68709-74-0Relevant academic research and scientific papers
Angiotensin I-converting enzyme (ace) inhibitors
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Page/Page column 9-10, (2009/12/04)
This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.
Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors
Nchinda, Aloysius T.,Chibale, Kelly,Redelinghuys, Pierre,Sturrock, Edward D.
, p. 4612 - 4615 (2007/10/03)
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 P2
