Synthetic method of 3-cyclopropyl-benzeneboronic acid
The invention discloses a synthetic method of 3-cyclopropyl-benzeneboronic acid, and belongs to the technical field of organic synthesis. The synthetic method comprises the steps: 3-chlorobromobenzeneand cyclopropylboronic acid serve as starting raw mater
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Paragraph 0027; 0030; 0031; 0034; 0035; 0038
(2019/12/25)
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
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.
Procopiou, Panayiotis A.,Barrett, Tim N.,Copley, Royston C.B.,Tame, Christopher J.
p. 1384 - 1393
(2017/11/09)
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