反应详情

(R)-5-(4-(((R)-3—Oxo-1-(4-methylbenzenesulfonyl)-1,2,3,4-tetrahydropyrazin-2-yl)-methyl)-1H-1,2,3-triazol-1-yl)-5,6,7,8-tetrahydronaphthalene-2-carbaldehyde (1.1 mmol, 1 eq) was dissolved in DCE and treated with 4 Å powdered molecular sieves. To the solution was added t-butyl amine (3.2 mmol, 3.0 eq) and AcOH (3.2 mmol, 3.0 eq). The reaction stirred at RT overnight. NaBH(OAc)3 (3.3 mmol, 3.0 eq) was added and after 3 h, the solvent was removed and the residue was purified by SiO2 to afford amine the title compound (MS (m/z): 549.3 (m+H)).

1. additiontreated with 4 Å
2. customthe solvent was removed
3. customthe residue was purified by SiO2