Synthesis and structure–activity relationships of novel benzofuran farnesyltransferase inhibitors
摘要:
A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC50 = 1.1 nM) and antitumor activity in human cancer xenografts in mice. (C) 2009 Published by Elsevier Ltd.
C(sp<sup>2</sup>)–H Borylation of Fluorinated Arenes Using an Air-Stable Cobalt Precatalyst: Electronically Enhanced Site Selectivity Enables Synthetic Opportunities
作者:Jennifer V. Obligacion、Máté J. Bezdek、Paul J. Chirik
DOI:10.1021/jacs.6b13346
日期:2017.2.22
Cobalt catalysts with electronically enhanced site selectivity have been developed, as evidenced by the high ortho-to-fluorine selectivity observed in the C(sp2)-H borylation of fluorinated arenes. Both the air-sensitive cobalt(III) dihydride boryl 4-Me-(iPrPNP)Co(H)2BPin (1) and the air-stable cobalt(II) bis(pivalate) 4-Me-(iPrPNP)Co(O2CtBu)2 (2) compounds were effective and exhibited broad functional
partially fluorinated arenes. A nickel-catalyzed cross-coupling between a polyfluoroarene and an organozincreagent in the presence of POP selectively produces a monosubstitution product. Aryl and alkylzinc reagents smoothly take part in the reaction. It is speculated that monosubstitution is the result of accelerated product expulsion from the product/catalyst complex.