Category: 129799-15-1

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

Potassium carbonate (1 .2 g, 8.7 mmol) was added to a solution of 3-(2-bromo-thiazol-4-yl)-5-(2,6-difluoro-phenyl)-4,5-dihydro-isoxazole (1.25 g, 3.6 mmol) and 1-N-Boc-2-piperazinecarboxylic acid methyl ester (1 .1 g, 4.4 mmol) in 15 ml of acetonitrile. The reaction mixture was stirred for 150 h at 90 00 and subsequently cooled and filtered. The solid potassium salt was washed with ethyl acetate and the filtrate as well as the washing layers were combined and evaporated. The remainder was purified by column chromatography onsilica gel (cyclohexane I ethyl acetate 4: 1) to obtain 4-{4-[5-(2,6-difluoro-phenyl)-4,5- di hydro-isoxazol-3-yl]-th iazol-2-yl}-piperazine-1 ,2-d icarboxylic acid 1 -tert-butyl ester 2-methyl ester as a light yellow foam. M.p. 68 – 72 00 1H-NMR (400 MHz, 0D013): oe = 1.42 – 1.53 (m, 9H), 3.09 (dd, 1 H), 3.33 (dt, 2H), 3.52 (dd, 1 H), 3.69 (t, 1 H), 3.74 (s, 3H), 3.91- 4.08 (m,2H), 4.42 (dd, 1H), 4.70 -4.93 (m, 1H), 6.02 (t, 1H), 6.89 (t, 2H), 7.00 (s, 1H), 7.24- 7.31 (m, 1H). MS: mlz = 509 (M+1).

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

Reference：
Patent; SYNGENTA PARTICIPATIONS AG; LAMBERTH, Clemens; SULZER-MOSSE, Sarah; CEDERBAUM, Fredrik; UMARYE, Jayant; SONAWANE, Ravindra; WO2013/127784; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Potassium carbonate (1 .2 g, 8.7 mmol) was added to a solution of 3-(2-bromo-thiazol-4-yl)-5-(2,6-difluoro-phenyl)-4,5-dihydro-isoxazole (1.25 g, 3.6 mmol) and 1-N-Boc-2-piperazinecarboxylic acid methyl ester (1 .1 g, 4.4 mmol) in 15 ml of acetonitrile. The reaction mixture was stirred for 150 h at 90 00 and subsequently cooled and filtered. The solid potassium salt was washed with ethyl acetate and the filtrate as well as the washing layers were combined and evaporated. The remainder was purified by column chromatography onsilica gel (cyclohexane I ethyl acetate 4: 1) to obtain 4-{4-[5-(2,6-difluoro-phenyl)-4,5- di hydro-isoxazol-3-yl]-th iazol-2-yl}-piperazine-1 ,2-d icarboxylic acid 1 -tert-butyl ester 2-methyl ester as a light yellow foam. M.p. 68 – 72 00 1H-NMR (400 MHz, 0D013): oe = 1.42 – 1.53 (m, 9H), 3.09 (dd, 1 H), 3.33 (dt, 2H), 3.52 (dd, 1 H), 3.69 (t, 1 H), 3.74 (s, 3H), 3.91- 4.08 (m,2H), 4.42 (dd, 1H), 4.70 -4.93 (m, 1H), 6.02 (t, 1H), 6.89 (t, 2H), 7.00 (s, 1H), 7.24- 7.31 (m, 1H). MS: mlz = 509 (M+1).

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

Reference：
Patent; SYNGENTA PARTICIPATIONS AG; LAMBERTH, Clemens; SULZER-MOSSE, Sarah; CEDERBAUM, Fredrik; UMARYE, Jayant; SONAWANE, Ravindra; WO2013/127784; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

To a solution of 7-benzyl-2,4-dichloro-6,8-dihydro-5H-pyrido [3,4-d] pyrimidine (5.00 g, 17.0 mmol) and 1-tert-butyl 2-methylpiperazine-1,2-dicarboxylate (4.24 g, 17.3 mmol) in DMSO (80 mL) was added DIEA (5.49 g, 42.5 mmol, 7.42 mL). After stirring at 55° C. for 12 hours, the mixture was diluted with ethyl acetate (100 mL), washed with brine (3 150 mL), dried over Na 2SO 4, filtered and concentrated under vacuum. The residue was purified by column chromatography (SiO 2, PE/EA=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-1,2-dicarboxylate (8.00 g, 15.9 mmol, 93.8% yield) as a yellow oil. ES+APCI MS m/z 502.1[M+H] +.

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

Reference：
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

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

4-Methanesulfonyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and mesylchloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was redissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 307.4 (M-H+), 129799-15-1

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

Reference：
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

4-Methanesulfonyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and mesylchloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was redissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 307.4 (M-H+), 129799-15-1

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

Reference：
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

4-Methanesulfonyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and mesylchloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was redissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 307.4 (M-H+), 129799-15-1

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

Reference：
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 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 40C for 3 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 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

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

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

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

To a stirred solution of 1-tert-butyl 2-methyl piperazine-l,2-dicarboxylate (1.0 g) and K2C03 (1.12 g, 2 eq) in DMF (15 mL), l-fluoro-4-nitrobenzene (0.86 g, 1.5 eq) was added and the mixture stirred at 90 C for 12 h. After TLC showed completion of starting material, the mixture was poured into ice cold water and extracted with ethyl acetate (3 x 100 mL). The organic layer was washed with water (3 x 50 mL), dried over Na2S04 and concentrated to afford the final compound (1.3 g, 87%) as yellow solid. 1H NMR (400MHz, CDCI3): delta 8.22 (d, 2H), 6.98 (d, 2H), 4.38 (t, 2H), 3.67 (t, 2H). LCMS calculated for (M) 365.39 and found (M+H) 366.21, LCMS showed 86.8 % purity., 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：
Patent; ASANA BIOSCIENCES, LLC; VENKATESAN, Aranapakam M.; SMITH, Roger A.; THOMPSON, Scott K.; LAPING, Nicholas; KULKARNI, Bheemashankar; HALLUR, Gurulingappa; VISWANADHAN, Vellarkad N.; PENDYALA, Muralidhar; KETHIRI, Raghava Reddy; TYAGI, Rajiv; SIVANANDHAN, Dhanalakshmi; BAKTHAVATCHALAM, Rajagopal; WO2015/38417; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

To a solution of 1-tert-butyl 2-methyl piperazine-1, 2-dicarboxylate (0.2g, 0.82 mmol) and triethylamine (1.2 mL, 8.2 mmol) in anhydrous THF (5 mL) atrt was added trimethylsilyl isocyanate (1.1 mL, 8.2 mmol) dropwise. The mixturewas stirred at rt for 8 h and quenched with ice-water (10 mL) , and then THFwas removed. The aqueous layer was extracted with EtOAc (10 mL × 3) . The combined organiclayers were dried over anhydrous Na2SO4 and concentratedto give 1-tert-butyl 2-methyl 4-carbamoylpiperazine-1, 2-dicarboxylate asa white solid (0.3 g, 90) . 1H NMR (400 MHz, CDCl3): delta ppm 4.24 (br.s, 2H) , 4.30 (d, J 13.3 Hz, 1H) , 3.98-4.14 (m, 1H) ,3.83-3.94 (m, 1H) , 3.78 (s, 3H) , 3.18-3.28 (m, 1H) , 3.03-3.12 (m, 1H) ,2.79-2.96 (m, 1H) , 1.50 (d, J 16.7 Hz, 9H) and MS-ESI: m/z 232.25 [M-55] +.

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

Reference：
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

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

To a solution of 1-tert-butyl 2-methyl piperazine-1, 2-dicarboxylate (0.2g, 0.82 mmol) and triethylamine (1.2 mL, 8.2 mmol) in anhydrous THF (5 mL) atrt was added trimethylsilyl isocyanate (1.1 mL, 8.2 mmol) dropwise. The mixturewas stirred at rt for 8 h and quenched with ice-water (10 mL) , and then THFwas removed. The aqueous layer was extracted with EtOAc (10 mL × 3) . The combined organiclayers were dried over anhydrous Na2SO4 and concentratedto give 1-tert-butyl 2-methyl 4-carbamoylpiperazine-1, 2-dicarboxylate asa white solid (0.3 g, 90) . 1H NMR (400 MHz, CDCl3): delta ppm 4.24 (br.s, 2H) , 4.30 (d, J 13.3 Hz, 1H) , 3.98-4.14 (m, 1H) ,3.83-3.94 (m, 1H) , 3.78 (s, 3H) , 3.18-3.28 (m, 1H) , 3.03-3.12 (m, 1H) ,2.79-2.96 (m, 1H) , 1.50 (d, J 16.7 Hz, 9H) and MS-ESI: m/z 232.25 [M-55] +.

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

Reference：
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