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KMID : 0043319840070020133
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Archives of Pharmacal Research
1984 Volume.7 No. 2 p.133 ~ p.136
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Synthesis of Higenamine, A Cardiotonic Principle of Aconite Root
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Chang KC
Yun HS/Lim JK/Park CW
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Abstract
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Higenamine (I), a cardiotonic principle of Aconite root, was synthesized from 4-methoxy-phenylacetic acid (II) and p-(3, 4-dimethoxyphenyl)-ethylamine (IV). Condensation of IV with 4-methoxyphenylacetyl chloride (III) was followed by cyclodehydration yielding 1-(4’’-methoxybenzyl)-6,7-crimethoxy-3,4-dihydroisoquinoline (VI). Reduction of VI to 1, 2. 3, 4-tetrahydroisoquinoline (VII) and subsequent demethylation provided desired product higenamine, 1-(4’’-hydroxybenzyl)-6,7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline.
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