KT-6352

Chemical Name: 9,13-Epoxy-10-methoxy-2,9-dimethyl-11-(methylamino)-2,3,10,11,12,13-hexahydro-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one
CAS No. 161510-80-1
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator)
合成路线: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.

合成路线: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.