| Autor: |
Brown, Nesbitt D., Leader, Haim, Phillips, Lawrence R., Smejkal, Ruthann M., Gordon, Richard K., Chiang, Peter K. |
| Zdroj: |
Journal of Pharmaceutical Sciences; June 1993, Vol. 82 Issue: 6 p563-564, 2p |
| Abstrakt: |
The preparation of 2-[N-(ethyl)-(N-β-hydroxyethyl)]aminoethyl 2,2-diphenylpropionate (1), a metabolite of aprophen [2-diethylaminoethyl 2,2-diphenylpropionate], is described. Hydrolysis of [2-(2-chloroethyl)ethylamino]ethyl acetate hydrochloride (2) in a basic solution, followed by acidic pH adjustment, gave the ethylcholineaziridinium ion (3) that upon treatment with 2,2-diphenylpropionic acid produced 1 in a 56% yield. Synthetic 1 was found to possess antimuscarinic activities, but was ~10-fold less potent than the parent compound aprophen. |
| Databáze: |
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