专利号:US-5663342-A 优先权日:1994-03-08 标 题 :2-chloro and 2-bromo derivatives of 1,5-iminosugars 发明人:BARTA THOMAS E; MUELLER RICHARD A 权利人:SEARLE & CO 摘要:Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.
专利号:US-4552984-A 优先权日:1982-01-21 标题 :Process for preparation of α,α-difluoroalkoxy or α,.alpha. 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of alpha , alpha -difluoroalkoxy or alpha , alpha -difluoroalkylthiophenyl sulfones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a sulfonic acid, a derivative or a precursor of this acid, in the presence of boron trifluoride in an amount such that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-2010204463-A1 优先权日:2007-08-07 标题 :Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation 发明人:LIOTTA DENNIS C; LI YONGFENG 权利人:LIOTTA DENNIS C; LI YONGFENG 摘要:This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.
专利号:US-4554381-A 优先权日:1982-01-21 标题:Process for sulfonylation of halobenzenes 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for sulfonylation of halobenzenes, in which a halobenzene is reacted with a sulfonic acid, a precursor or a derivative thereof in the presence of boron trifluoride in an amount such that the absolute pressure of boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:WO-2005058810-A1 优先权日:2003-12-17 标题:Novel intermediates for the synthesis of (r)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation
专利号:JP-2009505954-A 优先权日:2005-07-21 标题 :Interleukin-1 and tumor necrosis factor-a modifier, synthesis of such modifiers and methods of using such modifiers