With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.
HATU (184 mg, 0.48 mmol) was added to a stirred mixture of 4-(6-mefhyl-7-oxo-6,7-dihydro- lH-pyrrolo[2,3-c]pyridin-4-yl)benzoic acid (Intermediate D) (100 mg, 0.37 mmol), 1 – mefhylpiperazin-2-one (63 mg, 0.56 mmol), and diisopropylethylamine (168 mg, 1.30 mmol) in DMF (5 mL). The reaction mixture was stirred at room temperature for 8 h, at which time (0597) LCMS indicated that the reaction had gone to completion. The reaction mixture was partitioned between ethyl acetate (20 mL) and water (15 mL). The separated organic solution was washed with brine (2 x 10 mL), dried over sodium sulfate and concentrated under reduced pressure. The residue was purified by preparative HPLC, acetonitrile : water (10 nM ammonia bicarbonate) 35percent-65percent, to afford the title compound (47.9 mg, 15.8percent yield) as a white solid. 1H NMR (400 MHz, DMSC 5): 3 12.14 (s, 1 H), 7.66 (d, J= 8.4 Hz, 2 H), 7.52 (d, J- 8.4 Hz, 2 H), 7.45 (s, 1 H), 7.35 (s, 1 H), 6.47 (d, J= 2.0 Hz, 1 H), 4.12-4.09 (m, 4 H), 3.56-3.50 (m, 2 H), 3.47 (s, 3 H), 2.85 (s, 3 H). LCMS M/Z (M+H) 365.1. The following compounds were prepared in a similar fashion to Example 26: Examples 27-38, 59702-07-7
59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.
Reference：
Patent; GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC.; ALBRECHT, Brian, K.; BELLON, Steven, F.; BURDICK, Daniel, J.; COTE, Alexandre; CRAWFORD, Terry; DAKIN, Les, A.; HEWITT, Michael, Charles; HSIAO-WEI TSUI, Vickie; LEBLANC, Yves; MAGNUSON, Steven, R.; NASVESCHUK, Christopher, G.; ROMERO, F. Anthony; TANG, Yong; TAYLOR, Alexander, M.; WANG, Shumei; (128 pag.)WO2016/77380; (2016); A1;,
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