Ashworth, Ian W. published the artcileProcess Development of a Suzuki Reaction Used in the Manufacture of Lanabecestat, HPLC of Formula: 917471-30-8, the main research area is lanabecestat preparation; Suzuki coupling diethanolamine alkynylpyridinylboronate bromodispirocyclohexaneindaneimidazole key step; hydrolysis kinetics diethanolamine alkynylpyridinylboronate; effect diethanolamine removal palladium lanabecestat.
A process for preparation of the potential anti-Alzheimer’s agent lanabecestat was developed by coupling of an alkynylpyridinylboronic acid diethanolamine ester with a bromodispirocyclohexaneindaneimidazole in the presence of Pd(AmPhos)2Cl2 and K3PO4 in EtOH/H2O; the new process reduced the need for solvent changes and difficult isolation steps and decreased the amount of palladium detected in the final product without the use of solid-phase extractants. The kinetics of hydrolysis of the diethanolamine boronate and the free boronic acid was determined; diethanolamine generated in the hydrolysis decreased the rate of coupling but likely improved the purge of palladium from the product.
Organic Process Research & Development published new progress about Hydrolysis. 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, HPLC of Formula: 917471-30-8.