Butylate → (R)-5-(5-amino-2-fluoro-phenyl)-5-methyl-morpholin-3-one hydrochloride

Participants

Reaction Steps

In close analogy to the reaction sequence described for the preparation of Building block C, the cyclization of the (R)-N-[1-(5-bromo-2-fluoro-phenyl)-2-hydroxy-1-methyl-ethyl]-2-chloro-acetamide with potassium tent-butylate, followed by the palladium-catalyzed amination, and, finally, by the hydrolysis yielded the (R)-5-(5-amino-2-fluoro-phenyl)-5-methyl-morpholin-3-one hydrochloride as a light yellow solid. Mass (calculated) C11H14ClN2O2 [260.698]; (found) [M+H]+=225.

Provenance & Evidence