论文部分内容阅读
萘呋胺酯草酸盐是国外正在临床使用的一种新药,法国、西德等国均有产品。它具有改善中枢和周围血液循环,增加血液中氧分压,促进中枢和周围组织器官能量代谢及营养等作用。因而被用于由于中枢和周围组织器官血液供应不足而引起的功能减退、老年性耳聋、视力衰退、足下垂和行为障碍等病症。鉴于对这些病症的治疗,目前尚无其他较好的药物,以及在国内对于萘呋胺酯草酸盐尚未见有生产,我们进行了该药物的合成研制。我们采用了价格便宜、国内易得的丙二酸二乙酯等原料和试剂,经分次烷基化、水解脱羧、酯化和成盐五步反应,获得成功,产品分析合格。合成路线如下:
Naphthylamine fumarate oxalate is a new drug that is being used clinically abroad, with products from France, West Germany and other countries. It has to improve the central and peripheral blood circulation, increase blood oxygen partial pressure, and promote central and surrounding tissue and organ energy metabolism and nutrition role. Thus being used for conditions such as hypofunction, senile deafness, vision loss, ptosis and behavioral disorders due to insufficient blood supply to the central and surrounding tissues and organs. In view of the treatment of these conditions, there is no other better drugs, as well as the domestic production of naproxen oxalate has not yet seen, we conducted the synthesis of the drug. We have adopted the cheap, domestic easy to get raw materials and reagents such as diethyl malonate, after sub-alkylation, hydrolysis decarboxylation, esterification and salt into the five-step reaction, the success of product analysis qualified. The synthetic route is as follows: