新型镇静催眠药茚地普隆的合成

Synthesis of a novel sedative-hypnotic indiplon

目的改进茚地普隆的合成工艺。方法以3-氨基苯乙酮为起始原料,经3步反应制得N-[3-[(3-二甲基胺)-1-氧-2-丙烯基]-苯基-N-甲基]-乙酰胺(4);以2-乙酰噻吩为起始原料,经4步反应制得(3-氨基-1H-吡唑-4-基)-2-噻吩基甲酮(8),4和8在冰醋酸介质中加热关环得到茚地普隆。结果与结论改进了茚地普隆的合成工艺,产物结构经MS1、H-NMR以及元素分析确证,总收率为36.0%。

Aim To improve the synthetic procedure of indiplon. Methods N- [ 3- [ 3- （ dimethylamino）- 1-oxo- 2-propenyl]-phenyl]-N-methylacetamide（4） was synthesized from 3-aminoacetophenone via three steps. （3-Amino-1H-pyrazol-4-yl）-2-thienyl-methanone （8） was synthesized from 2-acetylthiophene via four steps. Indiplon（1） was obtained by the reaction between 4 and 8 in the presence of glacial acetic acid. Results and conclusion The structure of target compound was confirmed by MS, ^1H-NMR and dement analysis. The total yield was 36.0 %. The easily available and cheap starting material was used to synthesize indipolon. The purification method of the target compound was improved.