A Convergent Kilogram-Scale Synthesis of the PPARα Agonist LY518674: Discovery of a Novel Acid-Mediated Triazolone Synthesis

…, ME LeTourneau, MJ Martinelli, CL Meyer…

文献索引：Braden, Timothy M.; Coffey, D. Scott; Doecke, Christopher W.; LeTourneau, Michael E.; Martinelli, Michael J.; Meyer, Christopher L.; Miller, Richard D.; Pawlak, Joseph M.; Pedersen, Steven W.; Schmid, Christopher R.; Shaw, Bruce W.; Staszak, Michael A.; Vicenzi, Jeffrey T. Organic Process Research and Development, 2007 , vol. 11, # 3 p. 431 - 440

全文：HTML全文

被引用次数: 6

摘要

The first kilogram-scale synthesis of the PPARα agonist LY518674 (1) is described. The de novo convergent synthetic approach involved coupling of two rapidly assembled components, triazolone formation via a novel acid-promoted cyclization reaction, and final step saponification, delivering the compound in 32.5% overall yield via eight total steps with a six-step longest linear sequence. A regioselective alkylation on the dianion of 4- ...