专利号:US-8835477-B2 优先权日:2009-10-06 标题 :Method for the synthesis of 2-thiohistidine and the like 发明人:ERDELMEIER IRÈNE; DAUNAY SYLVAIN 权利人:ERDELMEIER IRÈNE; DAUNAY SYLVAIN; TETRAHEDRON 摘要:Methods for the synthesis of 2-thiohistidine or a derivative thereof of the formula (I), or of a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, from a compound of the formula (II) or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, by cleavage reaction in the presence of a thiol at a temperature higher than or equal to 60° C. The invention also relates to compounds of the formula (II) and a method for the synthesis thereof.
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-5506349-A 优先权日:1992-05-13 标 题 :Chemical synthesis of 2', 3'-dideoxycytidine 发明人:MATULIC-ADAMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:Method for synthesis of 2',3'-dideoxycytidine by providing 5'-silylated-2',3'-dideoxyuridine as an intermediate.
专利号:US-7767826-B2 优先权日:2007-10-05 标题 :Process for the synthesis of L-(+)-ergothioneine 发明人:TRAMPOTA MIROSLAV 权利人:PHARMATECH INTERNATIONAL INC 摘要:This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.
专利号:WO-9323413-A1 优先权日:1992-05-13 标 题:Synthesis of nucleotide monomers 发明人:BEIGELMAN LEONID; MATULIC-ACADEMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:Methods for synthesis of 2',3'-dideoxycytidine, 2',3'-dideoxyguanosine, 2',3'-dideoxyadenosine, 2',3'-dideoxyinosine and 2',3'-dideoxyguanosine, and 3'-O-benzoyl-2'-deoxyribonucleoside.
专利号:US-5925762-A 优先权日:1996-09-17 标 题:Practical synthesis of urea derivatives 发明人:THAVONEKHAM BOUNKHAM 权利人:BOEHRINGER INGELHEIM CA LTD 摘要:A very mild and efficient approach for the synthesis of ureas is described. Phenyl carbamates were used as intermediates for the preparation of N,N'- substituted ureas. The carbamates were treated with an approximate stoichiometric amount of amine in dimethyl sulfoxide at ambient temperature, generating the ureas in high yield. The reaction was simple, safe, fast, inexpensive, and amenable to large scale production of the product.
[参考文献]: Yedi Sun, Et Al. Synthesis Of Scyllo-Inositol Derivatives And Their Effects On Amyloid Beta Peptide Aggregation. Bioorg Med Chem. 2008 Aug 1;16(15):7177-84.
合成参考文献
摘要:Wicha, J., Science of Synthesis, (2009) 48, 207. 摘要:Wicha, J., Science of Synthesis, (2009) 48, 219. 摘要:Wicha, J., Science of Synthesis, (2009) 48, 190. 摘要:Wicha, J., Science of Synthesis, (2009) 48, 202. 摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 55.