Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于palladium On Activated Charcoal,水体系中,化学反应生成2-哌嗪羧酸盐酸盐 参考文献:Felder Et Al.,Chimia,1959,Vol. 13,P. 263 标题:Felder Et Al.,Chimia,1959,Vol. 13,P. 263
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-7495123-B2 优先权日:2004-04-05 标 题:Process for the preparation of enantiomerically enriched beta amino acid derivatives 发明人:XIAO YI; SUN YONGKUI; ROSNER THORSTEN; RIVERA NELO R; KRSKA SHANE W; CLAUSEN ANDREW M; ARMSTRONG III JOSEPH D; SPINDLER FELIX; MALAN CHRISTOPHE 权利人:SOLVIAS AG; MERCK & CO INC 摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-2012115907-A1 优先权日:2009-04-24 标题 :Novel compounds as inhibitors of renin 发明人:THOMBARE PRAVAIN; DESAI JIGAR; JAIN MUKUL R 权利人:THOMBARE PRAVAIN; DESAI JIGAR; JAIN MUKUL R; CADILA HEALTHCARE LTD 摘要:The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
专利号:RU-2125561-C1 优先权日:1993-07-16 标 题:Intermediate compounds for synthesis of hiv-protease inhibitors and a method of their synthesis
专利号:WO-2013084241-A1 优先权日:2011-12-09 标题:Compounds as inhibitors of renin 发明人:THOMBARE PRAVIN S; DESAI JIGAR N 权利人:CADILA HEALTHCARE LTD; THOMBARE PRAVIN S; DESAI JIGAR N 摘要:The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to processes for preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
参考文献:10.1007/bf01388175 摘要:Palomo C, Aizpurua JM, Ganboa I, Oiarbide M. From beta-lactams to alpha- and beta-amino acid derived peptides. Amino Acids. 1999;16(3-4):321–43. doi: 10.1007/bf01388175. 摘要:Wu G, Zhao H, Luo RG, Wei D, Malhotra SV. Chiral synthesis and enzymatic resolution of (S)-(-)piperazine-2-carboxylic acid using enzyme alcalase. Enantiomer. 2001;6(6):343–5.