B. Pita et al., A simple, efficient method for regioselective synthesis of 7-aminomethyl-7,8-dihydro-6H-quinolin-5-new potential CNS agents, TETRAHEDR L, 41(50), 2000, pp. 9829-9833
We have developed an efficient and convenient strategy for the regioselecti
ve synthesis of new conformationally restricted butyrophenones of the quino
line series. The 7-aminomethyl-7,8-dihydro-6H-quinolin-5-ones 9 were obtain
ed from protected alcohol 5 via the tosylate, and also in a one-pot reactio
n via bromo derivative 6, with moderate-to-good overall yields in both case
s. (C) 2000 Elsevier Science Ltd. All rights reserved.