Sep 2021 News 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.

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

Sep 2021 News Analyzing the synthesis route of (S)-tert-Butyl 2-methylpiperazine-1-carboxylate

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6.1. Example 1(S)-N-(3-bromo-4-fluorophenyl)-2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxamide The captioned compound was prepared in several steps.A. Preparation of (S)-tert-butyl 2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxylate. (S)-tert-butyl 2-methylpiperazine-1-carboxylate (3 g, 15 mmol), N,N-diisopropylethylamine (3 ml), and 4-chloro-5-methyl-7H-pyrrolo[2,3-d]pyrimidine (2 g, 12 mmol) were added to isopropanol (10 ml). The solution was heated at 120 C. in a sealed pressure tube for 12 hours. The reaction was concentrated under vacuum, and the residue was purified by flash chromatography (80 g SiO2, 0-5% MeOH: CH2Cl2, 50 min) to give clean (S)-tert-butyl 2-methyl-4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazine-1-carboxylate (1.5 g, 4.5 mmol, 38%).1H NMR (400 MHz, chloroform-d) delta ppm 10.42 (br. s., 1H), 8.39 (s, 1H), 6.96 (s, 1H), 4.40 (d, J=6.06 Hz, 1H), 3.83-4.01 (m, 2H), 3.43 (td, J=12.57, 3.41 Hz, 1H), 3.32 (dd, J=12.76, 3.92 Hz, 1H), 3.07 (td, J=12.32, 3.41 Hz, 1H), 2.44 (s, 3H), 1.50 (s, 9H), 1.24 (d, J=6.82 Hz, 3H); MS (ES+) [M+H]+=332.

169447-70-5, As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference:
Patent; Harrison, Bryce Alden; Kimball, Spencer David; Mabon, Ross; Rawlins, David Brent; Rice, Dennis S.; Voronkov, Michael Victor; Zhang, Yulian; US2009/42893; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate

The synthetic route of 314741-40-7 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step D: tert-butyl (3S)-4-[2-(3-cyano-4-fluorophenyl)-2-oxoethyl] -3-(hydroxymethyl)piperazine-1-carboxylate: 5-(Bromoacetyl)-2-fluorobenzonitrile (590 mg, 2.44 mmol) and (S)-4-N-BOC-2-hydroxymethyl-piperazine (527 mg, 2.44 mmol) were dissolved in THF (40 mL) at 0C thenTEA (247 mg, 2.44 mmol) was added. The reaction mixture was stirred at RT for 16 h, thenpoured into water and extracted with ethyl acetate. The organic layer was dried over Na2SO4,filtered, and evaporated to dryness. The crude product was purified by MPLC through an 80gRedi-sep column using 0-100% EtOAc/hexane to yield the title compound., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

7 Sep 2021 News New learning discoveries about tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate

192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

192130-34-0, tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 : /er/-Butyl 4-(2-(dinonylamino)ethyl)piperazine-l-carboxylate Chemical Formula: C29H59N3O2 (3037) Molecular Weight: 481.81 [00831] A mixture of 1-bromononane (1.81 g, 8.72 mmol), 4-(2-aminoethyl)-l-boc- piperazine (2.0 g, 8.72 mmol), K2C03 (2.4 g, 17.4 mmol), KI (145 mg, 0.872 mmol) in 44 mL MeCN was allowed to stir at 65 °C for 16 hours. The reaction mixture was cooled to room temperature, filtered, and the solids were washed with hexanes. The filtrate was extracted with hexanes, and the combined extracts were concentrated in vacuo. Purification by ISCO silica flash chromatography (0-20percent MeOH/DCM) provided tot-butyl 4-(2- (dinonylamino)ethyl)piperazine-l-carboxylate (924 mg, 1.92 mmol, 44percent). (3038) UPLC/ELSD: RT = 1.99 min. MS (ES): m/z (MH+) 482.36 for C29H59N3O2 (3039) lH NMR (400 MHz, CDC13) delta: ppm 3.45 (br. m, 4H); 3.10 (br. m, 2H); 2.59 (br. m, 2H); 2.44 (br. m, 8H); 1.60-1.00 (br. m, 37H); 0.91 (t, 6H)., 192130-34-0

192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; MODERNATX, INC.; BENENATO, Kerry E.; BUTCHER, William; (437 pag.)WO2017/112865; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

7 Sep 2021 News Downstream synthetic route of (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine

As the paragraph descriping shows that 300543-56-0 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.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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

7 Sep 2021 News Downstream synthetic route of 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2,5-dichloro-N-(3-nitrophenyl)pyrimidin-4-amine (0.9 g, 3.16 mmol), 2-methoxy-4-(4-methylpiperazin-1-yl)benzenamine (0.7 g, 3.16 mmol), in 2-BuOH (20 mL) was added TFA (0.25 mL, 3.16 mmol) and the resultant slurry was refluxed for 8 hours. The reaction mixture was allowed to cool to room temperature, neutralized with a saturated aqueous sodium bicarbonate solution and then extracted with ethyl acetate (3*500 mL). The combined organic extracts were dried anhydrous Na2SO4, filtered and concentrated at reduced pressure to give an oil which was purified by column chromatography on silica gel (100-200 mesh) eluting with 1-2% (v/v) methanol in dichloromethane to furnish the title compound as a pale brown solid (1 g, yield 72%). 1H NMR 400 MHz (DMSO-d6) delta 9.16 (s, 1H), 8.48 (s, 1H), 8.21 (t, J=7.8 Hz, 1H), 8.11 (s, 1H), 8.02 (s, 1H), 7.88 (dd, J1=7.9 Hz, J2=2.4 Hz, 1H), 7.50-7.46 (m, 1H), 7.38 (d, J=8.8 Hz, 1H), 6.59 (d, J=2.4 Hz, 1H), 6.35 (dd, J1=8.8 Hz, J2=2.4 Hz, 1H), 3.74 (s, 3H), 3.12 (t, J=4.8 Hz, 4H), 2.49 (t, J=4.8 Hz, 4H), 2.24 (s, 3H); LCMS m/e: 470 [M+1]+.

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference:
Patent; Sabila Biosciences LLC; MANSOUR, Tarek Suhayl; (66 pag.)US2018/208564; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

7 Sep 2021 News New learning discoveries about 1-(4-Trifluoromethylphenyl)piperazine

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

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 2-(2,4-dichlorophenyl)-4-oxo-1,2,3,4-tetrahydroquina zoline-6-sulfonyl chloride (0.1 g, 0.0002 mol) was added to a round bottomflask containing N,N-dimethylformamide (4 mL) under nitrogenatmosphere, N-phenyl piperzine derivatives (0.0002 mol) or 3-(4-phenylpiperazin-1-yl)propan-1-amine derivatives (0.0002 mol)was added at rt with stirring, followed by the addition of DIEA(1 mL). The stirring was continued for 1 h. After completion of thereaction, as indicated by TLC, The ice cold water was added to thereaction mixture stirred it for 5 min and then extract with Chloroform(10 mL). The chloroform layer was separated, dried overNa2SO4 and evaporated under vacuum to give corresponding sulphamidederivatives (5a-j, 6a-g) in good yields., 30459-17-7

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

Reference:
Article; Venkatesh, Ramineni; Kasaboina, Suresh; Jain, Nishant; Janardhan, Sridhara; Holagunda, Uma Devi; Nagarapu, Lingaiah; Journal of Molecular Structure; vol. 1181; (2019); p. 403 – 411;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Some tips on 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

The synthetic route of 694499-26-8 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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, Triphosgene (1.04 g, 3.5 mmol) and ClCH2CH2Cl (20 mL) were added into a 100 mL round-bottomed flask, and stirred at room temperature until triphosgene was completely dissolved and the system appears colorless and transparent. The reaction system was placed in an ice-salt bath and stirred, 3-iodo-4-methyl aniline (1.64 g, 7 mmol) in ClCH2CH2Cl (20 mL) solution was slowly added dropwise, and the system appears yellow milky. After the addition was complete, the mixture was stirred at room temperature for 4 hours. After the reaction was complete by TLC monitoring, Et3N (1.43 g, 14 mmol) was added, and stirred at room temperature for 0.5 hour. 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline (1.87 g, 7 mmol) was added and stirred at room temperature for 16 hours, and then the starting materials were monitored by TLC and LC-MS until the reaction was complete. The volatiles were removed by distillation under reduced pressure, and the residue was extracted with ethyl acetate (30 ml*3) and H2O (30 mL). The organic phases were combined, dried over anhydrous Na2SO4, concentrated and purified by column chromatography, to give a yellow solid. ESI-MS mz: [M+H]+=533.2.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; Wang, Yong; Zhao, Liwen; Zhang, Wenping; Chen, Hongyan; Bi, Sheng; Gao, Yiping; Chen, Hongbin; Liu, Yang; Xu, Xin; Zhang, Cang; US2015/152088; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Some tips on 1-Cbz-Piperazine

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: N-Cbz piperazine (0.55 g, 2.48 mmol, 1 eq) and carboxylic acid 8c?g (2.48 mmol, 1 eq) were dissolved in dry DMF (10 mL), the reaction mixture flushed with argon and cooled to 0 °C. N-methyl morpholine (NMM; 7.44 mmol,3 eq), hydroxybenzotriazole hydrate (HOBt; 2.98 mmol,1.2 eq) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimidehydrochloride HCl salt (EDC; 3.22 mmol, 1.3 eq) were slowly added. The reaction mixture was stirred under argon atmosphere for 5 h at 0 °C and an additional 15 h at room temperature. DMF was evaporated under reduced pressure and the residue redissolved in dichloromethane (10 mL).The dichloromethane phase was washed with H2O (1 x 10 mL), a 1 M HCl solution (3 x 10 mL), saturated aqueous NaHCO3 solution (3 9 10 mL), brine (1 x 20 mL), dried over Na2SO4, filtered, and the solvent evaporated under reduced pressure. The crude product was purified by flash column chromatography using ethyl acetate/hexane solvents as eluents to afford compounds 9c?g., 31166-44-6

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Juki?, Marko; Frlan, Rok; Chan, Fiona; Kirby, Robert W.; Madge, David J.; Tytgat, Jan; Peigneur, Steve; Anderluh, Marko; Kikelj, Danijel; Medicinal Chemistry Research; vol. 24; 6; (2015); p. 2366 – 2380;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of Methyl 1-Boc-piperazine-2-carboxylate

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

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