With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31321-68-3,(R)-Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.
To a solution of (R)-piperazine-2-carboxylic acid (70 g, 344.71 mmol, 1.0 equiv, 2HCl) in dioxane (1120 mL) and H2O (700 mL) was added 50% aq. NaOH until the solution was pH=11. Benzyl chloroformate (156.82 mL, 1.10 mol, 3.2 equiv) was added and the reaction mixture was stirred at room temperature for 12 h. To the solution was then added H2O (1200 mL) and the aqueous layer was washed with MTBE (3 x 800 mL). The aqueous layer was adjusted to pH=2 with concentrated HCl (12N) and extracted with EtOAc (2 x 1000 mL). The combined organic extracts were dried, filtered and the filtrate was concentrated under reduced pressure to afford the desired product (137 g, 99.8% yield) as a yellow solid. LCMS (ESI) m/z: [M + H] calcd for C21H22N2O6: 399.16; found 399.2., 31321-68-3
31321-68-3 (R)-Piperazine-2-carboxylic acid 6558437, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; REVOLUTION MEDICINES, INC.; PITZEN, Jennifer; GLIEDT, Micah James Evans; BURNETT, G. Leslie; AGGEN, James Bradley; KISS, Gert; CREGG, James Joseph; SEMKO, Christopher Michael; WON, Walter; WANG, Gang; LEE, Julie Chu-Li; THOTTUMKARA, Arun P.; GILL, Adrian Liam; MELLEM, Kevin T.; (484 pag.)WO2019/212990; (2019); A1;,
Piperazine – Wikipedia
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