Hernández Andrés S, Swartz Stephen G, Slusarchyk Dorothy, Yan Mujing, Seethala R Krishna, Sleph Paul, Grover Gary, Dickinson Kenneth, Giupponi Leah, Harper Timothy W, Humphreys W Griffith, Longhi Daniel A, Flynn Neil, Murphy Brian J, Gordon David A, Biller Scott A, Robl Jeffrey A, Tino Joseph A
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
Bioorg Med Chem Lett. 2008 Mar 15;18(6):2067-72. doi: 10.1016/j.bmcl.2008.01.100. Epub 2008 Jan 31.
1H-tetrazole-1-alkanenitrile SR-9g exhibits a >10-fold in vivo potency enhancement over the lead nitrile 1 and has acceptable oral bioavailability in rats and dogs. An enantiospecific synthesis of 1H-tetrazole-1-alkanenitrile nitriles 9 has been developed.
1H-四唑-1-链烷腈SR-9g在体内的效力比先导腈1提高了10倍以上，并且在大鼠和狗中具有可接受的口服生物利用度。已开发出1H-四唑-1-链烷腈9的对映体特异性合成方法。
