反应详情

3,4-Difluoro-2-methylbenzyl-2,2-dimethoxyethylamine (41, 37.8 g) was dissolved in dichloromethane (100 mL). Pyridine (42 mL) was added. At 0° C. a solution of p-toluenesulphonyl chloride (36.8 g, 193 mmol) in dichloromethane was added dropwise. The reaction was allowed to warm to room temperature and stirring continued until conversion was complete. For workup, the reaction mixture was diluted with dichloromethane (100 mL) and extracted twice with 1.5M hydrochloric acid, twice with sodium bicarbonate solution and once with brine. The organic layer was dried over magnesium sulphate, evaporated to dryness to give crude product as an orange oil (68.3 g). This was used without further purification.

1. extractionextracted twice with 1.5M hydrochloric acid, twice with sodium bicarbonate solution and once with brine
2. dry with materialThe organic layer was dried over magnesium sulphate
3. customevaporated to dryness