Реакция #8703

Уравнение реакции

4-[4,6-dichloro-5-(3-methoxy-phenoxy)-pyrimidin-2-yl]-morpholine

2-phenyl-ethanesulfonic acid amide potassium salt

→

2-phenyl-ethanesulfonic acid [6-chloro-5-(3-methoxy-phenoxy)-2-morpholin-4-yl-pyrimidin-4-yl]-amide

Выход 90.3%

Растворители

water

DMSO

Условия реакции

Обработка

1. 1
   Экстракцияextracted twice with diethyl ether (75 ml) before it
2. 2
   ЭкстракцияThe mixture was extracted twice with EA (150 ml)
3. 3
   ПромывкаThe organic phase was washed with water (50 ml)
4. 4
   ДругоеThe product precipitated upon evaporation of the solvent
5. 5
   ДругоеThe solid was collected
6. 6
   Промывкаwashed with diethyl ether
7. 7
   Другоеdried

Методика

A solution of 4-[4,6-dichloro-5-(3-methoxy-phenoxy)-pyrimidin-2-yl]-morpholine (1.0 g) and 2-phenyl-ethanesulfonic acid amide potassium salt (1.57 g, Referential Example 1e) in DMSO (15 ml) was stirred at 60° C. for 24 h. The solution was diluted with water (75 ml) and extracted twice with diethyl ether (75 ml) before it was acidified with 10% aq. citric acid. The mixture was extracted twice with EA (150 ml). The organic phase was washed with water (50 ml). The product precipitated upon evaporation of the solvent. The solid was collected, washed with diethyl ether and dried to give 2-phenyl-ethanesulfonic acid [6-chloro-5-(3-methoxy-phenoxy)-2-morpholin-4-yl-pyrimidin-4-yl]-amide (1.28 g) as off-white powder. LC-MS: tR=5.34 min, [M+1]+=505.12, [M−1]−=502.97.

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