The synthesis of potent marcocyclic renin inhibitors
作者:Daljit S. Dhanoa、William H. Parsons、William J. Greenlee、Arthur A. Patchett
DOI:10.1016/s0040-4039(00)91716-7
日期:1992.3
An efficient synthesis of a novel class of potent macrocylic renininhibitors exemplified by compounds 1 and 2, which involves the marcocyclization of 8 and 9 as the key step, is described. The macrocyclic design of renininhibitors 1 and 2 disclosed here incorporates (2R,3S)-3-amino-4-cyclohexyl-2-hydroxybutanoic acid (norACHPA) as the transition-state isostere. Determination of stereochemistry of