哌吡(艹卓)酮(Pirenzepine,Ⅵ),化学名:5,6-二氢-6-氧代-11-(4-甲基-1-哌嗪基)乙酰基吡啶并〔2,3-b〕〔1,4〕苯并二氮杂(艹卓),为抗胆碱药,对胃粘膜毒蕈碱受体具有高度选择性拮抗作用,其减少胃酸的作用似阿托品,但无一般抗胆碱药常有的口干、心率增快、瞳孔扩大、排尿困难等不良反应。本品的出现对胃溃疡、十二指肠溃疡以及胃炎的药物治疗,又有了新的进展。我们采用2-氯-3-氨基吡啶经五步反应制得哌吡(艹卓)酮二盐酸盐,总收率32％左右。 Pirenzepine (Ⅵ), chemical name: 5,6-dihydro-6-oxo-11- (4-methyl-1-piperazinyl) acetylpyrido [2,3 -b] [1,4] benzodiazepine (艹 Zhuo) for the anticholinergics, a highly selective antagonism of gastric mucosal muscarinic receptors, which reduce the role of gastric acid like atropine, but no common anticholinergic often Dry mouth, faster heart rate, dilated pupils, dysuria and other adverse reactions. The emergence of this product on gastric ulcer, duodenal ulcer and gastritis drug treatment, there has been new progress. We use 2-chloro-3-aminopyridine in five steps to produce piperapyrine dihydrochloride, the total yield of about 32%.