Реакция #10356

Уравнение реакции

Benzylsulfamic acid [6-chloro-5-(2-methoxy-phenoxy)-2-methylsulfanyl-pyrimidin-4-yl]-amide

citric acid

→

benzylsulfamic acid [6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-methylsulfanyl-pyrimidin-4-yl]-amide

Растворители

ethylene glycol

Условия реакции

Обработка

1. 1
   workup.ADDITIONThe reaction mixture was poured onto water (120 ml)
2. 2
   Температураcooled to 0° C
3. 3
   ФильтрацияThe precipitate was filtered off
4. 4
   Промывкаwashed with water
5. 5
   Другоеdried at HV

Методика

Benzylsulfamic acid [6-chloro-5-(2-methoxy-phenoxy)-2-methylsulfanyl-pyrimidin-4-yl]-amide (1.75 g) was added to a solution of potassium tert.-butylate (1.87 g) in ethylene glycol (30 ml) and stirred at 100° C. for 40 h. The reaction mixture was poured onto water (120 ml), acidified with solid citric acid (1.9 g) and cooled to 0° C. The precipitate was filtered off, washed with water and dried at HV to give benzylsulfamic acid [6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-methylsulfanyl-pyrimidin-4-yl]-amide (Example 203). LC-MS: tR=4.70; [M+H]+=493.09.

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