Category: 57260-71-6

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

STEP A: 4-(4-Bromo-2-cvano-phenyl)-piperazine-1-carboxylic acid tert-butyl ester. A mixture of 5-bromo-2-fluoro-benzonitrile (1.05g), piperazine-1 -carboxylic acid tert-butyl ester (1.08g) and Na2CO3 (1.03g) in DMF was heated to 1000C for 24h. The resulting mixture was cooled, diluted with water (50 ml_) and extracted with diethyl ether. The resulting mixture was dried over MgSO4, the solvent was removed and the resulting residue purified on SiO2 (hexanes/ EtOAc 0 to 25%) to yield the title compound., 57260-71-6

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; Janssen Pharmaceutica N.V.; WO2009/79593; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

In a pressure tube, 5-bromo-2-fluorobenzonitrile (2500 mg, 12.5 mmol), tert-butyl piperazine-1-carboxylate (2444.45 mg, 13.12 mmol), triethylamine (5.23 ml, 37.5 mmol) in dimethylsulfoxide (10 ml) were combined and refluxed at 100 C for ovn. The mixture was cooled, and partitioned between ethyl acetate and saturated aqueous sodium bicarbonate. The organic phase was dried using sodium sulfate and concentrated. The residue was purified by flash column chromatography on silica gel 5-60% ethyl acetate/hexane to provide a light brown oil, tert-butyl 4-(4-bromo-2-cyanophenyl)piperazine-1-carboxylate (3660 mg, 80%).

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Gilead Scientific Systems, Inc.; Cory, Kevin S; Doo, Jimin; Farrand, Julie; Guerrero, Juan A; Katana, Ashley A; Cato, Daryl; Laisaweed, Scott I; Lee, Jiayao; Lingco, John O; Nicolaus, May; Notte, Gregory; Phyen, Hyeoung-Jung; Sangy, Michael; Sumit, Arun C; Adam J, Surayyah; Stephens, Cork L; Venkatraman, Chandrasekar; Watkins, William J; Yang, Jong Yu; Jabloki, Jeff; Jifel, Shiela; Ro, Jennifer; Lee, Sung H; Jao, Chung Dong; Grove, Jeffery; Su, Jianjun; Blomgren, Peter; Mitchell, Scott A; Shyung, Jin Ming; Chandrasekar, Jayaraman; (460 pag.)KR2016/37198; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,57260-71-6

Synthesis of 4-(4-formyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (1). A mixture of 4-(tert-butyl-l -piperazinecarboxylate (556 mg, 3.0 mmol), 4- fluoro-benzaldehyde (315 mul, 3.0 mmol) and K2CO3 (514 mg, 3.7 mmol) in DMF (5 ml) was stirred at ambient temperature overnight. Reaction was diluted with water (30 ml) and extracted with EtOAc (50 ml x 2). Organic layer was washed with water (20 ml), 1 M aq. HCl (20 ml), water (20 ml x 2) and brine (20 ml) and dried over MgSO4 (anh.). Solvent was evaporated in vacuum. Residue was triturated with hexane. Formed precipitate was filtrated and dried in vacuum overnight to provide target compound (1) (342 mg, 39%) as off-white solid. LC-MS [M+H] 291.2 (C16H22N2O3+H, requires 291.38).

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACHAOGEN, INC.; WO2008/154642; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, General procedure: To a solution of 3a-3c (3.2mmol) and N, N-diisopropylethylamine (DIEA) (4.8mmol) in DMF (3mL) was added N-Boc-piperazine (3.6mmol), the resulting mixture was heated at 110C for 16h. The reaction mixture was poured into ice water (30mL) and extracted with ethyl acetate (3¡Á30mL), the combined organic layers were washed with brine (2¡Á30mL), dried over sodium sulfate, filtered and concentrated under reduced pressure. The crude residue was purified by silica gel chromatography with petroleum ether/ethylacetate (1: 3) to obtain 4a-4c.

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Liu, Yang; Yin, Yanzhen; Zhang, Zhen; Li, Carrie J.; Zhang, Hui; Zhang, Daoguang; Jiang, Changying; Nomie, Krystle; Zhang, Liang; Wang, Michael L.; Zhao, Guisen; European Journal of Medicinal Chemistry; vol. 138; (2017); p. 543 – 551;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 17Atert- Butyl 4-(cyclopropanecarbonyl)piperazine- 1 -carboxylate[00523] A mixture of compound tert-butyl piperazine-1 carboxylate (3.725 g, 20 mmol) and potassium carbonate (5.53 g, 40 mmol) in anhydrous dichloromethane (30 mL) was cooled to 0 C,cyclopropanecarbonyl chloride (2.30 g, 22 mmol) was then added dropwise. After the addition, the mixture was stirred at room temperature overnight. The mixture was diluted with dichloromethane (100 mL), washed with 10% citric acid (50 mL), followed by saturated sodium bicarbonate (50 mL), brine (100 mL), dried over anhydrous sodium sulfate, and concentrated to give tert-butyl 4- (cyclopropanecarbonyl)piperazine- 1 -carboxylate (3.7 g, yield 73%) as a white solid. ^-NMR (400 MHz, CDCI3) delta (ppm): 0.76-0.81 (m, 2H), 0.98-1.03 (m, 2H), 1.49 (s, 9H), 1.69-1.75 (m, 1H), 3.46-3.48 (m, 4H), 3.63-3.65 (m, 4H); LC-MS (ESI) m/z: 255(M+1)+., 57260-71-6

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; CHU, Daniel; WO2011/130661; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,57260-71-6

To the stirred solution of tert-butyl piperazine-l-carboxylate (6.0 g, 33.0 mmol, 1.0 eq) in acetonitrile (60 niL), the reaction mixture was cooled at 0 C, then added triethylamine (22 mL, 161 mmol, 5.0eq) and (bromomethyl)benzene (6.0 mL, 35.0 mmol, 1.1 eq) drop wise. The reaction mixture was stirred at room temperature for about 6 hours. The reaction mixture was diluted with water and extracted with CH2CI2. The combined organic extracts were dried over Na2S04, filtered and evaporated under reduced pressure to afford the desired product (6.5 g, yield: 76.0%) as a white solid.

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; HETERO RESEARCH FOUNDATION; BANDI, Parthasaradhi Reddy; KURA, Rathnakar Reddy; ADULLA, Panduranga Reddy; GAZULA LEVI, David Krupadanam; MUKKERA, Venkati; NEELA, Sudhakar; LANKA, Vl Subrahmanyam; (170 pag.)WO2017/17630; (2017); 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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,57260-71-6

EXAMPLE 125 N-Boc-N-bromoacetyl-piperazine The title compound was prepared as described above for N-bromoacetyl-N(bis-Boc-guanidinyl)piperazine from N-Boc-piperazine (prepared as per the procedure of Carpino, L.A., et al., J. Org. Chem., 1983, 48, 661-665) (23.0 g, 123 mmol), bromoacetyl bromide (25.0 g, 123 mmol), and diisopropyletyhl amine (21 mL, 156 g, 120 mmol) in 240 mL of CH2Cl2. Flash chromatographic purification afforded 25.0 g of the title compound as pale yellow crystals, yield 66%. Silica gel TLC Rf 0.34 (1:1 hexanes-EtOAc). 1H NMR delta1.37 (s, 9H), 3.30-3.56 (m, 8H), 3.80 (s, 2H). 13C NMR delta25.8, 28.2, 28.5, 41.9, 43.2, 46.5, 80.3, 154.4, 165.4. MS (FAB) m/z 331 (M+Na)+. HRMS (FAB) m/z 307.066 (M+H)+(C11H20BrN2O3 requires 307.065). Anal. Calcd. for C:LHlgBrN2O3: C, 43.01; H, 6.22; N, 9.12. Found: C, 43.24; H, 6.22; N, 9.37.

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ISIS Pharmaceuticals, Inc.; US6329523; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, The compound 1-tert-butoxycarbonyl piperazine (0.6g, 3.2mmol) and triethylamine (4.6mL, 32mmol) wasdissolved in dry tetrahydrofuran (10 mL), at room temperature, to this solution was added dropwisetrimethylsilyl isocyanate (4.2mL, 32mmol), stirred at rt for 1.5h, ice Water (10 mL), tetrahydrofuran spin, theaqueous phase with ethyl acetate (30mL ¡Á 3). The organic phase was dried over anhydrous Na 2 SO 4, removeThe solvent was concentrated and solid was washed with ethyl acetate (2mL) ultrasonic cleaning 1min, suctionfiltration, to give 0.3g white solid: 4-carbamoyl-piperazine 1-carboxylate, yield: 40%.

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl piperazine-l-carboxylate 4 (1 g, 5.38 mmol) in CH2C12 (15 mL) at 0 C, were added 2-bromoacetyl bromide (864 mg, 4.3 mmol) and TEA (1 mL, 7.53 mmol). The reaction mixture was warmed to RT and stirred for 4 h. The mixture was quenched with water (50 mL) and extracted with CH2C12 (2 x 40 mL). The combined organic extracts were washed with brine (20 mL), dried (Na2S04), filtered and concentrated under reduced pressure. The crude was purified (silica gel; eluting 25% EtOAc/ hexanes) to afford compound 2 (900 mg, 54%) as pale yellow solid. 1H MR (500 MHz, DMSO-i): delta 4.16 (s, 2H), 3.47-3.42 (m, 4H), 3.38-3.35 (m, 2H), 3.31-3.29 (m, 2H), 1.41 (s, 9H); LC-MS (ESI): m/z 328.1 (M+ + Na)., 57260-71-6

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference£º
Patent; PHARMAKEA, INC.; ROWBOTTOM, Martin W.; HUTCHINSON, John Howard; CALDERON, Imelda; (202 pag.)WO2016/144703; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Boc-pyridazine (compound F-1, 0.558 g, 3 mmol) was weighed in 10 mL of anhydrous CH2Cl2 in a 25 mL beaker and anhydrous Na2CO3 (0.848 g, 8 mmol) was weighed into 7 mL of deionized water. Pour into a 100 mL single-mouth bottle and stir it in an ice bath for 20 min. Dissolve bromoacetyl bromide (0.568 mL, 6.6 mmol) in 10 mL of anhydrous CH2C12 and quickly drip into a single-mouth flask. Add DMAP (36.7 mg) after the addition. 0.3 mmol), stirring continued, TLC traces until starting material conversion, transfer to room temperature reaction 1 h. Extract with CH2C12 (3 X 30 mL). Combine the organic layers and dry over anhydrous Na2SO4. Chromatographic separation of CH2Cl2/MeOH=60:1, v/ nu) 598 mg (Compound G-1) was obtained as a milky white solid, yield 65%.

57260-71-6, 57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; East China University of Science and Technology; Qian Xuhong; Xu Yufang; Jia Xiaotong; Zhu Weiping; Yang Youjun; (14 pag.)CN107619397; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics