Methyl 2-(1,6-dihydro-6-oxopyriMidin-4-yl)acetate hydrochloride synthesis

Yield:-

Reaction Conditions:

Stage #1: 3-oxopentanedioic acid dimethyl ester;formamidine acetic acidwith sodium methylate in methanol at 20; for 48 h;
Stage #2: with hydrogenchloride in methanol;water;

Steps:

(6-Oxo-1, 6-DIHYDRO-PVRIMIDIN4-YLLACETIC acid methyl ester [0420] 1, 3-Acetonedicarboxylate (196 pi, 1.3 mmol) formamidine acetate (158 mg, 1.42 mmol) and sodium METHOXIDE (111 mg, 1.95 mmol) were dissolved in methanol (5 ML). It was stirred for 48 h at room temperature. HCI (2N) was added and the formed precipitate was collected by filtration. The filtrate was extracted with DICHLOROMETHAN . The solvent was removed and the title compound was obtained as a slightly yellow solid. [OJ, 1H NMR (400 MHz, CDCL3) No. 3.23 (BR S, 2H), 3.93 (S, 3H), 5. 92 (s, 1H), 7. 33 (d, 1H), 8. 10 (d, 1H).

References:

WO2005/5378,2005,A2 Location in patent:Page/Page column 88