盐酸噻氯匹啶的合成

来源 :浙江大学学报(医学版) | 被引量 : 0次 | 上传用户:nvllnvll
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
目的 :合成噻氯匹啶 ,并对合成工艺作了适当改进。方法 :以噻吩甲醛为原料 ,用 Darzen反应、水解、脱羧 ,与盐酸羟胺反应制得噻吩乙醛肟 ,继而经 Raney Ni氢化还原制得噻吩乙胺 ,再经亚胺化、环合制得主环 4,5 ,6,7-四氢噻吩并 [3 ,2 -c]吡啶 ,再与邻氯氯苄缩合后成盐制得盐酸噻氯匹啶。结果 :利用上述合成方法 ,成功地制得目标化合物 ,总收率达 43 %。结论 :该方法总收率略低于文献[2 ] ,但简化了一些反应条件 ,使原料易得 ,操作简单。 Objective: To synthesize ticlopidine and to improve the synthesis process. Methods: Thiophene-formaldehyde as raw material, with Darzen reaction, hydrolysis, decarboxylation, and hydroxylamine hydrochloride reaction thiophene acetaldehyde oxime, followed by Raney Ni hydrogenation reduction of thiophene ethylamine, and then by imidization, the main ring system 4,5,6,7-tetrahydrothieno [3,2-c] pyridine, and then with the o-chlorobenzyl chloride condensation into salt ticlopidine hydrochloride. Results: The target compound was successfully obtained by the above synthesis method with an overall yield of 43%. Conclusion: The overall yield of this method is slightly lower than that of the literature [2], but some reaction conditions are simplified, making the raw materials easy to obtain and easy to operate.
其他文献