With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.675-20-7,Piperidin-2-one,as a common compound, the synthetic route is as follows.
Example 5. Synthesis of a compound of formula (II): l-(4- methoxyphenyl)-6-[4-(2-oxo-piperidinyl)phenyl]-7-oxo-4,5,6,7-tetrahydro- l//-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl esterII IICompound II, prepared as in Example 4 (35.90 g, 69.40 mmol) is suspended in 250 ml of toluene in a 1L 4-necked flask equipped with coolant, thermometer and magnetic stirrer, in nitrogen atmosphere, delta-valerolactam (13.74 g, 138.60 mmol), K3PO4 (30.25 g, 142.50 mmol) and Cul (2.54 g, 13.34 mmol) are then added in sequence. The suspension obtained is degassed 3 times at room temperature; N,N’-dimethylethylenediamine (1.65 ml, 26.78 mmol) is then added and the mixture is heated to reflux temperature. After 48 h the end-of-reaction mixture is filtered through a Buchner funnel, and the filter is washed with 200 ml of toluene. The toluene phase is washed with a solution of Na2S2O3 (50 g in 160 ml of H2O, 2×80 ml), 15% NH3 (2×80 ml) and a saturated solution of NaCl (1×80 ml). The organic phase is anhydrified on (Na2SO4), filtered and evaporated under low pressure. A solid product is obtained (37 g), which is crystallised by AcOEt. After crystallisation the product is obtained as a pure white solid (22.7 g, yield 67%).1H NMR (300 MHz, DMSO-dtf): 67.47 (2H, dd, J0=8.7 Hz, Ar-H), 7.32 (2H, dd, Jo=9.0 Hz, Ar-H), 7.28 (2H, dd, J0=8.7 Hz, Ar-H), 6.90 (2H, dd, Jo=9.0 Hz, Ar-H), 4.32 (2H, q, J=6.9 Hz, COOCEbCH^, 4.06 (2H, t, J=6.6 Hz, CH2CH2N), 3.79 (3H, s, Ar-OCH3), 3.57 (2H, m, N(?CH2CH2CH2CO) 3.19 (2H, t, J=6.6 Hz, ?CH2N), 2.36 (2H, m, NCH2CH2CH2CH2CO), 1.83 (4H, m, NCH2CH2CH2CH2CO), 1.31 (3H, t, J=6.9 Hz, COOCH2CH3).
675-20-7 Piperidin-2-one 12665, apiperidines compound, is more and more widely used in various.
Reference£º
Patent; DIPHARMA FRANCIS S.R.L.; VLADISKOVIC, Chiara; ATTOLINO, Emanuele; LOMBARDO, Alessandro; TAMBINI, Simone; WO2012/168364; (2012); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem