专利号:WO-0125179-A1 优先权日:1999-10-01 标 题:Preparation of tetracyclic intermediates 发明人:CHEN QING PING; WOODS ROSS ALEXANDER; ELLIOTT ROBYN LOUISE 权利人:INST OF DRUG TECHNOLOGY AUSTRA; CHEN QING PING; WOODS ROSS ALEXANDER; ELLIOTT ROBYN LOUISE 摘要:The invention provides a process for preparing deoxytetracyclic compounds of formula (I) useful in the synthesis of anthracyclines by the rearrangement of thiono ester derivatives followed by reduction, as well as intermediates useful therefor. In said formula, R is H or optionally protected OH.
专利号:US-7259263-B2 优先权日:2005-06-29 标题:Method of synthesis of azole-containing amino acids 发明人:HLASTA DENNIS J; ZIFICSAK CRAIG A 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): n nThe invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.
专利号:EP-1904465-B1 优先权日:2005-06-29 标 题 :Method of synthesis of imidazole-amino acid derivatives and related compounds 发明人:HLASTA DENNIS J; ZIFICSAK CRAIG A 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I). The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.
专利号:US-7678789-B2 优先权日:2005-02-11 标 题 :[1,2,4]-dithiazoli(di)ne derivatives, inducers of gluthathione-S-transferase and NADPH quinone oxido-reductase, for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular 发明人:FEENSTRA ROELOF W; KEIZER HISKIAS G; PRAS-RAVES MARIA L; VAN VLIET BERNARD J; VAN SCHARRENBURG GUSTAAF J M 权利人:SOLVAY PHARM BV 摘要:The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): n nwhereinn nwherein the symbols have the meanings given in the specification.
专利号:US-7208613-B2 优先权日:2002-06-20 标 题:Synthesis of s-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate 发明人:JADAV KANAKSINH JESINGBHAI; KAMBHAMPATI SUDHAKAR; CHITTURI TRINADHA RAO; THENNATI RAJAMANNAR 权利人:SUN PHARMACEUTICAL IND LTD 摘要:The present invention provides a convenient process for the preparation of S-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate, a compound of formula 1, comprisingn (a) treating 17β-[(N,N-dimethylcarbamoyl)thio]carbonyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene, a compound of formula 3 with alkali metal carbonate-alcohol system to obtain 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioic acid, a compound of formula 4; (b) reacting the compound of formula 4 with bromofluoromethane to yield the compound of formula 1.
专利号:US-2025179033-A1 优先权日:2021-12-30 标 题 :New antiviral triazole derivatives, their synthesis and their use for treatment of mammalian viral infections 发明人:MAKAROV VADIM; RIABOVA OLGA; LANE THOMAS R; EKINS SEAN 权利人:COLLABORATIONS PHARMACEUTICALS INC; FEDERAL RES CENTER FUNDAMENTALS OF BIOTECHNOLOGY RUSSIAN ACADEMY OF SCIENCE 摘要:A family of triazole derivatives is described. Also described is the use of these triazole derivatives in treating or preventing viral infections, such as human immunodeficiency virus (HIV) infections, and the diseases caused by these infections, such as acquired immunodeficiency syndrome (AIDS). The triazole derivatives, for example, comprise a central triazole group with two substituents comprising an aryl or heteroaryl group. Exemplary derivatives showed excellent HIV inhibitory activity against both wild-type and selected mutant strains of HIV.
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合成参考文献
参考文献:10.1007/s00894-011-1169-2 摘要:Singh DV, Adeppa K, Misra K. Mechanism of isoproturon resistance in Phalaris minor: in silico design, synthesis and testing of some novel herbicides for regaining sensitivity. Journal of Molecular Modeling. 2011 Jul 15;18(4):1431–45. doi: 10.1007/s00894-011-1169-2.