Development of Two Complementary Syntheses for a Privileged CGRP Receptor Antagonist Substructure
Organic Process Research & Development2012Vol. 16(2), pp. 244–249
Citations Over TimeTop 21% of 2012 papers
David K. Leahy, Lopa V. Desai, Rajendra P. Deshpande, Antony V. Mariadass, Sundaramurthy Rangaswamy, Santhosh K. Rajagopal, Lakshmi Madhavan, Shashidhar Illendula
Abstract
1-(Piperidin-4-yl)-1H-imidazo[4,5-b]pyridin-2(3H)-one (1) is a privileged substructure found in >1000 unique CGRP receptor antagonists. Two practical and efficient syntheses of 1 are described from complementary starting materials. One route features a chemoselective reductive amination, while the second route utilizes a Pd-catalyzed amination using an ammonia surrogate to overcome an issue of poor selectivity.
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