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-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:US-2010286211-A1 优先权日:2004-10-08 标题:Oxazolidinone derivatives as antimicrobials 发明人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 权利人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
专利号:US-RE29882-E 优先权日:1973-04-27 标题 :Synthesis of oxindoles from anilines and intermediates therein 摘要:Preparing oxindoles and intermediates therefor by reacting an N-haloaniline with β-thio ester or β-thio amides to form an azasulfonium halide, reacting the azasulfonium halide with a base to form an ortho[thio-ether (hydrocarbonoxycarbonyl) alkyl]aniline, or a [thio-ether (aminocarbonyl) alkyl]aniline, reacting the ortho-substituted aniline with an acid to form a 3-thio-ether-2-oxindole, and then reducing the 3-thio-ether-2-oxindole with Raney Nickel to form the 2-oxindole.
专利号:EP-0193910-A2 优先权日:1985-03-06 标题:Synthesis of a derivative of GRF and intermediate peptides
专利号:US-3996264-A 优先权日:1973-04-27 标 题 :Synthesis of oxindoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing oxindoles and intermediates therefor by reacting an N-haloaniline with β-thio esters or β-thio amides to form an azasulfonium halide, reacting the azasulfonium halide with a base to form an ortho-[thio-ether (hydrocarbonoxycarbonyl) alkyl]aniline, or a [thio-ether (aminocarbonyl) alkyl]aniline, reacting the ortho-substituted aniline with an acid to form a 3-thio-ether-2-oxindole, and then reducing the 3-thio-ether-2-oxindole with Raney Nickel to form the 2-oxindole.
参考文献:10.1021/jp9071026 摘要:Wisniowski PB, Hug GL, Pogocki D, Bobrowski K. Efficient alpha-(alkylthio)alkyl-type radical formation in (*)OH-induced oxidation of alpha-(methylthio)acetamide. J Phys Chem A. 2010 Jan 14;114(1):105–16. doi: 10.1021/jp9071026. 摘要:García Ruano, J. L.; Cid, M. B.; Martín-Castro, A. M.; Alemán, J., Science of Synthesis, (2008) 39, 260.