Downstream synthetic route of Piperazine-2-carboxylic acid dihydrochloride

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

Intermediate 1 : 1 ,4-Bis{[(1 ,1 -Dimethylethyl)oxy]carbonyl}-2- piperazinecarboxylic acidTo a solution of 2-piperazinecarboxylic acid (10 g) dihydrochloride in methanol (500 mL) at 0 C was added triethylamine (28.8 mL) dropwise via a dropping funnel. After addition, the solution was stirred for 30 minutes and then cooled to 0 C before addition of di-tert-butyl dicarbonate (27.4 mL). The reaction was stirred for 18 h at room temperature. The reaction mixture was concentrated under vacuum and then partitioned between ethyl acetate (500 ml) and water (500 mL). The organic phase was washed with further water (500 mL) and then brine (300 mL) before it was dried (Na2S04), filtered and the solvent removed under vacuum to give an oil of 3g, which was discarded. The aqueous layer was acidified to pH 2 with 5M HCI and then extracted with ethyl acetate (2 x 700 mL). The organic phase was dried (Na2S04), filtered and the solvent removed under vacuum to give the title compound as a white solid (14.58 g).LCMS (low pH) RT 0.98 min : m/z (ES) 331 [M+H]+

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; CONVERGENCE PHARMACEUTICALS LIMITED; NORTON, David; ANDREOTTI, Daniele; WARD, Simon E; PROFETA, Roberto; SPADA, Simone; PRICE, Helen Susanne; WO2012/98400; (2012); A1;,
Piperazine – Wikipedia
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