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叔丁氧羰基-脯氨酰-琥珀酰亚胺置于sodium Tetrahydroborate体系中,用 水 作为反应溶剂,以0.313 G的收率获得产物n-Boc-L-脯氨醇
参考文献:N保护的β-氨基醇和短肽 的便捷合成和晶体学分析†
标题:N保护的β-氨基醇和短肽 的便捷合成和晶体学分析†
摘要:一种简便,高效且无外消旋的方法,使用该方法合成n保护的β-氨基醇和肽醇n-羟基琥珀酰亚胺描述了活性酯.使用这种方法,可以高产率分离出二肽,三肽和五肽醇.分析了β-氨基醇,二肽和三肽醇的晶体构象,在三肽醇晶体中观测到了明确定义的iii型β角.发现该方法与fmoc-,Boc-和其他侧链保护基相容.
DOI:10.1039/c0Ob01226B

专利信息

专利号:US-5869725-A
优先权日:1994-05-17
标 题:Derivatives of aminosulfonic acids, utilization of the same in the synthesis of pseudopeptides and process for their preparation
发明人：GENNARI CESARE; POTENZA DONATELLA; SALOM BARBARA
权利人:PHARMACIA & UPJOHN SPA
摘要:Derivatives of gamma-amino-alpha,beta-unsaturated sulfonic acids, a process for the preparation of the same and their utilization in the synthesis of pseudopeptides characterized by the presence of at least a sulfonamide type bond conjugated to a double bond are described.

专利号:WO-2017021270-A1
优先权日:2015-08-03
标 题 :Process for the synthesis of ravidasvir
发明人：CASTALDI GRAZIANO; BARUTO ALESSANDRO; OLDANI ERMINIO; GABOARDI MAURO
权利人:HC-PHARMA AG
摘要:A process for the synthesis of ravidasvir and intermediates useful in the preparation thereof are disclosed.

专利号:US-4978744-A
优先权日:1989-01-27
标题:Synthesis of dolastatin 10
发明人：PETTIT GEORGE R; SINGH SHEO B
权利人:UNIV ARIZONA
摘要:A complicated but extremely important scheme of synthesis has been developed for synthesizing, dolaisoleuine, dolaproine, dolaphenine and dolavaline from readily available starting materials such as Z-(S,S)isoleucine, S-phenylalaline, S-phenylalaninol, S-prolinol, S-mandelate, and S-valine. The requisite amino acids have been combined using several peptide coupling procedures to create pharmaceutically pure dolastatin 10.

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

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-11053243-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.