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6964-95-0

2-Amino-5,6,7,8-tetrahydro-3H-pyrido[2,3-d]pyrimidin-4-one synthesis

3synthesis methods
-

Yield:6964-95-0 70%

Reaction Conditions:

with sodium ethanolate in ethanol;Reflux;

Steps:

2 Step 2: 2-amino-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidin-4-one.

Step 2: 2-amino-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidin-4-one. A solution of sodium ethoxide (21 % in EtOH, 197 μ, 2.51 mmol, 2.5 equiv.) was added to the mixture of ethyl 2-ethoxy-3,4,5,6-tetrahydropyridine-3-carboxylate (200 mg, 1 mmol, 1 equiv.) and guanidine hydrochloride (96 mg, 1 mmol, 1 equiv.) in EtOH (2 mL). The reaction mixture was stirred a reflux overnight. The solvent were removed under vacuum and the obtained solid was dried to afford the desired product as a light yellow solid (116 mg, 70% yield). 1 H NMR (400 MHz, CDCI3) 59.89 (1 H, br s), 6.18 (1 H, br s), 6.10 (2H, br s), 3.10 - 3.08 (2H, m), 2.20 - 2.18 (2H, m), 1.61 - 1.59 (2H, m).

References:

WO2015/187089,2015,A1 Location in patent:Page/Page column 63; 64