Microbial hydroxylation and simultaneous formation of the 4 ''-O-methylglucoside of the tyrosine-kinase inhibitor CGP 62706

Two fungal strains of Beauveria bassiana, DSM 875 and DSM 1344, hydroxylate d CGP 62706, an inhibitor of the EGF-receptor tyrosine kinase, in the C(4') position and subsequently formed the glucosylated metabolite with 5-11% an d 7-15% yield, respectively. The reaction could be successfully scaled up t o 31 fermentation volume with strain DSM 875. The structure of the glycosyl ated compound was determined by micro-H PLC-MS and NMR after production by fermentation on the mg scale. In addition, the biotransformation also provi des access to the free 4'-hydroxylated compound, as the glycoside can easil y be hydrolyzed.