Ammonia → Mirtazapine

반응식

[CH3:1][N:2]1[CH2:7][CH:6]([C:8]2[CH:13]=[CH:12][CH:11]=[CH:10][CH:9]=2)[N:5]([C:14]2[N:19]=[CH:18][CH:17]=[CH:16][C:15]=2[CH2:20]O)[CH2:4][CH2:3]1.S(=O)(=O)(O)O.N.[OH-].[Na+]>>[CH3:1][N:2]1[CH2:7][CH:6]2[N:5]([C:14]3[N:19]=[CH:18][CH:17]=[CH:16][C:15]=3[CH2:20][C:9]3[CH:10]=[CH:11][CH:12]=[CH:13][C:8]=32)[CH2:4][CH2:3]1

참가 물질

반응물 4

HCID 222Ammonia

HCID 1118Sulfuric Acid

HCID 14798Sodium Hydroxide

HCID 102214352-(4-Methyl-2-phenyl-1-piperazinyl)-3-pyridinemethanol

생성물 1

HCID 4205Mirtazapine수율 95%

실험 절차

1-(3-Hydroxymethylpyridyl-2)-4-methyl-2-phenyl-piperazine (1.8 g) is added to ˜5 mL of concentrated sulfuric acid. The resulting solution is mixed at 350° C. for 6 hours. After cooling, the reaction mixture is added to 25 g of ice under mixing and basified with a concentrated ammonia solution or sodium hydroxide solution to pH=10. The separated precipitate is extracted into methylene chloride and the extract is evaporated to dryness; 1.6 g of Mirtazapine is obtained (yield 95%).