Cheng Z J, Yang Z P
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing.
Yao Xue Xue Bao. 1993;28(8):633-8.
Penequine hydrochloride (I) is a new potent anticholinergic drug, the degradation mechanism of I in aqueous solutions is reported in this paper. I is an ethereal compound, stable in neutral and alkaline solutions, but it decomposes in strong acidic solutions. Its main degradation products have been separated and identified by means of TLC, MS, GC/MS and GC/FTIR. With reference to the general degradation rule of ethereal compound and the structure of the degradation products, we deduced that the ether linkage of I splits in acidic solutions by the catalysis of hydrogen ion, producing 3-quinuclidinol (DP1) and 1-phenyl-1-cyclopentyl glycol. The latter turns into 1-phenyl-1-cyclopentyl acetaldehyde through dehydration and rearrangement. In addition, small amounts of other degradation compounds, e. g. benzaldehyde, acetophenone, phenylcyciopentyl ketone, etc. have also been found, but the mechanism remains to be further studied.
盐酸戊喹(I)是一种新型强效抗胆碱能药物,本文报道了I在水溶液中的降解机制。I是一种醚类化合物,在中性和碱性溶液中稳定,但在强酸性溶液中会分解。其主要降解产物已通过薄层色谱法(TLC)、质谱法(MS)、气相色谱-质谱联用法(GC/MS)和气相色谱-傅里叶变换红外光谱联用法(GC/FTIR)进行了分离和鉴定。参照醚类化合物的一般降解规律及降解产物的结构,我们推断I的醚键在酸性溶液中受氢离子催化而断裂,生成3-奎宁环醇(DP1)和1-苯基-1-环戊基二醇。后者经脱水和重排转化为1-苯基-1-环戊基乙醛。此外,还发现了少量其他降解化合物,如苯甲醛、苯乙酮、苯基环戊基酮等,但其机制仍有待进一步研究。