The reaction of staurosporine (I) with benzyl chloroformate (II) by means of NaHCO3 in acetone gives the N-protected compound (II), which is oxidized with lead tetraacetate in HOAc to yield the hydroxy compound (III). Finally, this compound is deprotected by hydrogenation with H2 over Pd/C in DMF to obtain the target hydroxy staurosporine.

The known antibiotic staurosporine (I) was protected as the N-benzyloxycarbonyl derivative (II) by treatment with benzyl chloroformate in the presence of NaHCO3. Subsequent alkylation of (II) at the 2-N atom by treatment with iodomethane and NaH in DMF provided the N-methyl derivative (III). Finally, deprotection of the benzyloxycarbonyl group of (III) by hydrogenation over Pd/C furnished the title compound.