专利号:WO-2010103857-A1 优先权日:2009-03-12 标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device 发明人:NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.
专利号:US-12018094-B2 优先权日:2018-04-02 标 题 :Crystalline dipeptides useful in the synthesis of elamipretide 发明人:DUNCAN SCOTT M; REDMON MARTIN P 权利人:STEALTH BIOTHERAPEUTICS INC 摘要:Disclosed are crystalline forms of L-Lys(Boc)-Phe-NH2 and Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.
专利号:US-4504415-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 and desacetyl thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; STUDER ROLF; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin alpha 1 and desacetyl thymosin alpha 1 with t-Boc side chain protection and proceeding through novel intermediates is disclosed.
专利号:US-4517119-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; LERGIER WILLIAM; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin α 1 and proceeding through novel intermediates is disclosed.
专利号:US-8350042-B2 优先权日:2008-01-31 标题 :Antiviral compounds for the treatment of HCV infection 发明人:HERMANN THOMAS C; CARNEVALI MAIA 权利人:UNIV CALIFORNIA; HERMANN THOMAS C; CARNEVALI MAIA 摘要:Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.
专利号:US-10112976-B2 优先权日:2014-06-30 标 题:Process for the production of D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide 发明人:ZHAO XINJUN; ZHENG MINYU; YU XIAOZHONG; GAO HANRONG; CORNILLE FABRICE 权利人:FLAMMA SPA 摘要:The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.
参考标题:Hydrodehalogenation Of Alkyl Iodides With Base-Mediated Hydrogenation And Catalytic Transfer Hydrogenation: Application To The Asymmetric Synthesis Of N-Protected α-Methylamines 作者:Pijus K. Mandal,J. Sanderson Birtwistle,John S. Mcmurray |发布日期:2014.9.5 摘要:We Report A Very Mild Synthesis Of N-Protected α-Methylamines From The Corresponding Amino Acids. Carboxyl Groups Of Amino Acids Are Reduced To Iodomethyl Groups Via Hydroxymethyl Intermediates. Reductive Deiodination To Methyl Groups Is Achieved By Hydrogenation Or Catalytic Transfer Hydrogenation Under Alkaline Conditions. Basic Hydrodehalogenation Is Selective For The Iodomethyl Group Over Hydrogenolysis-Labile
合成参考文献
摘要:Ghosh, B.; Maleczka, R. E., Jr., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 355.