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An improved solvent-free synthesis of flunixin and 2-(arylamino) nicotinic acid derivatives using boric acid as catalyst

机译:以硼酸为催化剂的氟尼辛和2-(芳基氨基)烟酸衍生物的改进的无溶剂合成

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摘要

A simple solvent-free protocol for the preparation of flunixin, a potent non-narcotic, non-steroidal anti-inflammatory drugs is reported using boric acid as catalyst. Its salt, flunixin meglumine are then prepared under reflux in EtOH. This sustainable method are then extended for the synthesis of a series of 2-(arylamino) nicotinic acid derivatives. The present protocol combines non-hazardous neat conditions with associated benefits like excellent yield, straightforward workup, and use of readily available and safe catalyst in the absence of any solvent, which are important factors in the pharmaceutical industry. The pathway for catalytic activation of 2-chloronicotic acid with boric acid was also investigated using Gaussian 03 program package. Electronic supplementary materialThe online version of this article (10.1186/s13065-017-0355-4) contains supplementary material, which is available to authorized users.
机译:据报道,使用硼酸作为催化剂,可轻松制备氟尼辛(一种有效的非麻醉性,非甾体类抗炎药)的无溶剂方案。然后在乙醇中回流下制备其盐氟尼辛葡甲胺。然后将这种可持续的方法扩展到合成一系列的2-(芳基氨基)烟酸衍生物。本方案将无危险的纯净条件与相关的优点相结合,例如优异的收率,直接的后处理以及在没有任何溶剂的情况下使用易于获得且安全的催化剂,这是制药行业的重要因素。还使用高斯03程序包研究了用硼酸催化活化2-氯氰酸的途径。电子补充材料本文的在线版本(10.1186 / s13065-017-0355-4)包含补充材料,授权用户可以使用。

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