Synthesis of haloperidol ethanedithioketal HIV-1 protease inhibitors: magnesium chloride facilitated addition of Grignard reagents

…, DL Decamp, J Li, CS Craik, PRO de Montellano

Index: Sui; De Voss; DeCamp; Li; Craik; Ortiz De Montellano Synthesis, 1993 , # 8 p. 803 - 808

Full Text: HTML

Citation Number: 5

Abstract

Haloperidol ketals and ethanedithioketals of interest as HIV-1 protease inhibitors were synthesized by addition of organolithium and organomagnesium reagents to ketone precursors already containing the ketal or thioketal functionality. Addition of Grignard reagents to the thioketal containing ketone was enhanced remarkably, and to the ketal containing ketone moderately, by the addition of magnesium chloride. The effect of ...