Synthesis of tert-Butyl 6-Formyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxylate
The intermediate 1-(2-aminoethyl)pyrrole(A)was synthesized from pyrrole and 2-chloroethylamine hydrochloride in acetonitrile under the catalysis of tetrabutyl ammonium bisulfate.Intermediate A was subjected to the Pictet-Spengler reaction to obtain intermediate l,2,3,4-tetrahydropyrrole[1,2-a]pyrazine(B),Intermediate B was then used to synthesize intermediate 3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxylic acid tert-butyl ester(C)via N-Boc protection.The final product 6-formyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxylic acid tert-butyl ester was yielded from intermediate C by the Vilsmeier-Haack reaction,with a purity of 99.7％(HPLC)and a yield of 79.0％.The elemental analysis of the product was basically consistent with that of the standard sample,and the product's structure was confirmed by nuclear magnetic resonance(NMR)spectroscopy.
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