专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-5916899-A 优先权日:1996-10-18 标 题:Isoquinoline derivatives and isoquinoline combinatorial libraries 发明人:KIELY JOHN S; GRIFFITH MICHAEL C 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinolines as well as novel libraries comprised of many such compounds, and methods of synthesizing the libraries.
专利号:US-6111110-A 优先权日:1996-10-30 标 题 :Synthesis of benzo[f]quinolinones 发明人:BRENNAN JOHN; DOECKE CHRISTOPHER WILLIAM; HEATH PERRY CLARK; PATTERSON LAWRENCE EDWARD; UDODONG UKO EFFIONG; WEIGEL LELAND OTTO 权利人:LILLY CO ELI 摘要:A process for preparing intermediates and benzoquinolin-3-one pharmaceuticals, such pharmaceuticals are effective in treating conditions consequent on 5α-reductase.
专利号:US-4476315-A 优先权日:1982-04-30 标 题:Nucleophilic substitution process 发明人:STAHLY G PATRICK; STAHLY BARBARA C 权利人:ETHYL CORP 摘要:Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.
专利号:US-4499026-A 优先权日:1982-08-25 标题 :Nucleophilic substitution process 发明人:STAHLY BARBARA C; STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Nitroarylacetonitriles are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetonitrile in an inert solvent and in the presence of a base so that the nitrile undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their nitriles are useful intermediates for the synthesis of pharmaceuticals.
专利号:US-4124768-A 优先权日:1975-09-24 标题:Process for preparing pure substituted 2,5-diarylamino-terephthalates and the corresponding free acids 发明人:KIRSCH ALOYS; FUCHS OTTO; SPIETSCHKA ERNST 权利人:HOECHST AG 摘要:2,5-Diarylamino terephthalates are obtained in good yields and excellent purity when the aromatic nitro compound used for oxidizing the corresponding dihydro-2,5-diarylamino terephthalate contains the aromatic radical of said diarylamino groups, i.e. when the amine formed during the oxidation is that from which said diarylamino groups device. The products yield very pure quinacridone pigments and allow the synthesis of only one isomer of substituted quinacridones.
摘要:Mutation Research, 393,23,1997 摘要:Proceedings of the National Academy of Sciences of the United States of America, 72,5135,1975 摘要:JNCI, Journal of the National Cancer Institute, 62,911,1979 摘要:Mutation Research, 216,211,1989 摘要:Mutation Research, 608,88,2006