合成含氟4-酰基氨基-4,5,6,7-四氢苯并异恶唑的有效方法

T. S. Khlebnicova, Yu. A. Piven, I. Gerus, A. Sorochinsky, F. Lakhvich
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引用次数: 0

摘要

以4-乙酰氨基-3-氟烷基(芳基)-4,5,6,7-四氢-1,2-苯并异恶唑的合成为例,提出了合成新型4-乙酰氨基-4,5,6,7-四氢-1,2-苯并异恶唑的有效方法。在异丙醇中用硼氢化钠还原3-氟烷基(芳基)- 6,7-二氢-1,2-苯并恶唑-4-酮,得到3-氟烷基(芳基)- 4,5,6,7-四氢-1,2-苯并恶唑-4-醇,并在Ritter反应(乙腈、乙酸、硫酸)条件下得到目标4-酰基胺衍生物,产率为80 - 94%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Effective approach to a synthesis of fluorine-containing 4-acylamino-4,5,6,7-tetrahydrobenzisoxazoles
On the example of synthesis of 4-acetylamino-3-fluoroalkyl(aryl)-4,5,6,7-tetrahydro-1,2-benzisoxazoles, the effective approach to a synthesis of novel 4-acylamino-4,5,6,7-tetrahydro-1,2-benzisoxazoles is proposed. 3-Fluoroalkyl(aryl)- 6,7-dihydro-1,2-benzisoxazol-4-ones were reduced by a sodium borohydride in isopropanol to obtain 3-fluoroalkyl(aryl)- 4,5,6,7-tetrahydro-1,2-benzisoxazol-4-ols that in the conditions of the Ritter reaction (acetonitrile, acetic acid, sulfuric acid) gave target 4-acylamino derivatives with 80–94 % yields.
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