Tetrahedron letters

The synthesis of potent marcocyclic renin inhibitors

DS Dhanoa, WH Parsons, WJ Greenlee, AA Patchett

Index: Dhanoa, Daljit S.; Parsons, William H.; Greenlee, William J.; Patchett, Arthur A. Tetrahedron Letters, 1992 , vol. 33, # 13 p. 1725 - 1728

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Citation Number: 21

Abstract

Abstract An efficient synthesis of a novel class of potent macrocylic renin inhibitors exemplified by compounds 1 and 2, which involves the marcocyclization of 8 and 9 as the key step, is described. The macrocyclic design of renin inhibitors 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 the substituent R ( ...