专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-5523411-A 优先权日:1994-03-14 标题 :Synthesis of mitomycin and its analogs 发明人:JIMENEZ LESLIE; WANG ZHENG 权利人:UNIV RUTGERS 摘要:The present invention relates to the synthesis of mitomycin and analogs thereof that are useful as anticancer antibiotics. The invention further relates to analogs of mitomycin, which can be prepared according to the methods of synthesis provided. The synthetic method of the invention provides for reacting a derivitized indole with a dialkylvinylsulfonium salt to yield a tricyclic skeleton having the precursors of the fourth ring in one step, followed by an oxidation step or steps to close the fourth ring and prepare mitomycin or a related compound.
专利号:US-5597931-A 优先权日:1992-03-30 标 题:Total synthesis of taxol and analogues thereof 发明人:DANISHEFSKY SAMUEL J; MASTERS JOHN; YOUNG WENDY; LINK J THOMAS; ISAACS RICHARD; SNYDER LAWRENCE B 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
专利号:US-5488116-A 优先权日:1992-03-30 标 题:Total synthesis of taxol and analogues thereof 发明人:DANISHEFSKY SAMUEL J; BORNMANN WILLIAM G; QUENEAU YVES; MAGEE THOMAS V; KROL WALTER J; MASTERS JOHN J; JUNG DAVID K 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
专利号:US-5527924-A 优先权日:1992-03-30 标题 :Total synthesis of taxol 发明人:DANISHEFSKY SAMUEL J; BORNMANN WILLIAM G; QUENEAU YVES; MAGEE THOMAS V; KROL WALTER J 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides two basic routes for the total synthesis of taxol having the structure: The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.
专利号:US-11512075-B2 优先权日:2017-06-14 标 题:Synthesis of 20-nor-salvinorin A 发明人:SHENVI RYAN; ROACH JEREMY; SASANO YUSUKE; BOHN LAURA; SCHMID CULLEN 权利人:SCRIPPS RESEARCH INST 摘要:The invention provides 20-nor-salvinorin A, an analog of the kappa-opioid agonist salvinorin A. The 20-nor-salvinorin A is an active kappa-opioid modulator and can be used for treatment of medical conditions wherein modulation of the kappa-opioid receptor is medically indicated, such as pain, pruritis, depression, or inflammation, or conditions implicating perception and consciousness. 20-nor-salvinorin A can be less additive when used in treatment compared to a mu-opioid receptor agonist, and 20-nor-salvinorin A is more stable in vivo than is parent compound salvinorin A. The invention further provides synthetic intermediates and procedures for preparation of 20-nor-salvinorin A.