The compounds of formula (I)
wherein R1, R2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
Iminium carbonic acid derivative salts.<b>IX</b>. Synthesis of<i>N,S</i>-containing heterobicycles from<i>N</i>-protected 2-methylthio-1,3-thiazinium and 2-methylthiothiazolium salts part 1. Preparation of<i>N</i>-protected 2-methylthio-1,3-thiazinium and 2-methylthiothiazolium salts and their reaction with CH-acidic compounds
by methyl iodide or trimethyloxonium tetrafluoroborate. This activated species were reacted with CH-acidic compounds forming ketene-N,S-acetals. The protection group was removed with trifluoracetic acid to yield the N-unsubstituted ketene-N,S-acetals.
N -Boc保护的1,3-噻嗪-2-硫酮和噻唑烷-2-硫酮通过甲基碘或四氟硼酸三甲基氧鎓转化为相应的2-甲硫基-1,3-噻嗪鎓盐和2-甲基硫代噻唑鎓盐。该活化的物质与CH-酸性化合物反应形成烯酮-N,S-乙缩醛。用三氟乙酸除去保护基,得到N-未取代的烯酮-N,S-乙缩醛。
Heterocyclic sulfonamides
申请人:Hoffmann-La Roche Inc.
公开号:US06417360B1
公开(公告)日:2002-07-09
The compounds of formula (I)
wherein R1 has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
Perfluorinated rare earth metals catalyzed reactions of 5-methylene-2-oxazolidinone and 5-methylene-1,3-thiazolidine-2-thione with isocyanates
作者:Min Shi、Yu-Mei Shen
DOI:10.1016/s0022-1139(01)00384-0
日期:2001.7
5-Methylene-2-oxazolidinone (1) and 5-methylene-1,3-thiazolidine-2-thione (2) can react effectively with various isocyanates to give the corresponding condensed urethanes in high yields in the presence of perfluorinated rare earth metal catalyst under mild conditions.
Transition-Metal-Catalyzed Reactions of Propargylamine with Carbon Dioxide and Carbon Disulfide
作者:Min Shi、Yu-Mei Shen
DOI:10.1021/jo0014966
日期:2002.1.1
The reactions of propargylamine derivatives with carbondioxide and carbondisulfide have been systematically examined in the presence of transition-metal catalysts. Pd(OAc)(2) is the best catalyst for the formation of the corresponding oxazolidinones. In addition, we found that, in the reaction of propargylamine with carbondioxide catalyzed by palladium(0) metal catalyst in toluene, both oxazolidinone