136010-42-9Relevant academic research and scientific papers
A practical synthesis of the dihydroxyethylene dipeptide isostere, (2S, 3R, 4S) 2-[(tert-butyloxycarbonyl)amino]-1-cyclohexyl-3,4-dihydroxy-6-methylheptane, from D-isoascorbic acid
Baker, William R.,Condon, Stephen L.
, p. 1581 - 1584 (1992)
The N-Boc dihydroxyethylene dipeptide isostere 7 and its N-Boc 3-(thiazol-4-yl)alanyl derivative 8 were synthesized, without purification of intermediates, from (4S,5R)-2,2-dimethyl-4-(2-methylpropyl)-5-hydroxymethyl-1,3-dioxolane (3b), in 24 and 32% over
An efficient process for the synthesis of renin inhibitor, ABT-517
Singam, Pulla Reddy,Bradshaw, Curt W.,Menzia, Jerome A.,Narayanan,Rockway, Todd W.,Welch, Noel,Tien, Jien-Heh J.
, p. 2751 - 2756 (2007/10/03)
An efficient process for the preparation of renin inhibitor, ABT-517 is described. The process avoids solvent extractions or chromatographic purfications and is used on multi-kilogram scale.
Dipeptide Isosteres. 1. Synthesis of Dihydroxyethylene Dipeptide Isosteres via Diastereoselective Additions of Alkyllithium Reagents to N,N-Dimethylhydrazones. Preparation of Renin and HIV-1 Protease Inhibitor Transition-State Mimics
Baker, William R.,Condon, Stephen L.
, p. 3277 - 3284 (2007/10/02)
The amino and diamino dihydroxyethylene dipeptide isosteres 19a,b and 23 are important intermediates for the preparation of inhibitors of human renin and HIV-1 protease, respectively.A general synthetic strategy was developed to access both dipeptide isos
1,2,3-Trisubstituted Cyclopropanes as Conformationally Restricted Peptide Isosteres: Application to the Design and Synthesis of Novel Renin Inhibitors
Martin, Stephen F.,Austin, Richard E.,Oalmann, Christopher J.,Baker, William R.,Condon, Stephen L.,et al.
, p. 1710 - 1721 (2007/10/02)
The 1,2,3-trisubstituted cyclopropanes 6 and 7 are the first members of a novel class of isosteric replacements for peptide linkages that are more generally represented by the dipeptide mimics 2 and 3.These unique peptide surrogates are specifically desig
