合成路线1

The title compound has been prepared by solid-phase combinatorial synthesis. The protected diaminopropionic acid (I) is attached to 2-chlorotrityl resin, producing the resin-bound amino acid (II). The N-Fmoc group of (II) is then selectively removed by treatment with piperidine in DMF producing (III). Condensation of amine (III) with N-ethoxycarbonyl-2-methyl-3-piperidinothioacrylamide (IV) results in the thiouracil derivative (V). This is converted into the thiocyanate (VI) upon treatment with cyanogen bromide in the presence of diisopropylethylamine. Further displacement of the thiocyanate group of (VI) with N-(2-benzimidazolyl)-1,3-propanediamine (VII) leads to the aminopyrimidone resin (VIII). Finally, acidic cleavage from the solid support (VIII) gives rise to the desired compound.