Center for Metareceptome Research, College of Pharmacy, Chung-Ang University , 84 Heukseok-ro, Dongjak, Seoul 06974, Republic of Korea.
Org Lett. 2017 Jan 20;19(2):312-315. doi: 10.1021/acs.orglett.6b03348. Epub 2016 Dec 30.
A facile synthetic method to chromenones and thiochromenones has been developed using a one-pot Friedel-Crafts acylation of alkynes with suitably substituted benzoyl chlorides. This unified approach to (thio)chromenones is readily applicable to aryl- and alkylalkynes where the stereochemically well-defined β-chlorovinyl ketone intermediates undergo distinctively different cyclization pathways. The ready availability of both starting materials, alkynes and benzoyl chlorides, coupled with the experimental simplicity makes the current synthetic method to (thio)chromenones fast, efficient, and practical.
已经开发出一种简便的合成色烯酮和噻吩色烯酮的方法，该方法使用炔烃与适当取代的苯甲酰氯的一锅 Friedel-Crafts 酰化反应。这种（硫）色烯酮的统一方法适用于芳基和烷基炔烃，其中立体化学定义明确的β-氯代乙烯基酮中间体经历明显不同的环化途径。由于起始原料炔烃和苯甲酰氯都容易获得，并且实验操作简单，因此当前合成（硫）色烯酮的方法快速、高效且实用。
