反应详情

DIEA (4734, 2.72 mmol) was added into a solution of 3-bromo-4-methylbenzoic acid (189 mL, 0.881 mmol), 4-(2-(pyrrolidin-1-yl)ethyl)benzenamine (140 mg, 0.734 mmol), BOP (487 mg, 1.01 mmol) in DMF. The reaction mixture was stirred at rt under argon atmosphere overnight. The reaction mixture was diluted with AcOEt, and then washed with 1N NaOH aqueous solution three times. Organic phase was dried with anhydrous Na2SO4, and then evaporated to remove organic solvents. The obtained residue was further dried under high vacuum overnight to give crude product, which was used directly for the next step synthesis without further purification. MS (ESI+) m/z 387.0 [M+H]+.

1. washwashed with 1N NaOH aqueous solution three times
2. dry with materialOrganic phase was dried with anhydrous Na2SO4
3. customevaporated
4. customto remove organic solvents
5. customThe obtained residue was further dried under high vacuum overnight
6. customto give crude product, which
7. customwas used directly for the next step synthesis without further purification