Реакция #1941

Уравнение реакции

4-chloro-5-fluoro-2-(4-fluorobenzyl)-pyrimidine

4-Chloro-5-fluoro-2-(4-fluorobenzyl)-pyrimidine

4-methylpiperazine

→

title compound

Выход 96.9%

5-Fluoro-2-(4-fluorobenzyl)-4-(4-methylpiperazin-1-yl)-pyrimidine

Выход 96.9%

Растворители

methylene chloride

Условия реакции

Обработка

1. 1
   КонцентрированиеThe reaction mixture was concentrated in vacuo
2. 2
   workup.DISSOLUTIONthe residue was dissolved in methylene chloride
3. 3
   ПромывкаThe resultant solution was washed with 4 X 30 mL of water
4. 4
   Сушкаdried over anhydrous magnesium sulfate
5. 5
   Фильтрацияfiltered
6. 6
   Концентрированиеconcentrated in vacuo

Методика

A mixture of 0.48 g (2 mmol) of 4-chloro-5-fluoro-2-(4-fluorobenzyl)-pyrimidine from Step 2 and 1.53 mL (14 mmol) of 4-methylpiperazine in 10 mL of methylene chloride was stirred at ambient temperature for 1.5 hours. The reaction mixture was concentrated in vacuo and the residue was dissolved in methylene chloride. The resultant solution was washed with 4 X 30 mL of water, dried over anhydrous magnesium sulfate, filtered and concentrated in vacuo to give 0.59 g (95% yield) of the title compound as an oil; 1H NMR (CDCl3) d 2.32 (s, 3H), 2.47 (t, 4H), 3.78 (t, 4H), 3.99 (s, 2H), 6.97 (m, 2H), 7.29 (m, 2H), 7.97 (d, 1H). The product was carried on to the next step without purification.

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