N-methyl-2-pyrrolidone → 2-(2-chlorobenzyl)-3-[2-(tetrahydro-pyran-4-ylamino)-pyrimidin-4-yl]-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-one

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To a solution of 2-(2-chloro-benzyl)-3-(2-methanesulfonyl-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-one, 8, (0.10, 0.26 mmol) in NMP (2 mL) is added amino tetrahydropyran (0.09 mL, 0.78 mmol). After stirring 1.5 hours at 90° C., the reaction mixture is diluted with methanol (to 5 mL) and is purified by reversed phase liquid chromatography (CH3CN/water/1% TFA) to afford 44 mg (40%) of the desired product. 1H NMR (300 MHz, CDCl3) δ 8.30 (d, J=5.1 Hz, 1H), 7.39-7.12 (m, 4H), 6.57 (d, J=5.1 Hz, 1H), 4.10-3.94 (m, 9H), 3.60-3.48 (m, 2H), 2.80-2.68 (m, 2H), 2.95-1.95 (m, 2H), 1.65-1.50 (m, 2H); ESI− MS: m/z (rel intensity) 426.0 (100, M+−H).

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