NSC-638850, KW-2401, UCN-01

Chemical Name: (8alpha,9beta,10beta,12alpha)-(+)-2,3,9,10,11,12-Hexahydro-3-hydroxy-9-methoxy-8-methyl-10-(methylamino)-8,12-epoxy-1H,8H,2,7b,12a-trizadibenzo[a,g]cyclonona[cde]trinden-1-one
项目整合开发状态: Phase I/II
项目研究机构: Kyowa Hakko (Originator), National Cancer Institute (Licensee)
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.