1.
Org Lett
; 12(22): 5146-9, 2010 Nov 19.
Article
in English
| MEDLINE
| ID: mdl-20945851
ABSTRACT
A scalable synthesis of a potent renin inhibitor (1) is described. The absolute stereochemistry is set via an unprecedented diastereoselective Dieckmann cyclization directed by a remote chiral protecting group. This transformation enables preparation of chiral 1,3-[3.3.1]-diazabicyclononenes by desymmetrization of alkyl-esters, with selectivities ranging from 4 to 17:1.