Synthesis of tetrahydronaphthyl thioureas as potent appetite suppressants☆
摘要:
A series of thiourea derivatives (7-23, 25-27) of 1-aminotetrahydronaphthalene (4) and 1-amino-2-hydroxytetrahydronaphthalene (5) were synthesized in single pot in 48-90% yield and evaluated for their anorexigenic activity. Among them compounds 10, 14 15, 16 and 22 exhibited significant anorexigenic activity without any antidepressant effect and provided a new structural lead for appetite suppressants. (C) 2004 Elsevier Ltd. All rights reserved.
Selective C(sp3)–H isothiocyanation represents a significant strategy for the synthesis of isothiocyanate derivatives. We report herein an electrochemicalbenzylic isothiocyanation in a highly chemo- and site-selective manner under external oxidant-free conditions. The high chemoselectivity is attributed to the facile in situ isomerization of benzylic thiocyanates to isothiocyanates. Notably, the method