反应详情

In an analogous manner to that described for the preparation of Building block A [e)], the cyclization of (RS)-N-[1-(5-bromo-2-fluoro-phenyl)-1-cyclopropyl-2-hydroxy-ethyl]-2-chloro-acetamide with potassium tert-butoxide in tent-butanol at room temperature overnight yielded the (RS)-5-(5-bromo-2-fluoro-phenyl)-5-cyclopropyl-morpholin-3-one as a yellow oil (2.146 g, 88% of theory). Mass (calculated) C13H13BrFNO2 [314.153]; (found) [M+H]+=314, [M+2-H]+=316.