| 摘要 |
<p>NEW MATERIAL:A 4-sulfonylmethylindole derivative expressed by formula I (R<1> is lower alkyl or aryl; R<2> is H or a protecting group of the amino group). EXAMPLE:4-Benzenesulfonylmethyl-1-(p-toluenesulfonyl)indole. USE:Useful as a synthetic intermediate for indole based physiologically active compounds, e.g. 4-substituted indole based medicines, etc., and capable of synthesizing 4-substituted indoles by introducing a desired electrophilic reagent into the compound expressed by formula I and subjecting the resultant compound to reduction or substitution reaction and desulfurizing the resultant product. PREPARATION:4-Oxo-4,5,6,7-tetrahydroindole expressed by formula II is condensed with a methyl sulfone expressed by formula III in the presence of a base, e.g. methyllithium, etc., to give a 4-hydroxy-4,5,6,7-tetrahydroindole expressed by formula IV as a reaction product thereof. The resultant 4- hydroxy-4,5,6,7-tetrahydroindole expressed by formula IV is then dehydrated and dehydrogenated to afford the aimed compound expressed by formula I.</p> |
