Exploratory Process Development of a Novel Diacylglycerol Acyltransferase-1 (DGAT-1) Inhibitor
…, KB Bahnck, MJ Munchhof, A Nematalla…
文献索引：Shavnya, Andrei; Tao, Yong; Lilley, Susan C.; Bahnck, Kevin B.; Munchhof, Michael J.; Nematalla, Asaad; Waldo, Michael; Bill, David R. Organic Process Research and Development, 2013 , vol. 17, # 12 p. 1510 - 1516
A practical large-scale synthesis was developed for 1, a DGAT-1 inhibitor, involving an aza- Michael reaction, amidation, Dieckman cyclization, and conjugate addition of cyanamide followed by cyclization, to form the fused 4-amino-7, 8-dihydropyrido [4, 3-d] pyrimidin-5-one scaffold. The enabled process presented here substantially improved safety (in particular, due to eliminating a nitration step and optimizing a high-energy intermediate step), ...
