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通过碱促进的氟代苯甲酰胺与酰胺的SAr反应然后环化合成喹唑啉酮。

Quinazolinone Synthesis through Base-Promoted SAr Reaction of -Fluorobenzamides with Amides Followed by Cyclization.

作者信息

Iqbal Muhammad Asif, Lu Le, Mehmood Hina, Khan Dost Muhammad, Hua Ruimao

机构信息

Department of Chemistry, Key Laboratory of Organic Optoelectronics & Molecular Engineering of Ministry of Education, Tsinghua University, Beijing 100084, China.

出版信息

ACS Omega. 2019 May 7;4(5):8207-8213. doi: 10.1021/acsomega.9b00699. eCollection 2019 May 31.

Abstract

A transition-metal-free synthesis of quinazolin-4-ones by CsCO-promoted SAr reaction of -fluorobenzamides with amides followed by cyclization in dimethyl sulfoxide has been developed. The present procedure can provide efficient synthetic methods for the formation of both 2-substituted and 2,3-disubstituted quinazolin-4-one rings depending on the use of easily available starting materials and an efficient, one-pot protocol for the synthesis of the marketed drug product of methaqualone.

摘要

通过碳酸铯促进的邻氟苯甲酰胺与酰胺的SAr反应,随后在二甲基亚砜中环化,开发了一种无过渡金属合成喹唑啉-4-酮的方法。根据易于获得的起始原料的使用情况,本方法可为形成2-取代和2,3-二取代的喹唑啉-4-酮环提供有效的合成方法,以及为合成安眠酮市售药品提供一种高效的一锅法方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/567d/6647956/7e2e903e8425/ao-2019-00699f_0002.jpg

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