反应详情

N-[2-({1-[1-(4-Chlorophenyl)cyclobutyl]-3,4-dihydroisoquinolin-6-yl}oxy)ethyl]propane-1-sulfonamide (320 mg, 0.62 mmol) was dissolved in methanol (5 mL) and water (0.1 mL) and sodiumborohydride (47 mg, 1.25 mmol) was added at 4° C. in small portions. The reaction mixture was allowed to warm to room temperature and stirring was continued over night. The solvent was evaporated in vacuo, the residue was treated with dichloromethane and water. The aqueous layer was extracted several times with dichloromethane. The combined organic layers were dried (Na2SO4) and concentrated in vacuo. The crude product was purified by preparative HPLC (RP, acetonitrile, water). The purified amine was then converted into the corresponding hydrochloric acid salt by adding 5M isoporpanolic hydrochloric acid followed by concentration in vacuo. Yield: 35 mg (0.07 mmol, 11%, colorless solid).

1. waitwas continued over night
2. customThe solvent was evaporated in vacuo
3. additionthe residue was treated with dichloromethane and water
4. extractionThe aqueous layer was extracted several times with dichloromethane
5. dry with materialThe combined organic layers were dried (Na2SO4)
6. concentrationconcentrated in vacuo
7. customThe crude product was purified by preparative HPLC (RP, acetonitrile, water)
8. additionby adding 5M isoporpanolic hydrochloric acid
9. concentrationfollowed by concentration in vacuo