反应详情

Methyl 2(S)-[N-(2-methylaminoethyl)-N-methylaminocarbonyloxy]- 3-phenylpropionate (8.0 g) was dissolved in methylene chloride (40 ml), and triethylamine (4.13 g) was added thereto under cooling. Thereto was dropwise added morpholinocarbonyl chloride (4.07 g) at 0°-10° C. over 30 minutes. After the dropwise addition, the mixture was stirred at said temperature for 60 minutes, washed with 5% hydrochloric acid, water, an aqueous solution of 6% sodium hydrogencarbonate, and water in this order, and the solvent was evaporated under reduced pressure to give 9.83 g of methyl 2(S)-[N-methyl-N-[2-{N-(morpholinocarbonyl)-N-methylamino}ethyl]aminocarbonyloxy]-3-phenylpropionate (yield 88.8%).

1. temperatureunder cooling
2. customat 0°-10° C.
3. customover 30 minutes
4. additionAfter the dropwise addition
5. customfor 60 minutes
6. washwashed with 5% hydrochloric acid, water
7. customan aqueous solution of 6% sodium hydrogencarbonate, and water in this order, and the solvent was evaporated under reduced pressure