Downstream synthetic route of (R)-Piperazine-2-carboxylic acid

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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.

S-127 (200 mg) was converted to S-128 using B0C2O in the presence of NaOH in dioxane and H2O. The reaction was stirred at room temperature for 12 hours. After purification, 400 mg of S-128 was obtained., 31321-68-3

As the paragraph descriping shows that 31321-68-3 is playing an increasingly important role.

Reference£º
Patent; G1 THERAPEUTICS, INC.; STRUM, Jay, Copeland; JUNG, David; (207 pag.)WO2019/136244; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 31321-68-3

31321-68-3, The synthetic route of 31321-68-3 has been constantly updated, and we look forward to future research findings.

31321-68-3, (R)-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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 (1187) 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, The synthetic route of 31321-68-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; REVOLUTION MEDICINES, INC.; SEMKO, Christopher Michael; WANG, Gang; BURNETT, G. Leslie; AGGEN, James Bradley; KISS, Gert; CREGG, James Joseph; GLIEDT, Micah James Evans; PITZEN, Jennifer; LEE, Julie Chu-Li; WON, Walter; THOTTUMKARA, Arun P.; GILL, Adrian Liam; (356 pag.)WO2019/212991; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 31321-68-3

31321-68-3 (R)-Piperazine-2-carboxylic acid 6558437, apiperazines compound, is more and more widely used in various.

31321-68-3, (R)-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The Boc protecting group of previous compound was removed at room temperature for one hour with a solution of AcOEt/HCl 4M. The mixture was then concentrated in vacuo, diluted with MeOH and concentrated several times in vacuo. The residue was then coupled with the corresponding acid (1.1 eq.), in the presence of BOP (1.1 eq.) and NMM (2.2 eq.) for two hours, in DCM. The mixture was then concentrated in vacuo and the residue dissolved in AcOEt. The organic layer was successively washed with aqueous solutions of 1M KHSO4, saturated NaHCO3 and brine. The organic layer was then dried over Na2SO4, filtered and concentrated in vacuo to yield the desired compound which was then treated with 4M AcOEt/HCl as already described if necessary. The final compound purified by preparative HPLC on a C18 column using a water/acetonitrile/TFA 0.1% gradient (yield around 50% for the three steps).

31321-68-3 (R)-Piperazine-2-carboxylic acid 6558437, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; AETERNA ZENTARIS GmbH; CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE; University of Montpellier I; University of Montpellier II; US2009/239877; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics