1,3-丙二硫醇,三氯乙酸乙酯置于sodium Hydride体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 0.25H,以85%的收率获得1,3-二噻烷-2-甲酸乙酯 参考文献:A New Synthesis Of 2-Substituted-1,3-Dithianes From Trichloromethyl Compounds 标题:A New Synthesis Of 2-Substituted-1,3-Dithianes From Trichloromethyl Compounds 摘要:Trichloromethyl Compounds Are Efficiently Converted Into 1,3-Dithianes Upon Reaction With A Disodium 1,3-Propanedithiolate-1,3-Propanedithiol Mixture In Dmf Solution At 0 Degrees C. This Synthesis Is Limited To Those Substrates Where The Substituent Attached To The Trichloromethyl Group Is An Electron-Withdrawing Group. (C) 2006 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tetlet.2006.12.066
专利号:US-5399721-A 优先权日:1990-01-12 标题:Synthesis of optically pure 4-aryl-2-hydroxytetronic acids 发明人:HOPPER ALLEN T; WITIAK DONALD T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. the invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.
专利号:US-8324417-B2 优先权日:2009-08-19 标题:Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof 发明人:HART BARRY; DENER JEFF; GREEN MICHAEL; STANDEN MICHAEL; KOCIAN OLDRICH 权利人:HART BARRY; DENER JEFF; GREEN MICHAEL; STANDEN MICHAEL; KOCIAN OLDRICH; VIROBAY INC 摘要:The present invention relates to a process for the preparation of alkyl esters of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid, which are intermediates useful in the synthesis of (S)—N-(1-cyanocyclopropyl)-5-cyclopropyl-4,4-difluoro-2-((S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethylamino)pentanamide and related compounds, which are compounds that are cysteine protease inhibitors.
专利号:US-6960601-B2 优先权日:2001-09-24 标题 :Preparation and use of imidazole derivatives for treatment of obesity 发明人:SMITH ROGER A; O'CONNOR STEPHEN J; WIRTZ STEPHAN-NICHOLAS; WONG WAI C; CHOI SOONGYU; KLUENDER HAROLD C E; SU NING; WANG GAN; ACHEBE FURAHI; YING SHIHONG 权利人:BAYER PHARMACEUTICALS CORP 摘要:This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:US-4539410-A 优先权日:1982-09-30 标题:N-Substituted-2-(1-imidazolyl)indoles 发明人:RENFROE HARRIS B 权利人:CIBA GEIGY CORP 摘要:Various 1-carboxylic acid substituted-2-(1-imidazolyl)indoles and functional derivatives thereof are highly specific thromboxane synthetase inhibitors. Synthesis of, pharmaceutical compositions thereof, methods of treatment utilizing such compounds and intermediates for their synthesis are included.
专利号:US-5504108-A 优先权日:1990-01-12 标题:Optically pure 4-aryl-2-hydroxytetronic acids 发明人:WITIAK DONALD T; HOPPER ALLEN T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aidehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, and additionally as inhibitors of cyclooxygenase and 5-lipoxygenase. The invention further relates to the pharmaceutical use of such.compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis, and in the treatment of various inflammatory pathologies, especially arthritis.
专利号:US-4478842-A 优先权日:1981-11-19 标题:N-Substituted-2-pyridylindoles 发明人:RENFROE HARRIS B 权利人:CIBA GEIGY CORP 摘要:Various 1-carboxylic acid substituted-2-pyridylindoles and functional derivatives thereof are highly specific thromboxane synthetase inhibitors. Synthesis of, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds are included.
[参考文献]: Varinder K. Aggarwal, Et Al. Studies On The Asymmetric Oxidation Of Ester Derivatives Of 1,3-Dithiane-2-Carboxylates. Asymmetric Synthesis Of Trans-1,3-Dithiane 1,3-Dioxide. J Org Chem. 1998 Oct 16;63(21):7306-7310.
合成参考文献
摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 976.