【药物名称】
化学结构式(Chemical Structure):
参考文献No.574789
标题:AMP deaminase inhibitors. 4. Further N3-substituted coformycin aglycon analogues: N3-alkylmalonates as ribose 5'-monophosphate mimetics
作者:Bookser, B.C.; Kasibhatla, S.R.; Erion, M.D.
来源:J Med Chem 2000,43(8),1519
合成路线图解说明:

Dibenzyl malonate (I) was alkylated with 3-(trifluoromethyl)benzyl bromide (II) in the presence of Na in DMF to yield the 3-(trifluoromethyl)benzylmalonate (III). Further alkylation of (III) with 1,4-dibromobutane (IV) provided the bromobutyl derivative (V). Condensation of the known 6,7-dihydroimidazo[4,5-d][1,3]diazepin-8-one (VI) with bromide (V) in the presence of NaH and NaI furnished adduct (VII). The keto group of (VII) was then reduced to alcohol (VIII) employing NaBH4 in MeOH-CH2Cl2. Finally, hydrogenolysis of the benzyl ester groups of (VIII) in the presence of Pd/C and Et3N afforded the title dicarboxylate triethylammonium salt.

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