Some tips on 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

120737-78-2, General Procedure: To a round bottom flask equipped with a stir bar were added l-bromo-2- chloro-4-fluoro benzene (0.314 g, 1.5 mmol), 2-methyl-piperazine-l-carboxylic acid tert-butyl ester (0.451 g, 2.25 mmol), sodium tert-butoxide (0.216 g, 2.25 mmol) and toluene (15 mL). The reaction mixture was heated to 80 C and then a mixture of tris(dibenzylidine acetone)dipalladium (31.1 mg, 0.015 mmol) and racemic 2,2′-bis(diphenylphosphino)-l,l’- binaphthyl (13.7 mg, 0.05 mmol) in toluene (2 mL) was slowly added to the reaction mixture. The reaction mixture was stirred at 110 C overnight and then concentrated in vacuo. The residue was dissolved in ethyl acetate (100 mL) and washed with water (3 x 50 mL) and brine (50 mL). The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The crude residue was purified on silica gel using hexanes:diethyl ether = 100:0 to 80:20 in a gradient fashion, to give the desired product (147.9 mg, 28 %). 1H NMR (300 MHz5 CDCl3): delta 7.15 (m, IH)5 6.96 (m, 2H), 4.33 (m5lH), 3.95 (d, IH), 3.29 (m5 IH), 3.13 (m5 2H), 2.74 (m, 2H)5 1.49 (s, 9H)5 1.40 (d, 3H).

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2007/87135; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics