225112-10-7Relevant articles and documents
Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors
Mane,Li,Huang,Gupta,Nadkarni,Giridhar,Naik,Yadav
, p. 6296 - 6304 (2012/11/13)
Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido[1,2-a]pyrimidin-4-ones were synthesized and evaluat
Methyl (Z)-2-[(benzyloxycarbonyl)amino]-3-dimethyl-aminopropenoate in the synthesis of heterocyclic systems. Synthesis of (benzyloxycarbonyl)amino substituted fused pyrimidinones
Toplak, Renata,Svete, Jurij,Golic Grdadolnik, Simona,Stanovnik, Branko
, p. 177 - 189 (2007/10/03)
Methyl (Z)-2-[(benzyloxycarbonyl)amino]-3-dimethylaminopropenoate (1) was used as a reagent for preparation of 3-[(benzyloxycarbonyl)amino] substituted 4H-pyrido[1,2-a]pyrimidin-4-ones 17-21, 4H-pyrimido[1,2-b]pyridazin-4-ones 22 and 23, 5H-[1,2,4]triazolo[2,3-a]-pyrimidin-5-one 24, 5H-thiazolo[3,2-a]pyrimidin-5-one 25, and 4H-pyrazino[1,2-a]pyrimidin-4-one 26. Removal of the benzyloxycarbonyl group by catalytical transfer hydrogenation with Pd/C in the presence of cyclohexene is selective to give 3-amino-4H-pyrido[1,2-a]-pyrimidin-4-ones 27-30 in 85-92% yields, or with hydrogen bromide in acetic acid to give 3-amino-4H-pyrimido[1,2-b]pyridazin-4-one (31) and 6-amino-5H-thiazolo[3,2-a]pyrimidin-5-one (32) in 80% yields.