反应详情

A vial was charged with (±)-(E)-2-(7-bromo-1′-(3-(2-(trifluoromethyl)phenyl)acryloyl)-2,3-dihydrospiro[indene-1,4′-piperidine]-3-yl)acetic acid (5 mg, 0.01 mmol), N,N′-dimethylethylenediamine (0.007 mL, 0.066 mmol), HOBt (3 mg, 0.02 mmol), i-Pr2NEt (0.006 mL, 0.032 mmol) and CH2Cl2 (1 mL). EDC.HCl (4 mg, 0.021 mmol) was added. The mixture was stirred at rt for 1 d and evaporated to dryness. The residue was purified by preparative HPLC to afford (±)-(E)-2-(7-chloro-1′-(3-(2-(trifluoromethyl)phenyl)acryloyl)-2,3-dihydrospiro[indene-1,4′-piperidine]-3-yl)-N-methyl-N-(2-(methylamino)ethyl)acetamide (1.0 mg, 14%). LC-MS Method 1 tR=1.55, min, m/z=548, 550.

1. customevaporated to dryness
2. customThe residue was purified by preparative HPLC