专利号:US-4360684-A 优先权日:1981-04-08 标 题 :Process for the preparation of (2S)-tetrahydro-2α-methyl-6-oxo-4βα-carboxylic acid 发明人:CVETOVICH RAYMOND J; MELILLO DAVID G; RYAN KENNETH M; SLETZINGER MEYER 权利人:MERCK & CO INC 摘要:Disclosed is a process for preparing (2S)-tetrahydro-2 alpha -methyl-6-oxo-4 beta -amino-2H-pyran-3 alpha -carboxylic acid (I) which is useful in the synthesis of thienamycin. The process proceeds via a stereospecific reduction of the 2-acetyl-3-(R)- alpha -methylbenzylamino-2-pentenedioic acid diester (II). I II wherein R is, alpha -methylbenzyl, and R1 is lower alkyl having 1-6 carbon atoms or arylalkyl such as benzyl.
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.