反应详情

Preparation of example 246 from Intermediate 147(d) of Example 147 (300 mg, 0.794 mmol) was carried out in three steps in a manner similar to that described for the preparation of Example 233 except that 4-prop-2-ynyl-morpholine was used instead of dimethyl-prop-2-ynyl-amine in step 1. 4-Prop-2-ynyl-morpholine was prepared by refluxing 3-bromo-propyne, morpholine and K2CO3 in tetrahydrofuran for 1 hour. The title compound (34 mg, 0.073 mmol) was obtained as a yellow powder in 18% overall yield.