169701-56-8

Upstream product

• 68709-76-2 5(S)-<(butyloxycarbonyl)amino>-6-phenyl-4-oxohexanoic acid 
• 7524-50-7 methyl (2S)-2-amino-3-phenylpropanoate hydrochloride 
• 68709-74-0 ethyl (5S)-6-phenyl-5-[(tert-butyloxycarbonyl)amino]-4-oxo-hexanoate 

Relevant academic research and scientific papers

Angiotensin I-converting enzyme (ace) inhibitors

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

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

Synthesis of Xaa-Gly-Xaa' Keto-Methylene Tri-peptide Isosteres Incorporating Phenylalanine, Tyrosine and Valine Units.

The utility of amino-acid derived β-ketosulfones in the synthesis of keto-methylene tri-peptide isosteres Xaa-Gly-Xaa', incorporating phenylalanine, tyrosine and valine units is reported.Both L,L andL,D forms of the tripeptide systems have been prepared using this methodology.