反应详情

Isopropylmagnesium chloride (5.19 mL of a 2.0 M solution in THF) was added over 20 min ot a solution of cyclopropylamine (1.830 mL) and methyl 2-fluoro-5-[3-{[1-(2-hydroxyphenyl)cyclopropyl]amino}-2-oxopyrazin-1(2H)-yl]-4-methylbenzoate (Example 318f, 1.063 g) in THF (20 mL) stirring at room temperature under nitrogen. The reaction mixture was stirred for 1 h. Water and 2 M HCl were cautiously added and the volatiles removed in vacuo. The residue was basified with saturated aqueous sodium bicarbonate solution and extracted into DCM. The organics were combined, dried (MgSO4) and evaporated to give the subtitle compound (1.189 g).

1. stirringThe reaction mixture was stirred for 1 h
2. customthe volatiles removed in vacuo
3. extractionextracted into DCM
4. dry with materialdried (MgSO4)
5. customevaporated