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Short Paper | Regular issue | Vol 91, No. 7, 2015, pp.1445-1454
Published online, 22nd May, 2015
DOI: 10.3987/COM-15-13234
Development of a Facile and Inexpensive Route for the Preparation of α-Halobenzopyridines from α-Unsubstituted Benzopyridines

Osamu Sugimoto,* Hyuma Iwasaki, and Ken-ichi Tanji

*Laboratory of Organic Chemistry, School of Food and Nutritional Sciences, University of Shizuoka, 552-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan


A facile and inexpensive route for the preparation of α-halobenzopyridines from α-unsubstituted benzopyridines via N-methylbenzopyridin-α-ones was developed. α-Unsubstituted benzopyridines were converted easily into the corresponding N-methylbenzopyridin-α-ones, which were halogenated using PPh3-TCICA or PPh3-DBICA without using solvent to give α-halobenzopyridines.