CAS: 87694-50-6; (S)-N-Methyl-N-Methoxy-2-(Tert-Butoxycarbonylamino)-4-Methylpentanamide

相似化合物

1172623-95-8 87694-51-7 87694-52-8

上下游产品

CAS号13139-15-6 B°C-L-亮氨酸 | CAS号1117-97-1 甲氧基甲基胺 | CAS号6638-79-5 二甲羟胺盐酸盐 | CAS号543-27-1 氯甲酸异丁酯 | CAS号61-90-5 L-亮氨酸 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号54430-65-8 (S)-tert-butyl ... | CAS号247068-82-2 卡非佐米中间体 | CAS号58521-49-6 (3S,4S)-4-((叔丁氧...

📜Boc-L-亮氨酸置于n-甲基吗啉,三乙胺,氯甲酸异丁酯体系中,用 四氢呋喃,异丙醇 作为反应溶剂,化学反应生成 N-(叔丁氧基羰基)-L-亮氨酸-N'-甲氧基-N'-甲酰胺
参考文献:卡非佐米生产中的连续过程改进,第1部分:制备环氧酮战斗部的工艺理解和商业路线的改进
标题:卡非佐米生产中的连续过程改进,第1部分:制备环氧酮战斗部的工艺理解和商业路线的改进
摘要:环氧酮4是商业蛋白酶体抑制剂卡非佐米(kyprolis)生产过程中的分离中间体.商业流程开发和优化工作,以制备环氧酮4强调了一些改进流程的机会.在本文中,提出了三个案例研究,这些案例研究证明了对反应机理的详细了解如何导致改进,从而提高了过程的整体稳定性.在第一个案例研究中,研究了α-手性烯酮外消旋化的机理,从而开发了改进的水后处理程序.接下来,研究了用于步骤3环氧化反应的漂白剂/吡啶混合物的稳定性,从而确定了吡啶作为关键原料,并改善了反应条件和控制策略,以达到转化目标.最后,氧化的丁基化羟基甲苯(obht)被确定为是在氧化之前的步骤中使用bht稳定的四氢呋喃产生的杂质.从这些调查中获得的过程理解导致了过程改进的实施,从而改进了过程的鲁棒性.第二代路线的发展4是本系列第2部分的主题(doi:10.1021 / Acs.Oprd.0C00052).
DOI:10.1021/acs.Oprd.0C00051

专利信息

专利号:US-7829669-B2
优先权日:1999-06-28
标 题:Catalytically active recombinant memapsin and methods of use thereof
发明人：KOELSCH GERALD; TANG JORDAN J N; HONG LIN; GHOSH ARUN K; LIN XINLI
权利人:OKLAHOMA MED RES FOUND; UNIV ILLINOIS
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bond to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

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:US-2002049303-A1
优先权日:1999-06-28
标 题 :Catalytically active recombinant memapsin and methods of use thereof
发明人：TANG JORDAN J N; LIN XINLI; KOELSCH GERALD; HONG LIN
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogs including isosteres at the sites of the critical amino acid residues were developed and the substrate analogs, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

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:US-2013150290-A1
优先权日:2007-10-04
标 题:Crystalline Peptide Epoxy Ketone Protease Inhibitors and the Synthesis of Amino Acid Keto-Epoxides