摘要
1933年,Graf发现:如果在烟酰胺的氮原子上引入一个羟甲基,就可以获得一种对治疗胆囊炎有效的新药物——N-羟甲基烟酰胺(Ⅰ)。此后,国内外化学和药学工作者在Ⅰ的合成、检测和效能等方面做了许多研究工作,取得了一些研究成果,但仍存在不少问题。 我们对Ⅰ的合成方法进行了研究。
N-Hydroxymethyl-nicoyinamide, an antimicrobic agent was prepared in good yieldby treating nicotinamide with excess of formaldehyde in the presence of potassium carbonate. The con-denaation reaction was studied under different conditions, changing the amount of formaldehyde, withdifferent kinds of bases and reaction time. The yield was 72.4% when the reaction was carried outusing 3. 0 g of nicotinamide, 5.0 ml of formaldehyde (36.8% aq. solution) and 0.03 g of potassiumcarbonate in boiling water bath for one hour. More than 5.0 ml of formaldehyde did not contribute tohigher yield. The results showed that potassium carbonate was better than other bases, and one hour ofreaction time was enough.
出处
《药学学报》
CAS
CSCD
北大核心
1992年第8期629-631,共3页
Acta Pharmaceutica Sinica
