With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.
Step AF.1 : 4-[3-(4-Chloro-5-iodo-pyrrolo[2,3-d]pyrimidin-7-yl)-cyclobutylmethy.]-1-methyl- piperazin-2-oneMethylpiperazin-2-one HCI salt (290 mg, 1.2832 mmol), 3-(4-Chloro-5-iodo-pyrrolo[2,3- d]pyrimidin-7-yl)-cyclobutanecarbaldehyde (Step AF.2, 265 mg, 0.733 mmol), and DIPEA (1.306 mL, 7.33 mmol) were dissolved in 1,2-dichloroethane (32 mL) and stirred at RT for 45 min. After adding NaBH(OAc)3 (409 mg, 1.832 mmol) the reaction mixture was stirred for 35 min at RT. Then, concentrated NaHC03 solution (50 mL) was added and the reaction mixture was extracted with DCM ( 40 mL, 4 x). The combined organic phases were washed with brine (10 mL), dried (Na2S04), and the solvent was evaporated, the resulting residue was purified by means of a Sepacore Control chromatographer (Buchi, Flawil, Switzerland) using RediSept silica gel column (12 g) (30 mL min; DCM: 10 min, DCM -> DCM/MeOH/NH3(99.45:0.5 :05) in 30 min) yielding the title compound as white solid. HPLC (Method B) tRel = 1.724 min. HPLC/MS tR = 0.52 min, M+H = 441.1. 1H NMR (600 MHz, DMSO-d6) delta ppm 8.16 (s, 1H), 7.74 (s, 1H), 6.15 (s/b, 2H), 5.00 (quintet, 1H), 3.26 (t, 2H), 2.95 (s, 2H), 2.78 (s, 3H), 2.65 (t, 2H), 2.56 (t, 2H), 2.50/2.15 (m/m, 2H/2H), 2.29 (m, 1H).
109384-27-2, 109384-27-2 1-Methylpiperazin-2-one hydrochloride 17060766, apiperazines compound, is more and more widely used in various fields.
Reference：
Patent; NOVARTIS AG; IRM LLC, a Delaware Limited Liability Company; CHEN, Bei; FAIRHURST, Robin, Alec; FLOERSHEIMER, Andreas; FURET, Pascal; JIANG, Songchun; LU, Wenshuo; MARSILJE, Thomas, H.; VAUPEL, Andrea; WO2011/64211; (2011); A1;,
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