Реакция #1435742

Уравнение реакции

sodium borohydride

2-(3,5-bis-trifluoromethyl-phenyl)-N-[4-(2-formyl-phenyl)-6-(4-methyl-piperazin-1-yl)-pyridin-3-yl]-N-methyl-isobutyramide

→

title compound

Выход 68.2%

2-(3,5-Bis-trifluoromethyl-phenyl)-N-[4-(2-hydroxymethyl-phenyl)-6-(4-methyl-piperazin-1-yl)-pyridin-3-yl]-N-methyl-isobutyramide

Выход 68.2%

Растворители

brine

methanol

Условия реакции

Обработка

1. 1
   workup.ADDITIONwere added at 0° C
2. 2
   workup.ADDITIONwas added at 0° C
3. 3
   workup.DISTILLATIONMethanol was distilled off
4. 4
   workup.ADDITIONthe residue was diluted with 20 ml ethyl acetate
5. 5
   Промывкаwashed with 20 ml brine
6. 6
   СушкаThe organic layer was dried over sodium sulfate
7. 7
   Концентрированиеconcentrated
8. 8
   Другоеpurified by flash chromatography

Методика

To a mixture of 15 mg (0.41 mmol) sodium borohydride in 2 ml methanol were added at 0° C. 200 mg (0.338 mmol) 2-(3,5-bis-trifluoromethyl-phenyl)-N-[4-(2-formyl-phenyl)-6-(4-methyl-piperazin-1-yl)-pyridin-3-yl]-N-methyl-isobutyramide. After stirring at 0° C. for 1 h 1 ml brine was added at 0° C. The mixture was stirred for 30 min. Methanol was distilled off and the residue was diluted with 20 ml ethyl acetate and washed with 20 ml brine. The organic layer was dried over sodium sulfate, concentrated and purified by flash chromatography to give 137 mg (68%) of the title compound as a light brown solid.

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