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-8030496-B2 优先权日:2005-02-17 标 题:Intermediate compound for synthesis of viridiofungin a derivative 发明人:KATO TATSUYA; KIMURA NOBUAKI; MIZUTANI AKEMI; MAKINO TOSHIHIKO; KAWASAKI KENICHI; FUKUDA HIROSHI; KOMIYAMA SUSUMU; TSUKUDA TAKUO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. n A compound represented by the formula (1-8): n n n n n n n n n n n n wherein Y represents a group represented by the following formula: n n n n n n n n n n n n n n n n Q represents a protected carbonyl group; D represents —(CH 2 ) m —R′, etc.; and n represents an integer of 0 to 10.
专利号:US-4629784-A 优先权日:1983-08-16 标 题:Synthesis of cyclopropane amino acids 发明人:STAMMER CHARLES H 权利人:UNIV GEORGIA RES FOUND 摘要:Cyclopropane ('Cyclopropyl') amino acids and peptides containing at least one cyclopropyl amino acid are disclosed. The processes for synthesizing cyclopropyl amino acids and peptides containing at least one cyclopropyl amino acid are also disclosed. Cyclopropyl amino acids are useful as enzyme inhibitors and as substitutes for natural amino acids in peptide hormones such as regulators of bodily functions to enhance bioactivity, to stabilize the peptide into which it is incorporated to cleavage by enzymes and to convert such peptides into enzyme inhibitors.
专利号:BR-PI0202783-B1 优先权日:2001-07-19 标 题:process for the rapid synthesis of a peptide in solution in an organic solvent or a mixture of organic solvents, and methods for the combinatorial synthesis of peptide collections and for automated solution peptide synthesis
专利号:US-2012088848-A1 优先权日:1998-03-19 标 题 :Methods and compositions for controlled polypeptide synthesis 发明人:DEMING TIMOTHY J; YU MIAOER; CURTIN SCOTT A; HWANG JUNGYEON; WYRSTA MICHAEL D; NOWAK ANDREW; SEIDEL SCOTT W 权利人:DEMING TIMOTHY J; YU MIAOER; CURTIN SCOTT A; HWANG JUNGYEON; WYRSTA MICHAEL D; NOWAK ANDREW; SEIDEL SCOTT W 摘要:Methods and compositions for the generation of polypeptides having varied material properties are disclosed herein. Methods include means for initiating the polymerization of aminoacid-N-carboxyanhydride (NCA) monomer by combining the monomer with an amido-containing metallacycle, for making self assembling amphiphilic block copolypeptides and related protocols for adding oligo(ethyleneglycol) functionalized aminoacid-N-carboxyanhydrides (NCAs) to polyaminoacid chains. Additional methods include means of adding an end group to the carboxy terminus of a polyaminoacid chain by reacting an alloc-protected amino acid amide with a transition metal-donor ligand complex to forming an amido-amidate metallacycle for use in further polymerization reactions. Novel compositions for use in peptide synthesis and design including five and six membered amido-containing metallacycles and block copolypeptides are also disclosed.
专利号:EP-1773870-B1 优先权日:2005-05-03 标 题:Methods for the production of peptide having a c-terminal amide 发明人:IVCHENKO ALEXANDER; ALON HAGI; ELSTER SHAI; SHUSHAN SHIMON; EIDELMAN CHAIM; TOVI AVI; GADI TEHILA; BAR-OZ LEAH; ALTERMAN ELEONORA; ZAOVI GIL; BUTILCA GABRIEL-MARCUS 权利人:NOVETIDE LTD 摘要:The invention relates to a method for the preparation of leuprolide by a combination of solid-phase synthesis and post assembly solution phase synthesis. The invention also relates to pure leuprolide acetate.
参考标题:Diazonamide Studies. A Direct Synthesis Of The Indole Bis-Oxazole Fragment From Tri- And Tetra-Peptides Using Biomimetic Oxidative Cyclizations 作者:Jonathan Sperry,Christopher J. Moody |发布日期:2010.8 摘要:Oxidation Of Several Readily Prepared Tryptophan Containing Tri- And Tetrapeptides With Ddq Results In A Biomimetic Cyclization And Direct Formation Of The Indole Bis-Oxazole Fragment Of Diazonamide A, Establishing That Such A Transformation Is A Viable Route When Considering The Biosynthetic Formation Of The Heterocyclic Core Of The Natural Product.
合成参考文献
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