Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 17, Pages 4612-4615Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.06.003
Keywords
ACE inhibitor; Keto-ACE; Horner-Emmons; olefination
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Novel analogues of the angiotensin I-converting enzyme (ACE) inhibitor keto-ACE were synthesized via a facile Horner-Emmons olefination of a phosphonoketone precursor with ethyl glyoxylate. Introduction of a bulky aromatic tryptophan at the P'(2) position of keto-ACE resulted in a significant increase in C-domain-selectivity. (c) 2006 Elsevier Ltd. All rights reserved.
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