应用德法两国的专利方法制造尼可剎米(二乙烟醯胺)

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尼可刹米(Nikethamide)为常用的强心兴奋剂,已为中国药典所收载,其合成方法虽多,但以德、法两国专利所载的制造方法较为合理,产量亦较高,兹将其译出,以供参考。德国专利方法~(1),取经80℃干燥过的烟酸克分子,置于三口圆底烧瓶内,加入二氯亚砜(Thionyl chloride)约3克分子,中间装以搅拌器,其它一口装冷凝管,管上接连氯化钙干燥管以防湿气的侵入,在另一口上装分液漏斗。在水浴中回流8-10小时后,将冷凝管横放,改为蒸溜用的冷却器,在减压下溜去多余的二氯亚砜, Nikethamide, a commonly used cardiac stimulant, has been accepted by the Chinese Pharmacopoeia. Although its synthesis methods are numerous, the manufacturing methods contained in the patents of Germany and France are more reasonable and the yields are also higher. It will be translated for reference. German patent method ~ (1), take the nicotinic acid molecules dried at 80 ℃, placed in a three-necked round-bottomed flask, add about 3 moles of thionyl chloride, equipped with a stirrer in the middle, the other one loaded Condenser, pipe connected to the calcium chloride drying tube to prevent the invasion of moisture, in the other mouth uploading separatory funnel. After refluxing in a water bath for 8-10 hours, the condenser tube was placed horizontally and replaced with a cooler for steaming. The excess of thionyl chloride was slipped under reduced pressure,
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