Synthesis and Antiobesity Properties of 6‑(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)­methoxy)-3-methoxyphenyl)­thieno[3,2‑<i>d</i>]pyrimidin-4(3<i>H</i>)‑one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound <b>2b</b> is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound <b>10</b>) as a highly efficacious antiobesity agent with a relatively clean in vitro and in vivo safety profile