专利号:US-4374979-A 优先权日:1981-04-27 标 题:Regiospecific synthesis of anthracyclinone compounds such as daunomycinone 发明人:MITSCHER LESTER A 权利人:UNIV KANSAS ENDOWMENT ASS 摘要:A regiospecific synthesis for anthracyclinones asymmetric is disclosed. The synthesis is based upon a regiospecific bromination of the C-7 position of the alpha -tetralone which after transposing the keto group to the beta -position and reaction with an organo-lithium compound is condensed with a phthalate ester.
专利号:US-5175302-A 优先权日:1987-07-13 标 题 :Nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4837327-A 优先权日:1987-07-13 标 题 :Process for nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to alkehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4999429-A 优先权日:1989-01-09 标 题 :Process for the preparation of α,α,β-1-trifluoro-1-olefinic derivatives 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-2001024798-A1 优先权日:1998-06-11 标题:Biomimetic combinatorial synthesis 发明人:SHAIR MATTHEW D; LINDSLEY CRAIG W; PELISH HENRY E; SHEEHAN SCOTT M; GOESS BRIAN C; LAYTON MARK E; CHAN LAWRENCE K; CHEN CHUO; WESTWOOD NICHOLAS J 摘要:The present invention provides biomimetic compounds and libraries thereof, as well as methods for their production. In general, the inventive method involves the selection of a desired biological synthetic pathway and mimics that synthetic pathway utilizing modern synthetic tools. The structures formed from this method are preferably generated in fewer than four steps. These scaffold structures can then be functionalized to yield biomimetic compounds and libraries of compounds. In preferred embodiments, biomimetic compounds and libraries are generated from an oxidative phenolic coupling reaction. In other particularly preferred embodiments, the compounds and libraries of compounds are generated from cascade reactions to yield bicyclo [n. 3.1 ] ring systems, medium ring systems, and fused ring systems. In addition to compounds, libraries and methods for their production, the present invention also provides pharmaceutical compositions and methods and kits for determining one or more biological activities of the library members.
专利号:US-6020341-A 优先权日:1994-12-01 标题 :Enediyne quinone imines and methods of preparation and use thereof 发明人:DANISHEFSKY SAMUEL J; SHAIR MATTHEW D; YOON TAEYOUNG; CHOU TING-CHAO; MOSNY KAROLINE K 权利人:SLOAN KETTERING INST CANCER 摘要:A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R 1 , R 2 and R 3 are independently the same or different and are H, Br, Cl, F, NH 2 , CO 2 H, OH, linear or branched alkyl, etc.; wherein R 4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R 5 is H, Br, Cl, F, Oâ•?, OH or S--SR, or linear or branched alkyl, etc.; wherein R 6 is H, Br, Cl, F, CO 2 H, OH or S--SR', or linear or branched alkyl, etc.; wherein R 7 is H, OH or S--SR', or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R' are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl. Also provided are conjugates of the compound with cleavable peptides, enzymes, carbohydrates and monoclonal antibodies immunoreactive with cancer cells, as well as compositions comprising the analogues and conjugates, and methods of synthesis and treatment of tumos.
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合成参考文献
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