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Method of preparation of carboxamides of the oxo - 1,2 benzothiazine preferably cannot, or substantially dioxides 1,1 - - -

机译:氧代-1,2-苯并噻嗪的羧酰胺的制备方法优选不能或基本上不能被氧化的1,2,1---

摘要

Disclosed herein is an improved process for the production of carboxamides of 3,4-dihydro-oxo-1,2-benzothiazine-1,1-dioxides. Said process comprises contacting either a 4-alkoxy-1,2-benzothiazine-3-carboxylic acid-1,1-dioxide or a 3-alkoxy-1,2-benzothiazine-4-carboxylic acid-1,1-dioxide with an amine followed by cleavage of the ether moiety with an appropriate reagent such as hydrogen bromide to produce a carboxanilide with previously disclosed pharmaceutical value as a non-steroidal anti inflammatory agent. The alkoxy-benzothiazine carboxylic acids are themselves novel compounds and valuable synthetic intermediates.
机译:本文公开了一种生产3,4-二氢-氧-1,2-苯并噻嗪-1,1-二氧化物的羧酰胺的改进方法。所述方法包括使4-烷氧基-1,2-苯并噻嗪-3-羧酸-1,1-二氧化物或3-烷氧基-1,2-苯并噻嗪-4-羧酸-1,1-二氧化物与胺,然后用适当的试剂(如溴化氢)裂解醚部分,制得羧苯甲酰苯胺,该苯甲酰苯胺作为非甾体类抗炎剂具有先前公开的药物价值。烷氧基-苯并噻嗪羧酸本身是新颖的化合物,也是有价值的合成中间体。

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