反应详情

To a solution of 2-aminonicotinic acid (3245 mg, 23.49 mmol) in N,N-dimethylformamide (200 mL) were added C-(5-phenoxy-thiophen-2-yl)methylamine (5305 mg, 25.84 mmol) described in Preparation Example 24, benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (12.49 g, 28.19 mmol) and triethylamine (7.86 mL, 56.38 mmol), and the solution was stirred for 2 days at room temperature. Water was added to the reaction mixture, which was then extracted with ethyl acetate, the organic layer was sequentially washed with an aqueous solution of saturated sodium bicarbonate, water, then brine, the solvent was evaporated in vacuo, and 2-amino-N-(5-phenoxy-thiophen-2-ylmethyl)-nicotinamide (4999 mg, 15.36 mmol, 65%) was obtained as crude product.

1. extractionwas then extracted with ethyl acetate
2. washthe organic layer was sequentially washed with an aqueous solution of saturated sodium bicarbonate, water
3. custombrine, the solvent was evaporated in vacuo