Efficient and Scalable Synthesis of Ethyl 2, 6-Dichloro-5-Fluoronicotinoyl Acetate Using the Blaise Reaction as a Key Step1

…, H Choi, YK Kim, KK Lee, KW Lee, JH Lee…

文献索引：Shin, Hyunik; Choi, Bo Seung; Lee, Ki Kon; Choi, Hyeong-Wook; Chang, Jay Hyok; Lee, Kyu Woong; Nam, Do Hyun; Kim, No-Soo Synthesis, 2004 , # 16 p. 2629 - 2632

全文：HTML全文

被引用次数: 16

摘要

An efficient synthesis of 2, 6-dichloro-5-fluoronicotinoyl acetate (1) has been accomplished in a single step using the Blaise reaction of ethyl bromoacetate with 3-cyano-2, 6-dichloro-5- fluoropyridine (4). Use of methanesulfonic acid as an in situ activator of zinc removed the induction period of the Blaise reaction to render it safe and viable for a large-scale operation.