Determination of the absolute configuration of two αvβ6 integrin inhibitors for the treatment of idiopathic pulmonary fibrosis and investigations on the asymmetric 1,4-addition of arylboronic acids to crotonate esters bearing a C4-oxygen substituent

Add time:07/12/2019    Source:sciencedirect.com

The absolute configuration of two novel αvβ6 integrin inhibitors was established via degradation to the corresponding C3-aryl substituted butyrolactone. The configuration of the resulting lactones was established by asymmetric synthesis using 1,4-addition of arylboronic acids to butenolide, catalysed by bis(norbornadiene)rhodium (I) tetrafluoroborate in the presence of (R)-BINAP, and confirmed by X-ray crystallography. Studies on arylboronic acid conjugate additions to acyclic crotonate esters bearing a γ-oxygen substituent are also reported. Three Rh catalysts were investigated and the one giving the highest enantioselectivity was bis(norbornadiene)rhodium (I) tetrafluoroborate.

We also recommend Trading Suppliers and Manufacturers of 5-Benzyloxy-2-chlorophenylboronic acid (cas 1256346-10-7). Pls Click Website Link as below: cas 1256346-10-7 suppliers

Prev:4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP)
Next:Mutagenicity of anthraquinone and benzanthrone derivatives in the salmonella/microsome test: Activation of anthraquinone glycosides by enzymic extracts of rat cecal bacteria)