Iqbal Muhammad Asif, Lu Le, Mehmood Hina, Khan Dost Muhammad, Hua Ruimao
Department of Chemistry, Key Laboratory of Organic Optoelectronics & Molecular Engineering of Ministry of Education, Tsinghua University, Beijing 100084, China.
ACS Omega. 2019 May 7;4(5):8207-8213. doi: 10.1021/acsomega.9b00699. eCollection 2019 May 31.
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.
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。
