Dechloromethylation of the berberine to berberrubine — tricks to obtain pure product

Abstract

Berberine (1), as a compound with interesting biological activities, can be modified at various positions to obtain more potent substances. Modifications at position 9 are based on demethylation with simultaneous dechloration resulting in berberrubine. The most frequent process is thermal dechloromethylation and this work describes this method with detailed tricks to obtain almost pure product in high yield.