期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 4, 期 6, 页码 514-516出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml400045j
关键词
Metabolic stability; metabolism; clearance; tertiary butyl; tert-butyl; t-butyl
Susceptibility to metabolism is a common issue with the tert-butyl group on compounds of medicinal interest. We demonstrate an approach of removing all the fully sp(3) C-Hs from a tert-butyl group: replacing some C-Hs with C-Fs and increasing the s-character of the remaining C-Hs. This approach gave a trifluoromethylcyclopropyl group, which increased metabolic stability. Trifluoromethylcyclopropyl-containing analogues had consistently higher metabolic stability in vitro and in vivo compared to their tert-butyl-containing counterparts.
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