反应详情

To a solution of 5-aminomethyl-2-{[bis-(3-methyl-pyridin-2-ylmethyl)-amino]-methyl}-benzoic acid methyl ester (0.382 g, 0.944 mmol) and Et3N (0.191 g, 1.89 mmol) in dry THF (20 mL) was added MsCl (0.162 g, 1.42 mmol) at room temperature. After the addition the mixture was stirred at room temperature for 2 h saturated aqueous NaHCO3 (20 mL) was added. THF was then removed, and the aqueous residue was extracted with CH2Cl2 (3×20 mL). The extracts were combined and dried over MgSO4. After filtration the solvent was removed to afford 2-{[bis-(3-methyl-pyridin-2-ylmethyl)-amino]-methyl}-5-(methanesulfonylamino-methyl)-benzoic acid methyl ester as a pale yellow foam (0.460, 100%).

1. additionAfter the addition the mixture
2. additionwas added
3. customTHF was then removed
4. extractionthe aqueous residue was extracted with CH2Cl2 (3×20 mL)
5. dry with materialdried over MgSO4
6. filtrationAfter filtration the solvent
7. customwas removed