发明名称 AMINOBENZENESULFONIC ACID DERIVATIVE
摘要 NEW MATERIAL:A compound expressed by formula I (R1 is H, 1-6C alkyl, 3-7C cycloalkyl, 1-4C halogenated alkyl, halogen or 6-12C aryl; R2 is H, 1-6C alkyl or 7-12C aralkyl which may have a substituent group; n is 1-4) or pharmaceutically acceptable salt thereof. EXAMPLE:2-(1-Piperazinyl)-5-methylbenzenesulfonic acid. USE:A remedy for ischemic cardiopathy, cardiac insufficiency, hypertension, arrhythmia, etc., capable of inhibiting excessive accumulation of intracellular Ca<2+> without side effects on circulatory systems. PREPARATION:An aniline expressed by formula II is reacted with isocyanic acid, etc., in a polar solvent, such as acetic acid, to provide a compound expressed by formula III, which is then sulfonated and then hydrolyzed to afford an aminobenzenesulfonic acid. The resultant aminobenzenesulfonic acid is subsequently reacted with an amine expressed by formula IV in a polar solvent, such as water or ethanol, at 50-200 deg.C to provide the compound expressed by formula I.
申请公布号 JPH037263(A) 申请公布日期 1991.01.14
申请号 JP19900064811 申请日期 1990.03.15
申请人 MITSUBISHI KASEI CORP 发明人 OKUJIMA HIROMI;KOBAYASHI MAKIO;SATO NAOYA;MORITA MIYUKI;NARIMATSU AKIHIRO
分类号 C07D243/08;A61K31/415;A61K31/495;A61K31/55;A61P3/00;A61P9/00;A61P9/06;A61P9/10;A61P9/12;C07D233/02;C07D295/08;C07D295/096 主分类号 C07D243/08
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