An efficient and cost-effective synthesis of 2-phenyl-3-aminopyridine
S Caron, SS Massett, DE Bogle…
文献索引:Caron, Stephane; Massett, Steve S.; Bogle, David E.; Castaldi, Michael J.; Braish, Tamim F. Organic Process Research and Development, 2001 , vol. 5, # 3 p. 254 - 256
The synthesis of 2-phenyl-3-aminopyridine, a key intermediate in the preparation of 2- phenyl-3-aminopiperidine, from 2-chloro-3-aminopyridine is described using an imine as a protecting group for an aminopyridine. The in situ protection of 2-chloro-3-aminopyridine with benzaldehyde followed by Suzuki coupling with phenylboronic acid and subsequent acid hydrolysis provided the titled compound in a single, high-yielding step from ...