| Autor: |
Harrison, T., Owens, A. P., Williams, B. J., Swain, C. J., Williams, A., Carlson, E. J., Rycroft, W., Tattersall, F. D., Cascieri, M. A., Chicchi, G. G., Sadowski, S., Rupniak, N. M. J., Hargreaves, R. J. |
| Zdroj: |
Journal of Medicinal Chemistry; November 2001, Vol. 44 Issue: 24 p4296-4299, 4p |
| Abstrakt: |
1-(5-{[(2R,3S)-2-({(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethyl}oxy)-3-(4-fluorophenyl)morpholin-4-yl]methyl}-2H-1,2,3-triazol-4-yl)-N,N-dimethylmethanamine hydrochloride 3 is a high affinity, orally active, h-NK1 receptor antagonist with a long central duration of action and a solubility in water of >100 mg/mL. The construction of the 5-dimethylaminomethyl 1,2,3-triazol-4-yl unit, which incorporates the solubilizing group of 3, was accomplished by thermal rearrangement of a propargylic azide in the presence of dimethylamine. Compound 3 is highly effective in pre-clinical tests that are relevant to clinical efficacy in emesis and depression. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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