Some tips on Methyl 1-Boc-piperazine-2-carboxylate

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

The compound N-1- t-butoxycarbonyl-2-piperazine-carboxylate (0.2g, 0.82mmol) and triethylamine (1.2mL,8.2mmol) was dissolved None Water tetrahydrofuran (5mL), at room temperature, to this solution was addeddropwise trimethylsilyl isocyanate (1.1mL, 8.2mmol), stirred at room temperature 8H, ice water (10 mL),tetrahydrofuran spin, the aqueous phase with ethyl acetate (10mL ¡Á 3). The organic phase was dried overanhydrous Na 2 SO 4 Drying, the solvent was removed, and concentrated to give 0.2g white solid: 2-methoxycarbonyl-4-carbamoyl-piperazine-1-carboxylate, yield: 90%.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Piperazine-1, 2-dicarboxylic acid, 1-tert-butyl ester, 2- methyl ester (250 mg, 1.03 mmol) was added dropwise to a stirred solution of 4-bromobenzoyl chloride (250 mg, 1.14 mmol), triethylamine (0.43 mL, 3.09 mmol) and DMAP (5 mg) in anhydrous 1,2-dichloroethane (10 mL) at room temperature. The reaction mixture was stirred for 2 hrs (TLC control) and then poured into water (25 mL) and extracted with diethyl ether (3 x 25 mL). The combined extract was washed with water (2 x 10 mL), brine (3 x 10 mL), dried over anhydrous MGS04, filtered and concentrated in vacuo. Purification of the product by flash column chromatography, using 40 % ethyl acetate/hexane as eluent, afforded the title compound as a white foam (310 mg, 71 %)., 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; THE INSTITUTE OF PHARMACEUTICAL DISCOVERY, LLC; WO2004/99192; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 129799-15-1

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-1, 2-dicarboxylic acid, 1-TERT-BUTYL ester, 2- methyl ester (250 mg, 1.03 mmol) was added dropwise to a stirred solution of 4-bromobenzenesulfonyl chloride (290 mg, 1.14 mmol) and pyridine (1 mL) in anhydrous 1,2-dichloroethane (10 mL) at room temperature. The reaction mixture was stirred for 1 hr (TLC control) and then poured into water (25 mL) and extracted with diethyl ether (3 x 25 mL). The combined extract was washed with water (2 x 10 mL), brine (3 x 10 mL), dried over anhydrous MGS04, filtered and concentrated in vacuo. Purification of the product by flash column chromatography, using 40 % ethyl ACETATE/HEXANE as eluent, afforded the title compound as a white foam (350 mg, 74 %).

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; THE INSTITUTE OF PHARMACEUTICAL DISCOVERY, LLC; WO2004/99192; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of Methyl 1-Boc-piperazine-2-carboxylate

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-1,2-dicarboxylic acid, 1-tert-butyl ester, 2-methyl ester (250 mg, 1.03 mmol) was added dropwise to a stirred solution of 4-bromobenzoyl chloride (250 mg, 1.14 mmol), triethylamine (0.43 mL, 3.09 mmol) and DMAP (5 mg) in anhydrous 1,2-dichloroethane (10 mL) at room temperature. The reaction mixture was stirred for 2 hrs (TLC control) and then poured into water (25 mL) and extracted with diethyl ether (3¡Á25 mL). The combined extract was washed with water (2¡Á10 mL), brine (3¡Á10 mL), dried over anhydrous MgSO4, filtered and concentrated in vacuo. Purification of the product by flash column chromatography, using 40% ethyl acetate/hexane as eluent, afforded the title compound as a white foam (310 mg, 71%), 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; The Institutes for Pharmaceutical Discovery, LLC; US2006/122222; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 129799-15-1

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-1,2-dicarboxylic acid, 1-tert-butyl ester, 2-methyl ester (250 mg, 1.03 mmol) was added dropwise to a stirred suspension of 4-bromobenzyl bromide (283 mg, 1.14 mmol) and cesium carbonate (1.0 g, 3.09 mmol) in anhydrous DMF (10 mL) at room temperature. The reaction mixture was stirred at 40 C. for 3 hrs (TLC control) and then poured into water (25 mL) and extracted with diethyl ether (3¡Á25 mL). The combined extract was washed with water (2¡Á10 mL), brine (3¡Á10 mL), dried over anhydrous MgSO4, filtered and concentrated in vacuo. Purification of the product by flash column chromatography, using 40% ethyl acetate/hexane as eluent, afforded the title compound as a white foam (270 mg, 64%)

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; The Institutes for Pharmaceutical Discovery, LLC; US2006/122222; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of Methyl 1-Boc-piperazine-2-carboxylate

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 7-benzyl-2,4-dichloro-6,8- dihydro-5H-pyrido[3,4-d] pyrimidine (2.00 g, 6.80 mmol, 1.00 eq) in DMSO (40.0 mL) was added DIEA (1.76 g, 13.6 mmol, 2.38 mL, 2.00 eq) and 1-tert-butyl 2-methylpiperazine-l,2- dicarboxylate (1.74 g, 7.14 mmol, 1.05 eq). The mixture was stirred at 55 C for 16 hours. The mixture was diluted with water (100 mL) and extracted with ethyl acetate (3 x 100 mL). The combined organic layers were washed with brine (3 chi 100 mL), dried over Na2S04, filtered and concentrated to dryness. The residue was purified by column chromatography (S1O2, diethyl ether/ethyl acetate = 1 :0 to 3 : 1) to give 1-tert-butyl 2-methyl-4-(7-benzyl-2-chloro-6,8-dihydro- 5H-pyrido[3,4-d]pyrimidin -4-yl)piperazine-l,2-dicarboxylate (3.10 g, 5.70 mmol, 83.8 % yield, 92.3 % purity) as a yellow semisolid. ESI MS m/z 502.2 [M+H]+.

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,129799-15-1

A mixture of (S) -5- (1- ( (tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4- (difluoromethoxy) phenyl) oxazole-4-carboxylic acid (0.25 g, 0.53 mmol) , 1-tert-butyl 2-methyl piperazine-1, 2-dicarboxylate (157 mg, 0.64 mmol) , EDCI (153 mg, 0.80 mmol) and HOAT (181 mg, 1.33 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.37 mL, 2.13 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 5 h. The mixture was concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 3/1 to give the title compound as colorless thick oil (260 mg, 70) .1H NMR (400 MHz, CDCl3) : delta ppm 7.55-7.62 (m, 2H) , 7.26 (d, J 8.4 Hz, 1H) , 6.72 (t, JF-H 75.1 Hz, 1H) , 5.25-5.29 (m, 1H) , 3.97-4.01 (m, 3H) , 3.79 (br. s, 1H) , 3.58-3.63 (m, 2H) , 1.50-1.52 (m, 3H) , 1.48 (s, 9H) , 1.45 (s, 9H) , 1.32-1.35 (m, 1H) , 0.68-0.73 (m, 2H) , 0.42-0.44 (m, 2H) and MS-ESI: m/z 695.3 [M+H] +.

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about Methyl 1-Boc-piperazine-2-carboxylate

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

129799-15-1, Step 3 4-(4-Chloro-phenyl)-piperazine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester 4-Chloro phenyl boronic acid (2.0 equiv, 3.68 mmol) and piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (1.0 equiv, 1.84 mmol) were dissolved in dichloromethane followed by the addition of copper acetate (1.0 equiv), 4 A molecular sieves and pyridine (2.0 equiv). The reaction mixture was stirred at room temperature for 72 h. The reaction mixture was concentrated in vacuo, dissolved in ethyl acetate, filtered through celite and concentrated. The crude product was purified using gradient elution from hexane/ethyl acetate (5%) to hexane/ethyl acetate (20%). ESI-MS m/z: 354 (M+1), UV retention time: 2.88 min.

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; Millennium Pharmaceuticals, Inc.; Kyowa Hakko Kirin Co., Ltd.; LULY, Jay R.; NAKASATO, Yoshisuke; OHSHIMA, Etsuo; HARRIMAN, Geraldine C.B.; CARSON, Kenneth G.; GHOSH, Shomir; ELDER, Amy M.; MATTIA, Karen M.; (190 pag.)US2016/31908; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of Methyl 1-Boc-piperazine-2-carboxylate

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 6-bromo-4,7-dichloroquinazoline (300 mg, 1.08 mmol), tert-butyl methyl piperazine-1,2-dicarboxylate (395 mg, 1.62 mmol), DIEA (836 mg, 6.48 mmol) in 1,4-dioxane (8 mL) was stirred at 80C for 1 h. The mixture was allowed to cool to RT, quenched with saturated NaHCO3 solution and then extracted with ethyl acetate. The organic layer was washed with brine, dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by flash column chromatography onsilica gel (ethyl acetate/petroleum ether = 1:5) to afford the desired product (367 mg,70% yield) as a white solid., 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about Methyl 1-Boc-piperazine-2-carboxylate

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

To a mixture of 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (5.0 g, 22.6 mmol, 1.00 eq) in MeOH (50.0 mL) was added HCl/dioxane (4.0 M, 134 mL). The reaction mixture was degassed and purged with nitrogen 3 times, and the mixture was stirred at 25¡ã C. for 12 hours under a nitrogen atmosphere. The reaction mixture was concentrated under reduced pressure to dryness to give methyl piperazine-2-carboxylate (4.89 g, 2HCl, crude) as a white solid, which was used directly in the next step without further purification., 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics