Improved Practical Synthesis of DY-038, an Oral Available Antiplatelet Agent

摘要

Recently, we reported the promising activity of a series of novel bicyclic pyridine derivatives as antiplatelet agents. Herein, we describe a modified and improved chemical synthesis of the lead compound, 1-(3-cyano-5-oxo-5,7-dihydrofuro[3,4-b] pyridin-2-yl)-4-methyl-N-((4-methylbenzyl)sulfonyl)piperidine-4- carboxamide (1), with the aim to produce from milligrams to 10 g of the pure compound that is necessary for the preclinical studies.