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. 2017 Aug 14;60(17):7555–7568. doi: 10.1021/acs.jmedchem.7b00950

Scheme 1. Synthesis of 1,3-Disubstituted-1H,3H-pyrido[2,1-f]purine-2,4-dione Derivatives.

Scheme 1

(a) ethyl cyanoacetate, NaOEt, EtOH, reflux, overnight; (b) (i) NBS, CH3CN, 80 °C, 1 h, (ii) 4-methoxypyridine, 80 °C, overnight; (c) R1-Br, DBU, CH3CN, 80 °C, overnight; (d) 20% Pd(OH)2, ammonium formate, EtOH, reflux, overnight; (e) R2-Br, K2CO3, DMF, 40 °C, overnight.