Synthesis 2016; 48(07): 1029-1045
DOI: 10.1055/s-0035-1561287
paper
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Fluorescent 2-Substituted 6-(Het)aryl-7-deazapurine Bases {4-(Het)aryl-pyrrolo[2,3-d]pyrimidines} by Aqueous Suzuki–Miyaura Cross-Coupling Reactions

Nazarii Sabat
a   Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences & IOCB Research Center, Flemingovo nam. 2, 16610 Prague 6, Czech Republic
b   Department of Organic Chemistry, Faculty of Science, Charles University in Prague, Hlavova 8, 12843 Prague 2, Czech Republic   Email: hocek@uochb.cas.cz
,
Petr Nauš
a   Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences & IOCB Research Center, Flemingovo nam. 2, 16610 Prague 6, Czech Republic
,
Ján Matyašovský
a   Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences & IOCB Research Center, Flemingovo nam. 2, 16610 Prague 6, Czech Republic
,
Dmytro Dziuba
a   Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences & IOCB Research Center, Flemingovo nam. 2, 16610 Prague 6, Czech Republic
,
Lenka Poštová Slavětínská
a   Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences & IOCB Research Center, Flemingovo nam. 2, 16610 Prague 6, Czech Republic
,
Michal Hocek*
a   Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences & IOCB Research Center, Flemingovo nam. 2, 16610 Prague 6, Czech Republic
b   Department of Organic Chemistry, Faculty of Science, Charles University in Prague, Hlavova 8, 12843 Prague 2, Czech Republic   Email: hocek@uochb.cas.cz
› Author Affiliations
Further Information

Publication History

Received: 16 November 2015

Accepted after revision: 20 November 2015

Publication Date:
11 January 2016 (online)


Abstract

A series of 4-(het)aryl-pyrrolo[2,3-d]pyrimidines [6-(het)aryl-7-deazapurine bases] bearing a H, NH2, CH3, F, or Cl group at the 2-position and either H or F at the 5-position (position 7 of 7-deazapurine) were prepared in a single step by the aqueous Suzuki–­Miyaura cross-coupling reactions of the corresponding 6-chloro-7-deazapurines with (het)arylboronic acids. Unlike their ribonucleoside derivatives, which are potent cytostatics, the deazapurine bases did not show significant biological activity but most of them exerted bright fluorescence with emission maxima 368–468 nm and high quantum yields up to 0.83.

Supporting Information