| 摘要 |
PURPOSE:To provide the new compound useful as a selective low antagonistic agent against 5HT in a 5-HT3 receptor and especially useful for the therapy of emesis and nausea induced by the therapy of cancers. CONSTITUTION:The compound of the formula I [A is group of formula II, III or IV (R1 is H, 1-10C alkyl, arylalkyl, etc.; R3, R4, R5 are H, amino, halogen, etc.,); X is 0, NH; R is 1-4C alkyl; Y is NR, O, S], e.g. 1H-indole-3-carboxylic acid (endo-9-methyl-3-thia-9-azabicyclo[3,3.1]nona-7-yl) ester. The compound of formula I is obtained by reacting an aromatic carboxylic acid of formula: A-COOH with 3,9-diaza-3-oxa-9-aza- or 3-thia-9-aza-bicyclo[3,3,1]nonane derivative in the presence of a base (e.g. potassium carbonate) in an inert solvent (e.g. dimethylformamide) at -20 deg.C to the boiling point of the solvent. |
