专利号:EP-0097994-B1 优先权日:1982-06-24 标 题:Method for the solid-phase synthesis of retro-inverso polypeptides 摘要:This invention relates to a method for the solid-phase synthesis of polypeptides containing retro-inverted peptide bonds, using polydimethylacrylamide-co-acryloylsarcosimethylester resin cross-linked with N, N min -ethylene-bis-acrylamide as the insoluble support for lengthening the polypeptide chain in stages by the addition of suitable amino acid derivatives and/or peptides in succession. In particular, the method described in the present invention allows the easy preparation, on the polymer matrix, of monoacylated gem-diamino residues using the reagent I, I-bis (trifluoroacetoxy) iodobenzene in mixed aqueous-organic solvents.
专利号:US-4774319-A 优先权日:1985-03-06 标题:Synthesis of a derivative of GRF and intermediate peptides 发明人:ONO KEIICHI; KAI YOSHIYUKI; TAKEBAYASHI YOSHIAKI; SANO AKIHIKO; SUWA KAZUSHI 权利人:SUMITOMO PHARMA 摘要:A process for the manufacture of a polypeptide (I) having the formula: ##STR1## which comprises steps of: (a) coupling, successively and in the order of the sequence of the polypeptide (I), the four protected fragments A, B, C and D or five protected fragments A, B, C, E and F, n said fragment A by the formula, Leu-Gin-Asp-Ile-Met-Ser-Arg-NH 2 n said fragment B by the formula, Gln-Leu-Ser-Ala-Arg-Lys-Leu n said fragment C by the formula, Arg-Lys-Val-Leu-Gly n said fragment D by the formula, Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr n said fragment E by the formula, Ile-Phe-Thr-Asn-Ser-Tyr n and said fragment F by the formula, Tyr-Ala-Asp-Ala being represented, respectively, and n (b) eliminating, at the end of sequence, all the protecting groups to provide the polypeptide (I) which is active on the stimulation of the release of the growth hormone and thus is very useful as medicine for treatment of growth hormone deficiency disease and the like.
专利号:US-9303041-B2 优先权日:2012-08-21 标题 :Haptens of olanzapine 发明人:DONAHUE MATTHEW GARRETT; GONG YONG; SALTER RHYS; HRYHORENKO ERIC; DECORY THOMAS R; REMMERIE BART; SANKARAN BANUMATHI 权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC 摘要:The invention relates to compounds of Formula I, wherein R 1 , R 2 , and R 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from olanzapine. The invention also relates to conjugates of an olanzapine hapten and a protein.
专利号:US-9795685-B2 优先权日:2012-08-21 标 题 :Haptens of aripiprazole 发明人:LIN RONGHUI; SALTER RHYS; DECORY THOMAS R; HRYHORENKO ERIC; REMMERIE BART M; SANKARAN BANUMATHI 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention relates to compounds of Formula I, wherein R 1 , R 2 , and R 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from aripiprazole. The invention also relates to conjugates of an aripiprazole hapten and a protein.
专利号:US-6972320-B2 优先权日:2000-05-12 标题 :Ligation method and reagents to form an amide bond 发明人:RAINES RONALD T; KIESSLING LAURA L; NILSSON BRADLEY L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.
专利号:EP-0193910-A2 优先权日:1985-03-06 标题:Synthesis of a derivative of GRF and intermediate peptides
参考标题:Microwave-Assisted Preparation Of Fused Bicyclic Heteroaryl Boronates: Application In One-Pot Suzuki Couplings 作者:Erin F. Dimauro,Jason R. Vitullo |发布日期:2006.5.1 摘要:The Rapid And Efficient Synthesis Of Various Disubstituted 5,6-Fused Heterocycles Using A Microwave-Assisted One-Pot Cyclization−suzuki Coupling Approach Is Described. This Work Highlights The Tolerance Of The Boronic Ester Functional Group To A Variety Of Reaction Conditions And The Utility Of Functionalized Boronates As Penultimate Intermediates In The Synthesis Of Diverse Compound Libraries.
合成参考文献
摘要:Wirth, T., Science of Synthesis, (2008) 39, 881.