NEW ACONITINE-BASED COMPOUND AND ANALGESIC ANTIPHLOGISTIC MEDICINE

摘要

PROBLEM TO BE SOLVED: To obtain a new aconitine-based compound having a strong analgesic antiphlogistic activity, having lower toxicity than those of mesaconitine, aconitine, etc., and useful as an analgesic antiphlogistic medicine.;SOLUTION: An aconitine-based compound of the formula (R is m- chlorobenzoyl, veratroyl or the like; R2 is methyl or ethyl; R3 and R4 are each H or hydroxyl group; R5 is hydroxyl group; R6 is hydroxyl or forms a carbonyl group together with the 15-C carbon atom), for example, 14-O-veratroyl aconine. The 14-O-veratroyl aconine has physical properties such as colorless amorphous powder; soluble in ether, chloroform, benzene, ethanol, etc.; insoluble in water. The compound of formula can be obtained, for example, by subjecting a known aconitine type alkaloid such as aconitine, mesaconitine or hypaconitine as a starting raw material to an oxygen-removing reaction at the 3, 8, 13 or 15-position, or replacing substituents at the N atom and 14-position by various substituents.;COPYRIGHT: (C)2000,JPO