A one pot, two-step synthesis of 5-arylpyrrolo[2,3-d]pyrimidines and screening of their preliminary antibacterial properties

作者：Saikia Lakhinath; Roudragouda P; Thakur Ashim J^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(3): 992-998.

DOI：10.1016/j.bmcl.2015.12.047

• Pyrrolo[2,3-d]pyrimidine
• Michael type addition
• Na2S2O4
• NaOH
• Reductive cyclization

A one pot two step methodology for the synthesis of ten derivatives of 5-arylpyrrolo[2,3-d]pyrimidine has been reported. The methodology exploits the strong reducing nature of alkaline Na2S2O4 solution coupled with favorability of Michael type addition reaction in alkaline medium. The methodology demands attraction as it is non-catalytic, quite general for wide range of nitrostyrenes and possesses comprehensive advantages over most of the earlier methods in terms of reaction time as well as yield. The methodology enjoys additional advantage of utilizing cheaper and easily available chemicals as reagent for the purpose. Some of the synthesized compounds are found to possess remarkable activity against some of the tested bacterial strains.

• 出版日期2016-2-1