79098-75-2, 3-Piperidin-4-yl-3,4-dihydro-1H-quinazolin-2-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated
79098-75-2, EXAMPLE 65 (+)-N-(1-(lH-Imidazol-2-yl)-2-(7-methyl-lH-indazol-5-yl) ethyl)-4-(2-oXo-1, 2- dihydroquinazolin-3 (4H)-yl) piperidine-1-carboxamide; tert-Butyl-l- (1H-imidazol-2-yl)-2- (7-methyl-2- [ {2- [trimethylsilyl] ethoxy} methyl]-2H-indazol-5-yl) ethylcarbamate (100 mg, 0.212 mmol) was dissolved in a trifluoroacetic acid/methylene chloride mixture (1: 1,2 mL) and stirred under nitrogen for 3 h. The solvent was removed in vacuo and the resulting crude mixture passed through a strong cationic exchange column. After washing the column with several volumes of methanol, the desired amine was obtained by washing the column with 2M ammonia in methanol. After concentration, the amine was dissolved in dimethylformamide (1.5 mL) at 0C and treated with carbonyl diimidazole (34.0 mg, 1.1 equiv). The reaction was stirred for 5 min at 0C, warmed to room temperature, stirred for 10 min, and treated with 3-piperidin-4-yl-3, 4-dihydro-lH-quinazolin-2-one (48.0 mg, 1. 1 equiv). The mixture was stirred at room temperature overnight. The solvent was evaporated and the residue purified by column chromatography to afford 48 mg (50%). 1H-NMR (CD3OD, 500 MHz) 8 1.50-1. 70 (m, 4H), 2.55 (s, 3H), 2.70- 2.95 (m, 3H), 3.40 (m, 1H), 4.00-4. 50 (m, 6H), 5.23 (dd, J=6. 4,9. 2, 1H), 6.79 (d, J=7. 6, 1H), 6.93-7. 05 (m, 5H), 7.04-7. 20 (m, 2H), 7.40 (s, 1H), 7.40 (s, 1H). Mass spec.: 499.4 (MH) +.
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Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2005/56550; (2005); A2;,
Piperidine – Wikipedia
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