Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of II-l-c (30 mg, 0.12 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)benzenamine (26.5 mg, 0.12 mmol), X-Phos (5.1 mg), Pd2(dba)3 (6.6 mg) andK2CO3 (49.8 mg, 0.36 mmol) in t-BuOH (1.5 mL) was heated at 100 “C in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The solvent was removed in vacuo and the residue was purified by reverse-phase prep-HPLC using a water (0.05% TFA)/acetonitrile (0.05% TFA) gradient to afford the title compound II-l as TFA salt (19 mg). 1H NMR (600 MHz, CD3OD) delta 7.76 (s, IH), 7.62 (s, br, IH), 6.77 (d, J= 2.4 Hz, IH), 6.67 (dd, J= 2.4, 8.4 Hz, IH), 4.08- 4.06 (m, IH), 3.95-3.85 (m, 6H), 3.77 (dd, J= 8.4, 12.6 Hz, IH), 3.65-3.60 (m, 2H), 3.40-3.25 (m, 5H), 3.15-3.05 (m, 2H), 2.98 (s, 3H), 2.90 (dd, J= 10.8, 14.4 Hz, IH), 2.75 (d, J= 15 Hz, IH), 2.31-2.27 (m, IH), 2.09-2.06 (m, IH), 1.98-1.93 (m, IH), 1.75-1.72 (m, IH). MS (ESI) m/z 438 (M+H)+

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; DENG, Xianming; KWIATKOWSKI, Nicholas, Paul; WO2010/80712; (2010); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

11 g (2.35 g, 10 mmol) was dissolved in a methanol solvent,Under nitrogen protection, 200 mg of Pd / C was added,And then through the H2 reaction,6h after the reaction is complete.The filtrate was collected by filtration, and concentrated to give 1.89 g of a solid. Yield 92%.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nantong University; Ling, Yong; Mou, Jiefei; Xu, Qibing; Feng, Jiao; Zhu, Peng; Liu, Ji; Wang, Tingting; Ge, Xiang; Liang, Shanshan; (26 pag.)CN106432235; (2017); A;,
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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 solution of 21 (200 mg, 0.93 mmol) in CH2C12 (5.0 mL) was charged with TFA (1.0 mL) at 0C. The reaction mixture was stirred at room temperature for 3 h. The reaction mixture was concentrated in vacuo to afford 22 [100 mg (cmde), 94%j as a liquid.

The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IOMET PHARMA LTD.; MERCK SHARP & DOHME CORP.; COWLEY, Phillip, M.; WISE, Alan; BROWN, Thomas, J.; MCGOWAN, Meredeth, A.; ZHOU, Hua; HAN, Yongxin; (223 pag.)WO2017/7700; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

4-Methyl-l-(hydroxypropyl)-piperazine (0.27 g, 1.7 mmol) and KOH (freshly ground, 0.15 g, 2.7 mmol) were added sequentially to a solution of tert-butyl {[trans-4-({[(2- chloroquinolin-4-yl)carbonyl]amino}methyl)cyclohexyl]-methyl} carbamate (Example 35) (0.15 g, 0.35 mmol) in a mixture of THF (1 mL) and ACN (3 mL). The reaction mixture was heated at 500C for 12h and then DMSO was added and the mixture purified by HPLC (Standard method G). The fractions containing the title compound were partly concentrated in vacuo and then a saturated aq. solution OfNaHCO3 was added. DCM was added and the layers were separated. The organic layer was dried (phase separator) and concentrated in vacuo to give the title compound (90 mg, 47%). 1H NMR (400 MHz, CDCl3) delta 8.05 (d, IH), 7.82 (d, IH), 7.63 (t, IH), 7.40 (t, IH), 6.92 (s, IH), 6.16-6.02 (m, IH), 4.65-4.56 (m, IH), 4.52 (t, 2H), 3.37 (t, 2H), 2.97 (t, 2H), 2.62-2.36 (m, 10H), 2.28 (s, 3H), 2.09-1.96 (m, 2H), 1.91-1.75 (m, 4H), 1.63-1.52 (m, IH), 1.44 (s, 9H), 1.42-1.35 (m, IH), 1.13-0.85 (m, 4H); m/z (M+H)+ 554.1.

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2009/82346; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.67455-41-8,4-(Piperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of 4-(piperazin-l-yl)aniline (348 mg, 1.968 mmol), (E)-methyl 3-(2-(2-chloropyrimidin-5-yl)vinyl)-5-methoxybenzoate (600 mg, 1.968 mmol) and TFA (672 mg, 5.904 mmol) in propan-2-ol (30 mL) was stirred at 150 C for 40 min under microwave. The resulting mixture was concentrated, basified with ammonia water, purified via ISCO (DCM/MeOH) to afford the title compound as a yellow solid (320 mg, 36.6% yield). MS (m/z): 446.3(M+H)+.

67455-41-8 4-(Piperazin-1-yl)aniline 422925, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; ZHANG, Weihan; LI, Jinshui; WO2014/139465; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

[0240] Example 23: Synthesis of 2-[Benzenesulfonyl-(2-chloro-5-trifluoromethyl-phenyl)- amino]-N-[4-(4-methyl-piperazin-l-yl)-benzyl]-acetamide. [0241] To a stirred mixture of 2-(N-(2-chloro-5-(trifluoromethyl)phenyl) phenylsulfonamido)acetic acid (40.3 mg, 0.10 mmol), l-ethyl-3-(3- dimethylaminopropyl)carbodiimide HCl (24.2 mg, 0.13 mmol), and hydroxybenzotriazole (17.6 mg, 0.13 mmol) in methylene chloride (1 mL) was added a solution of (4-(4-methylpiperazin-l- yl)phenyl)methanamine (20 mg, 0.10 mmol) in N,N-dimethylformamide: methylene chloride (0.1 mL : 1 mL). The resulting solution was stirred at room temperature for a week. The mixture was concentrated, purified on silica gel eluted with a gradient of methanol: methylene chloride from 0 : 1 to 1 : 9 to provide the title product (39.2 mg). lU NMR (300 MHz, CDC13): delta 7.64-7.56 (m, 3H), 7.50-7.41 (m, 4H), 7.15-7.12 (m, 1H), 7.11-7.04 (m, 2H), 6.97 (t, = 5.3 Hz, 1H), 6.85-6.78 (m, 2H), 4.30 (d, = 5.3 Hz, 2H), 4.13 (broad s, 2H), 3.18-3.10 (m, 4H), 2.56-2.46 (m, 4H), 2.29 (s, 3H); Calculated for C27H28C1F3N403S, 580.15; observed MS (ESI) (m/z) 581.2 (M + 1)+

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference£º
Patent; INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH; CUCONATI, Andrea; GUO, Haitao; BLOCK, Timothy M.; GUO, Ju-Tao; XU, Xiaodong; LU, Huagang; CAI, Dawei; WO2013/130703; (2013); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

Compound (e) (222.11 mg, 511.45 muiotaetaomicronIota, 1.5 eq.) was taken in a flask along with DMF as a solvent (approx. 1.5 mL per 1 mmol). (4-((4-methylpiperazin-l- yl)methyl)phenyl)methanamine (70 mg, 340.97 muiotaetaomicronIota, 1 eq.), HOBT (92.14 mg, 681.93 muiotatauiotaomicronIota, 2 eq.), and DIC (93.43 muIota_, 596.69 muiotaetaomicronIota, 1.75 eq.) were added respectively at room temperature and under N2. After 18 hours, the reaction was finished. The solution was quenched with water and then extracted with ethyl acetate. The organic layer was combined and dried with anhydrous MgS04 and concentrated in vacuo. The crude solid was purified through column chromatography using silica gel and eluent ethyl acetate and methanol (up to 2%). The product, 32, was obtained as a brown solid with 51% yield. (0153) FT-IR (Neat) : v (cm”1) = 2941, 2797, 1720, 1634, 1548, 1514, 1451, 1435, 1290, 1275, 1174, 1142, 1112; 1H-NMR (400 MHz, CDCI3) : delta ppm 7.98 (d, J = 9.1 Hz, 2H), 7.33 (s, 1H), 7.25 – 7.30 (m, 2H), 7.21 (d, J = 8.6 Hz, 2H), 6.89 (d, J = 8.6 Hz, 2H), 6.40 (t, J = 4.78 Hz, NH), 4.46 (d, J = 5.54 Hz, 2H), 3.91 (s, 3H), 3.33 (s, 3H), 3.18 – 3.24 (m, 4H), 2.55 – 2.62 (m, 4H), 2.36 (s, 3H) ; 13C-NMR (100 MHz, CDCI3) : delta 166.20, 159.32, 151.02, 144.67, 140.53, 136.40, 130.56, 129.23, 129.05, 127.84, 127.52, 127.33, 126.03 (2C), 116.11 (2C), 115.83 (2C), 55.01 (2C), 52.35 (2C), 48.87, 46.12, 43.76, 30.36; HRMS-ESI (m/z) : calcd. for C26H29BrN405S2 = 621.0763, found = 621.0828.

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference£º
Patent; KING’S COLLEGE LONDON; THURSTON, David Edwin; KHONDAKER, Mirazur Rahman; JAMSHIDI, Shirin; NAHAR, Kazi Sharmin; (77 pag.)WO2019/30538; (2019); A1;,
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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

General procedure: Method B: Oxalyl chloride (2 M in CH2Cl2) was added dropwiseto an ice-cooled solution of 2 in dry CH2Cl2 under an argon atmosphere. After 1 h, the ice-bath was removed and the reaction batch was stirred overnight at ambient temperature in an atmosphere of Ar. Subsequently the solvent was evaporated in vacuo and the crude acyl chloride was dissolved in dry DMF and added dropwise to a stirred suspension of amine and K2CO3 in dry DMF at 0 ¡ãC. The stirring was continued for 1 h and then at ambient temperature overnight. After 20 h the suspension was filtered, the solvent evaporated, the residue taken up in water and extracted with CH2Cl2. The organic layer was washed with 5percent aqueous NaHCO3 and brine.Then it was dried over anhydrous sodium sulfate, filtered and the solvent was evaporated in vacuo yielding the raw quinoline-4-carboxamides 9?11, which were further purified by column chromatography.

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hochegger, Patrick; Faist, Johanna; Seebacher, Werner; Saf, Robert; Maeser, Pascal; Kaiser, Marcel; Weis, Robert; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2251 – 2259;,
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350684-49-0, tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture of compound 10a-10e (3.24 mmol), compound 9(1.04 g, 3.4 mmol), Pd(OAc)2 (0.11 g, 0.5 mmol), Xantphos (0.28 g,0.5 mmol), and K3PO41.38 g, 6.48 mmolin DMF (8 mL) was heated 22 h at 125 C under argon followed by cooling to roomtemperature.The mixture was extracted with dichloromethane(20 mL x 3), the combined organic phase was washed with water(15mL x 2), dried over anhydrous Na2SO4 and concentrated toafford the crude product. The crude product was purified by columnchromatography to obtain compounds 11a-11e.

350684-49-0 tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate 2763355, apiperazines compound, is more and more widely used in various.

Reference£º
Article; Su, Yue; Li, Ridong; Ning, Xianling; Lin, Zhiqiang; Zhao, Xuyang; Zhou, Juntuo; Liu, Jia; Jin, Yan; Yin, Yuxin; European Journal of Medicinal Chemistry; vol. 177; (2019); p. 32 – 46;,
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5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-ethylpiperazine (3.40g, 29.8mmol), 80 K2CO3 (4.10g, 29.6mmol), and 93 TBAI (0.42g, 1.2mmol) were added to a solution of 82 5-bromo-2-nitropyridine (4.00g, 19.7mmol) in 83 DMSO (40mL). The mixture was heated at 80C for 16h, and the reaction was poured into ice water, and extracted with DCM. The combined organic layers were washed with water, dried over anhydrous Na2SO4, concentrated under a vacuum, and purified by silica gel column chromatography (DCM/MeOH=100:1-10:1) to obtain 94 1-ethyl-4-(6-nitropyridin-3-yl)piperazine (3.59g; yield, 56%) as a yellow solid. Pd/C (0.10g) was added to the 1-ethyl-4-(6-nitropyridin-3-yl)piperazine (0.90g, 3.8mmol) in EA/MeOH (9 mL/9mL) solution. The mixture was degassed by H2, stirred at RT under a H2 atmosphere for 2h, and filtered and concentrated under a vacuum to obtain INT-2 (720.0mg; yield, 92%) as an off-white solid. ESI-MS: m/z 207.2 [M+H]+.

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Article; Yin, Lei; Li, Heng; Liu, Wenjian; Yao, Zhenglin; Cheng, Zhenzhen; Zhang, Huabei; Zou, Hui; European Journal of Medicinal Chemistry; vol. 144; (2018); p. 1 – 28;,
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