engleski

N-1 alkyl, 1, 2, 3-triazolyl and C-5 alkynyl cytosine, uracil an C-6 alkyl pyrrolo[2, 3-d]pyrimidine derivatives: synthesis, cytostatic and antibacterial evaluations

N-alkylated pyrimidine and pyrrolo[2, 3-d]pyrimidine derivatives have a great role in modern medicine and have shown rather marked antitumor and antiviral activities. In light of these findings we efficiently synthesized the novel N-1 substituted and C-5 alkynylated N4-benzoylcytosine and uracil derivatives by N-alkylation of pyrimidine bases and subsequent Pd-catalysed Sonogashira cross-coupling reaction. N-1 triazolyl derivatives were afforded via "click" reaction, while C-6 substituted pyrrolo[2, 3-d]pyrimidine derivatives were prepared by in situ N-heteroannulation of C-5 alkynylated derivatives.

C-6 substituted pyrrolo[2 ; 3-d]pyrimidine derivatives ; C-5 alkynylated pyrimidine derivatives ; 1 ; 2 ; 3-triazole ; Sonogashira cross-coupling reaction ;

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