528597-08-2Relevant articles and documents
Synthesis of 7-Aza-5,8,10-trideazafolic acid and its 4-amino-derivative as potential antifolates
Wollein, Guenther,Troschuetz, Reinhard
, p. 1195 - 1200 (2007/10/03)
o-Aminoamide 8, an intermediate in our multistep synthesis of the title compounds was prepared from 1,3-diketone 3. The following condensation of 8 with chloroformamidine-HCl (9) gave pyrido[3,4-d]pyrimidine 10. Dehydratisation of amide 8 led to o-aminonitrile 15, which was cyclocondensated with guanidine (16) to yield pyrido[3,4-d]pyrimidine-2,4-diamine 17. Coupling of the acids 11 and 18 with diethyl L-glutamate (12) and following saponification provided 7-aza-5,8,10-trideazafolic acid 14 and its 4-amino-derivative 20.