| 摘要 |
PURPOSE:To obtain the titled compound useful as an intermediate for pindolol which is a remedy for circulatory diseases, easily, by reacting a 4- oxotetrahydroindole precursor with an amination agent using a partially etherified polyhydric alcohol as the solvent, and dehydrogenating the reaction product. CONSTITUTION:4-Oxotetrahydroindole of formula IV (R5 and R6 are R1) is produced by reacting the 4-oxotetrahydroindole precursor of formula I - formula III (R1-R4 are H or hydrocarbon residue) with an amination agent (e.g. ammonium salt, organic amine, etc.) at 70-170 deg.C using a partially etherified polyhydric alcohol (e.g. ethylene glycol monobutyl ether) as the solvent. The reaction system is added with 1-30wt% dehydrogenation catalyst (preferably Pd/C) based on the compound of formula IV, and the compound is dehydrogenated at 120-250 deg.C, preferably 150-200 deg.C to obtain the objective compound of formula V.
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