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-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-9458188-B2 优先权日:2010-12-22 标 题 :Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT; BTG INT LTD 摘要:A new method for the synthesis of L-Glutamyl-γ-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
专利号:US-9284266-B2 优先权日:2012-01-19 标题:Method for synthesizing ramalin and ramalin precursor by using glutamic acid derivative and hydroxy aniline or hydroxy aniline having protected hydroxy group 发明人:YIM JOUNG HAN; KIM IL CHAN; KIM DOCKYU; HAN SE JONG; LEE HYOUNG SEOK; BHATTARAI HARI DATTA; KIM TAI KYOUNG; KIM KEUN SIK 权利人:YIM JOUNG HAN; KIM IL CHAN; KIM DOCKYU; HAN SE JONG; LEE HYOUNG SEOK; BHATTARAI HARI DATTA; KIM TAI KYOUNG; KIM KEUN SIK; KOREA INST OF OCEAN SCIENCE AND TECHNOLOGY 摘要:Disclosed is a method of the synthesis of ramalin. It comprises reacting a glutamic acid derivative, which is prepared using alkylchloroformate, with a hydrazine salt compound, which is prepared from hydroxy aniline, whether protected or not. The synthesis method allows ramalin, excellent in antioxidant and anti-inflammatory activity, to be simply synthesized at stable yield even without use of a highly toxic solvent such as DMF. In addition, the method is cost competitive, and provides ramalin at high efficiency, thus enabling the mass production of ramalin.
专利号:US-6737541-B2 优先权日:2000-01-26 标题 :Preparation of nitrogen mustard derivatives 发明人:SIEDLECKI PAUL STANISLAW; GLANVILLE MARTIN DAVID MICHAEL 权利人:ASTRAZENECA AB 摘要:This invention relates to an improved synthesis of 5-(N-[(S)-N-{N,N-bis( 2-chloroethyl)amino}phenoxycarbonyl)-gamma-glutamyl]amino)isophthalic acid (also named ZD9063P), a prodrug used in Antibody Directed Enzyme Prodrug Therapy (ADEPT), a targeted cytotoxic cancer therapy. Another aspect of the invention comprises a compound of Formula (I) in which R<1 >and R<2 >are chloro, R<3 >is an alphamethylbenzylamine salt of carboxylic acid, (R<4>)n represents a benzyl protected 3,5-dicarboxylic acid and the asterisked chiral carbon in Formula (I) has S configuration, preferably in crystalline form.