Recommanded Product: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 126456-43-7, Name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol,introducing its new discovery.
Systematic modifications of HIV protease inhibitor (2R,3S,4S)-4- [[(benzyloxycarbonyl)-L-valyl]amino]-3-hydroxy-2-[(4-methoxybenzyl)amino]-5- (phenylpentanoyl)-L-valine 2-(aminomethyl)-benzimidazole amide led to a novel series of inhibitors with a shortened, modified carboxy terminus. Their synthesis, in vitro enzyme inhibitory data, and antiviral activities are reported. Of particular interest are derivatives featuring the (1S,2R)-1- amino-2-hydroxyindan moiety at the P2′-position since some of them exhibit substantial oral bioavailability in mice. The influence of aqueous solubility and structural parameters on the oral resorption of the inhibitors is discussed. Optimum enhancement of oral bioavailability was observed with L- tert-leucine in P2-position, resulting in the discovery of (2R,3S,4S)-4- [[(benzyloxycarbonyl)-L-tert-leucyl]amino]-3-hydroxy-2-[(4- methoxybenzyl)amino]-5-phenylpentanoic acid (1S,2R)-1-amino-2-hydroxyindan amide which combines high antiviral activity (IC50 = 250 nM) with a good pharmacokinetic profile (AUC = 82.5 muM · h at a dose of 125 mg/kg po in mice).
Future efforts will undeniably focus on the diversification of the new catalytic transformations. These may comprise an expansion of the substrate scope from aromatic and heteroaromatic compounds to other hydrocarbons. Recommanded Product: (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 126456-43-7, in my other articles.
Reference：
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis