专利号:US-5144073-A 优先权日:1988-08-31 标 题 :Process for preparation of dipeptides 发明人:HUBBS JOHN C 权利人:HUBBS JOHN C 摘要:Disclosed is a process for synthesis of a dipeptide such as N-acetyl-L- alpha -aspartyl-L-phenylalanine methyl ester wherein one amino acid serves as a chiral template which allows for synthesis of a second amino acid residue to form said dipeptide. The process involves several novel steps such as a nucleophile addition step. In addition, several novel intermediates are described.
专利号:US-4309346-A 优先权日:1980-03-27 标 题:Process for the preparation of 1-carbapenems and intermediates via trithioorthoacetates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via intermediates II and III: I II III wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R6 and R7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R1' is hydrogen or a protecting group; and Ra, Rb and Rc are independently selected from alkyl, aryl and aralkyl.
专利号:US-4378315-A 优先权日:1980-05-29 标题:Process for the preparation of thienamycin and intermediates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## R=H, blocking group or salt cation.
专利号:US-4290947-A 优先权日:1979-04-27 标 题:Process for the preparation of thienamycin and intermediates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMAN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## R=H, blocking group or salt cation.
专利号:US-4739048-A 优先权日:1980-05-29 标 题:Process for the preparation of thienamycin and intermediates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1##
专利号:US-4383946-A 优先权日:1980-03-27 标题:Process for the preparation of 1-carbapenems and intermediates via silyl-substituted dithioacetals 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via central intermediates II and III: I II III wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R6, R7 and R8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R1'and Re are hydrogen, or a readily removable protecting group; Ra, Rb and Rc are selected from alkyl, aryl or aralkyl.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/s10989-019-09998-x 摘要:Hegde N, Juvale K, Prabhakar B. p-Toluenesulfonyl Chloride Catalysed Facile Synthesis of O-benzyl-l-amino Acids and Their In Vitro Evaluation. International Journal of Peptide Research and Therapeutics. 2020 Jan 03;26(4):2129–35. doi: 10.1007/s10989-019-09998-x.