发明名称 Hydroxy methyl benzothiazine di:oxide carboxylic acid derivs. prepn.
摘要 Derivs. of 4-hydroxy 2-methyl 2H(1,2)-benzothiazine 1,1-dioxide 3-carboxylic acid of formula (I), in which R is an aminic radical, for use as anti-inflammatory agents, are made by (a) carboxylating a cpd. of formula (II) with methyl Mg carbonate or similar to obtain cpds of formula (III); (b) mesylating to obtain (IV), in which P is mesyl; (c) forming an adduct with dimethyl acetamide or other N,N-dialkyl amide; (d) treatment with thionyl chloride in inert solvent, in presence of an amine e.g. 2-amino pyridine, 3-amino 5-methyl thiazole or 2-amino thiazole, to give cpds. of formula (I) with 98% purity.
申请公布号 ES8702386(A1) 申请公布日期 1987.03.16
申请号 ES19740005500 申请日期 1985.12.18
申请人 URQUIMA,S.A. 发明人
分类号 A61K31/54;C07D279/02;(IPC1-7):C07D279/02 主分类号 A61K31/54
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