专利号:US-4287123-A 优先权日:1980-01-14 标题 :Synthesis of thienamycin via (3SR, 4RS)-3-((RS)-1-acyloxyethyl)-2-oxo-4-azetidineacetate 发明人:LIU THOMAS M H; MELILLO DAVID G; RYAN KENNETH M; SHINKAI ICHIRO; SLETZINGER MEYER 权利人:MERCK & CO INC 摘要:Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: II wherein R is a readily removable carboxyl protecting group; and is a readily removable acyl group.
专利号:US-4384998-A 优先权日:1981-03-30 标题:Synthesis of thienamycin from D-glucose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-4282148-A 优先权日:1980-01-14 标 题:Synthesis of thienamycin via esters of (3SR, 4RS)-3-[(SR)-1-hydroxyethyl]-β,2-dioxo-4-azetidinebutanoic acid 发明人:LIU THOMAS M H; MELILLO DAVID G; RYAN KENNETH M; SHINKAI ICHIRO; SLETZINGER MEYER 权利人:MERCK & CO INC 摘要:Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: II wherein R3 is a readily removable carboxyl protecting group.
专利号:US-4414155-A 优先权日:1980-01-14 标题 :Synthesis of thienamycin via esters of (3SR, 4RS)-3-[(SR)-1-hydroxyethyl]-β,2-dioxo-4-azetidinebutanoic acid 发明人:LIU THOMAS M H; MELILLO DAVID G; RYAN KENNETH M; SHINKAI ICHIRO; SLETZINGER MEYER 权利人:MERCK & CO INC 摘要:Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: II wherein R3 is a readily removable carboxyl protecting group.
专利号:US-4841045-A 优先权日:1985-03-12 标 题 :Synthesis of vinblastine and vincristine type compounds 发明人:KUEHNE MARTIN 权利人:UNIV VERMONT 摘要:A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.
专利号:US-4448976-A 优先权日:1981-03-30 标题 :Chiral synthesis of thienamycin from D-gluocose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
参考标题:Synthesis Of Potent Cytotoxic Epidithiodiketopiperazines Designed For Derivatization 作者:Chase R. Olsson,Joshua N. Payette,Jaime H. Cheah,Mohammad Movassaghi |发布日期:2020.4.3 摘要:We Describe Our Design, Synthesis, And Chemical Study Of A Set Of Functional Epidithiodiketopiperazines (Etps) And Evaluation Of Their Activity Against Five Human Cancer Cell Lines. Our Structure-Activity Relationship-Guided Substitution Of Etp Alkaloids Offers Versatile Derivatization, While Maintaining Potent Anticancer Activity, Offering Exciting Opportunity For Their Use As There Are No Examples
合成参考文献
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 241. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 298. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 296. 摘要:Weimar, M.; Fuchter, M. J., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 161.