl)Carbamate 247068-82-2

    合成工艺路线路线简述

      📜N-[(2S)-4-甲基-1-[(2R)-2-甲基环氧乙烷-2-基]-1-氧代-2-戊基]氨基甲酸叔丁酯置于三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 1.5H,反应生成(2S)-2-氨基-4-甲基-1-[(2R)-2-甲基环氧乙烷基]-1-戊酮
      参考文献:Carmaphycins:新的蛋白酶体抑制剂展示来自海洋蓝藻的 α,β-环氧酮弹头
      标题:Carmaphycins:新的蛋白酶体抑制剂展示来自海洋蓝藻的 α,β-环氧酮弹头
      摘要:新的蛋白酶体抑制剂:库拉索岛海洋蓝藻symploca Sp. 的集合.海洋蓝藻产生 Carmaphycin A 和 B.这些化合物对酿酒酵母20S 蛋白酶体的 β5 亚基(糜蛋白酶样)表现出纳摩尔抑制,并对肺癌和结肠癌细胞系具有强细胞毒性.
      Doi:10.1002/cbic.201200007

      海关参考信息

      专利信息


      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

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      ✅ COA系统入驻 | 共享模式

      主要参考文献

      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

      合成参考文献


      摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2014).
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