反应详情

tert-Butyl [7-(aminomethyl)-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate (120 mg, 0.276 mmol, cf. Example 38) was dissolved in dichloromethane (5 mL). 4-Dimethylaminopyridine (35 mg, 0.289 mmol) was added. After stirring at room temperature for 5 min propane-1-sulfonyl chloride (39 mg, 0.031 mmol) was added and stirring was continued over night. The reaction mixture was diluted with dichloromethane and washed successively with 0.5 N hydrochloric acid (2×2 mL) and saturated NaHCO3 (1×2 mL). The organic phase was dried (MgSO4) and concentrated in vacuo. The crude product was used for the next step without further purification. Yield: 125 mg (0.231 mmol, 84%).

1. additionwas added
2. waitwas continued over night
3. washwashed successively with 0.5 N hydrochloric acid (2×2 mL) and saturated NaHCO3 (1×2 mL)
4. dry with materialThe organic phase was dried (MgSO4)
5. concentrationconcentrated in vacuo
6. customThe crude product was used for the next step without further purification