Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.

To the solution of product of Step A (690 mg, 2.44 mmol) in DCM (10 mL) was added 1- ethylpiperazine (279 mg, 2.44 mmol) followed by Et3N (247 mg, 2.44 mmol). The solution was stirred at room temperature for 4 hours. TLC (PE/EA = 5/1) showed the reaction was completed. The resulting solution was concentrated and the residue (770 mg, yield: 99%) was used in next step directly. MS: IVJIe 318 (M+1)., 5308-25-8

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BEIGENE, LTD.; ZHOU, Changyou; ZHANG, Guoliang; WO2014/206343; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

187669-60-9, 1-(4-(Methylsulfonyl)phenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 67; 4-{2-[4-(4-Methanesulfonylphenyl)piperazin-l-yl]acetyl}piperidine-l- carboxylic acid tert-butyl ester; To a solution of l-(4-methanesulfonylphenyl)piperazine (0.055g, 0.23mmol) in MeCN (2mL) was added 4-(2-bromoacetyl)piperidine-l-carboxylic acid tert-butyl ester (0.07g, 0.23mmol) and K2CO3 (0.035g, 0.25mmol). The mixture was heated at reflux for 4h then allowed to cool. EtOAc (2OmL) was added and the organic phase washed with water, brine, dried (MgSO4) and the solvent removed in vacuo. The crude mixture was purified by flash chromatography with EtOAc as eluent to afford the title compound (0.07g, 65%): RT = 2.45 min; m/z (ES+) = 466.4 [M+ H]+

187669-60-9, As the paragraph descriping shows that 187669-60-9 is playing an increasingly important role.

Reference：
Patent; PROSIDION LIMITED; WO2007/3964; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of 0.32 mmol 5-cyano-2-isopropylsulfanyl-benzoic acid in 5 ml tetrahydrofuran were added successively 0.31 mmol TBTU, 0.84 mmol N-ethyldiisopropylamine and 0.22 mmol 1-(4-trifluoromethylphenyl)-piperazine (commercially available, e.g. from Fluorochem). The reaction mixture was stirred at 35 C. for 16 h and then concentrated in vacuo. Chromatography (SiO2, ethyl acetate/heptane) followed by trituration in pentane afforded the title compound as an off-white solid (yield 94%). MS (m/e): 434.4 (M+H+, 100%)., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Patent; Jolidon, Synese; Narquizian, Robert; Norcross, Roger David; Pinard, Emmanuel; US2006/149062; (2006); 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.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: The title compound was prepared according to General Protocol B. NMR (400 MHz, DMSO-c delta 7.48 – 7.14 (m, 9H), 4.29 (s, 1 H), 2.38 (s, 4H), 2.34 – 2.20 (m, 6H); LCMS ti (Method 1) = 4.630 min, m/z 317.2 [M+H+].General Protocol B. A solution of amine (0.105 mmol) in MeOH (1.00 mL) was treated at room temperature with aldehyde (0.525 mmol to 1.05 mmol, 5.0 to 10.0 equiv.), NaCNBH4 (19.7 mg, 0.315 mmol, 3.0 equiv.) and acetic acid (0.018 mL, 0.315 mmol, 3.0 mmol). The reaction mixture was stirred at room temperature for 1 – 8 h and quenched with 1 N NaOH solution. The mixture was dried by blowing air, re-dissolved in DMSO, filtered and purified by HPLC. The title compound was prepared according to General Protocol B as a TFA salt. LCMS t, (Method 1) = 3.990 min, m/z 445.2 [M+H+]., 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

Reference：
Patent; THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; LIANG, Tsanyang Jake; FERRER, Marc; HE, Shanshan; HU, Xin; HU, Zongyi; MARUGAN, Juan Jose; SOUTHALL, Noel Terrence; XIAO, Jingbo; ZHENG, Wei; WO2015/80949; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

934-98-5,934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Spirothiazamenthane 3 (1.0 eq) was dissolved in toluene (0.1 M concentration) in a microwave vial and the solution was treated with amine (10 eq) and PTSA (20 mol percent). This mixture was heated at 150 °C using microwaves for 4 h. After cooling, the solvents were removed by evaporation and the resulting residue was taken up in 1:1 Et2O/2M NaOH. The layers were separated and the aqueous layer was extracted 2 × with Et2O. The organic layers were combined, dried over Na2SO4, filtered and concentrated. The resulting crude products were purified as described below. Variations in reaction conditions are also noted below.

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Arns, Steve; Balgi, Aruna D.; Shimizu, Yoko; Pfeifer, Tom A.; Kumar, Nag; Shidmoossavee, Fahimeh S.; Sun, Sharon; Tai, Sheldon S.-H.; Agafitei, Olga; Jaquith, James B.; Bourque, Elyse; Niikura, Masahiro; Roberge, Michel; European Journal of Medicinal Chemistry; vol. 120; (2016); p. 64 – 73;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5625-67-2

Step 1: tert-Butyl-3-oxopiperazine-1-carboxylate To a solution of piperazin-2-one (22.00 g, 219.7 mmol) in THF (300 mL) was added a mixture of NaHCO3 (29.53 g, 307.6 mmol) in H2O (100 mL), (Boc)2O (43.16 g, 197.8 mmol), then the reaction solution was stirred at rt for 16 h. The mixture was concentrated, poured into water (100 mL) and extracted with EtOAc (100 mL*2). The combined organic layers were dried over Na2SO4, filtered and concentrated to obtain tert-butyl-3-oxopiperazine-1-carboxylate (40.00 g, 90.91%) as white solid. ESI-MS (EI+, m/z): 145.2[M+H-56]+. 1H NMR (500 MHz, CDCl3) delta 4.08 (s, 2H), 3.62 (t, J=5.2 Hz, 2H), 3.37 (s, 2H), 1.47 (s, 9H).

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A vial was charged with 5-amino-3,6-dichloro-l,2,4-triazine (736 mg, 4.46 mmol), diisopropylethylamine (2.0 mL, 11.48 mmol), tert-butyl 2-(3,3-dimethylpiperazin-l- yl)acetate (1.0875 g, 4.52 mmol) in dioxane (8 mL). The mixture was heated at 155 C for 12 h using microwave. The mixture was concentrated to remove all of solvent. The residue was treated with saturated sodium bicarbonate solution, extracted with dichloromethane (4 x 50 mL). The combined organic solution was washed with brine, dried over anhydrous sodium sulfate, concentrated. The residue was separated with flash column chromatography on silica gel using 1-10% methanol in dichloromethane, and 30-100% ethyl acetate/Hexane to afford product (201.8 mg) in 13% yield. NMR (500 MHz, Chloroform-*/) delta 5.12 (s, 2H), 4.06 – 4.02 (m , 2H), 3.52 – 3.46 (m, 2H), 1.50 (s, 6H), 1.44 (s, 9H). MS for C 14H23CIN6O2: 343.2 (MH+).

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A 100-mL round-bottom flask was charged with triphosgene (0.743 g, 2.50 mmol, 0.50 equiv), tert-butyl (R)-3-methylpiperazine-1-carboxylate (1.00 g, 5.00 mmol, 1.00 equiv), and dichloromethane (10 mL). DIPEA (1.94 g, 15.0 mmol, 3.00 equiv) was added at 0 C. The reaction was stirred for 3 hours at room temperature and quenched with water (80 mL). The mixture was extracted with dichloromethane (2*100 mL) and the organic layers were combined, washed with brine (2*80 mL), dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to provide 1.40 g of tert-butyl (R)-4-(chlorocarbonyl)-3-methylpiperazine-1-carboxylate as a yellow oil. LCMS (ESI, m/z): 263 [M+H]+.

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ABIDE THERAPEUTICS, INC.; GRICE, Cheryl A.; CISAR, Justin S.; DUNCAN, Katharine K.; FENG, Yu; WIENER, John J.M.; WEBER, Olivia D.; (79 pag.)US2018/256566; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 30 2-piperazin-1-ylethyl 4-phenylpiperazine-1-carboxylate trihydrochloride To a solution of 1-(2-hydroxyethyl)piperazine (51.7 g, 398 mmol) in DCM (500 mL) was added NEt3 (70.0 mL, 526 mmol) and di-tert-butyl dicarbonate (80.0 g, 367 mmol). The reaction mixture was stirred overnight at room temperature then washed with 1 M aq Na2CO3 solution (2*300 mL), dried (MgSO4) and concentrated in vacuo to give tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (66.0 g, 72%) as a colourless oil. Analytical LCMS: (System D RT=1.54 min), ES+: 231.4 [MH]-4., 103-76-4

103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Biovitrum AB; US2009/281087; (2009); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of the product of step A (500 mg, 2.5 mmol), methyl 4-(bromomethyl)-3- (trifluoromethyl)benzoate (891 mg, 3.0 mmol) and Et3N(505 mg, 5.0 mmol) in DCM (20 mL) was stirred at room temperature for 2 hours. The reaction mixture was diluted with DCM (lOOmL), washed with brine (30 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was purified by column chromatography (silica weight: 10 g, eluted with petroleum ether/EA: 10/1) to give the title compound (700 mg, 70%) as oil. 1H MR (400 MHz, CDC13) delta 8.31 (s, 1H), 8.19 (d, J= 8.0 Hz, 1H), 7.95 (d, J= 8.0 Hz, 1H), 4.26-4.16 (m, 1H), 3.95 (s, 3H), 3.86-3.80 (m, 1H), 3.66 (s, 2H), 3.18 – 3.07 (m, 1H), 2.76- 2.68 (m, 1H), 2.58-2.51 (m, 1H), 2.30-2.23 (m, 1H), 2.18 – 2.08 (m, 1H), 1.46 (s, 9H), 1.28- 1.25 (m, 3H)ppm.

169447-70-5, The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BEIGENE, LTD.; ZHOU, Changyou; ZHANG, Guoliang; WO2014/206344; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics