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-4161609-A 优先权日:1977-09-14 标题:Synthesis of carboxylic acid esters 发明人:CRAMER RICHARD D 权利人:DU PONT 摘要:A method is provided for converting a carboxylic acid amide to a carboxylic acid ester by reacting a vaporized mixture of the amide and an aliphatic alcohol or a phenol in the presence of a suitable catalyst at temperatures of from 100 DEG C. to 400 DEG C. The process is especially useful for the conversion of methacrylamide to methyl methacrylate.
专利号:EP-0830136-B1 优先权日:1995-03-07 标 题:New cryptophycins from synthesis 发明人:MOORE RICHARD E; TIUS MARCUS A; BARROW RUSSELL A; LIANG JIAN; CORBETT THOMAS H; VALERIOTE FREDERICK A; HEMSCHEIDT THOMAS K; GOLAKOTI TRIMURTULU 权利人:UNIV HAWAII; UNIV WAYNE STATE 摘要:Novel cryptophycin compounds are disclosed, together with methods of producing cryptophycins by total synthesis and methods for the use of such cryptophycins in pharmaceuticals to inhibit the proliferation of mammalian cells and to treat neoplasia.
专利号:US-6013626-A 优先权日:1993-12-21 标题 :Cryptophycins from synthesis 发明人:MOORE RICHARD E; TIUS MARCUS A; BARROW RUSSELL A; LIANG JIAN; CORBETT THOMAS H; VALERIOTE FREDERICK A; GOLAKOTI TRIMURTULU; HEMSCHEIDT THOMAS K 权利人:UNIV HAWAII; UNIV WAYNE STATE 摘要:A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods of producing cryptophycins by total synthesis and methods of using cryptophycins in pharmaceuticals. It is a further object of this invention to use cryptophycins to inhibit the proliferation of mammalian cells. Moreover, methods of using cryptophycins to treat neoplasia is also provided.
专利号:US-5880146-A 优先权日:1995-06-07 标 题 :Inhibition of IL-12-induced IFN-γ synthesis by specific bis-phenol compounds as a method of immune modulation 发明人:GILLIES STEPHEN D; WESOLOWSKI JOHN 权利人:FUJI IMMUNOPHARMACEUTICALS COR 摘要:Disclosed are chemical agents for modulating certain cellular immune reactions that can lead to autoimmune disorders. By specific modulation, harmful immune reactions can be lessened in severity or even prevented without resorting to potentially dangerous general immune suppression. The described chemical agents inhibit IL-12 induction of the secretion of key immune modulators. The described chemical agents are specific inhibitors of IL-12 induced Th1 immune response.
专利号:US-4105668-A 优先权日:1975-01-10 标题:Process for 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam 发明人:NAKANISHI SUSUMU 权利人:PFIZER 摘要:Certain 6-amino-2,2-dimethyl-3-(1-substituted tetrazol-5-yl)penam and 6-(protected amino)-2,2-dimethyl-3-(1-substituted tetrazolyl-5-yl)penam compounds react with hydrogen fluoride to produce 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, a useful intermediate for the synthesis of antibacterial agents.
摘要:González-Bello, C., Science of Synthesis Knowledge Updates, (2018) 1, 245. 摘要:Selt, M.; Waldvogel, S. R., Science of Synthesis: Special Topics, (2021) 1, 258. 摘要:L. Sucha, Z. Urner and M. Suchanek, Collect. Czech. Chem. Commun. 35, 3651 (1970). 摘要:Angelini, E.; Sarlah, D., Science of Synthesis: Dearomatizations, (2026) . 摘要:Cunha, J. C.; Dedeiras, B.; Negrão, A. C. R.; Marques, M. M. B., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .