Edotecarin, ED-749, J-107088

12-(β-D-葡萄吡喃基)-2,10-二羟基-6-[2-羟基-1-(羟甲基)乙基氨基]-6,7,12,13-四氢-5H-吲哚[2,3-a]吡咯罗[3,4-c]卡巴唑-5,7-二酮Chemical Name: 12-(beta-D-Glucopyranosyl)-2,10-dihydroxy-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione
CAS No. 174402-32-5
项目整合开发状态: Phase III
项目研究机构: Banyu (Originator), Merck & Co. (Originator), Pfizer (Licensee)
合成路线:The condensation of 6-(benzyloxy)indolylmagnesium bromide (I) with dihalomaleimide (II) afforded the diindolylmaleimide (III),which was oxidatively cyclized to produce indolocarbazole (IV).Glycosylation of (IV) with 1-chloro-tetrabenzylglucose (V) yielded the glycosyl derivative (VI).Subsequent deprotection of the benzyl ethers of (VI) by hydrogenolysis over Pd/C gave (VII).Conversion of the imide function of (VII) to anhydride (VIII) was then effected by treatment with KOH.Finally,coupling of (VIII) with hydrazine (IX) in DMF at 80 C yielded the title compound.