反应详情

A 5 mL CH2Cl2 solution of 7-(3-piperidin-1-yl-propoxy)-1,2,3,4-tetrahydro-isoquinoline dihydrochloride (175 mg, 0.5 mmol) and NEt3 (0.25 mL, 1.7 mmol) is stirred under N2, a 1 mL CH2Cl2 solution of acetyl chloride (0.043 mL, 0.6 mmol) is added, and reaction is stirred at room temp. for 5-6 hours. Reaction mixture is quenched with MeOH, concentrated and the residue is purified by chromatography (SCX-MeOH wash, elute 2M NH3/MeOH; then (SiO2; 0-10% MeOH/CH2Cl2/1% NH4OH gradient) to give the product (90 mg, 58% yld). MS(ES+)317.1(M+H)+

1. customreaction
2. customReaction mixture
3. customis quenched with MeOH
4. concentrationconcentrated
5. customthe residue is purified by chromatography (SCX-MeOH
6. washwash
7. washelute 2M NH3/MeOH
8. customthen (SiO2; 0-10% MeOH/CH2Cl2/1% NH4OH gradient) to give the product (90 mg, 58% yld)