Heterocyclic Building Blocks-piperazine

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 11 An experiment was carried out as described for Example 9, except that 45.55 g of 1-butanol and 4.61 g of water (water content 9.2 wt%) were used instead of 50.00 g of 1-butanol. As a result, the conversion of 2-methylpiperazine was 94.3%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 85.8% (reaction yield 80.9%).Comparative Example 8 An experiment was carried out as described for Example 9, except that 37.56 g of 1-butanol and 12.67 g of water (water content 25.2 wt%) were used instead of 50.00 g of 1-butanol. As a result, the conversion of 2-methylpiperazine was 81.6%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 70.9% (reaction yield 57.9%).Comparative Example 9 An experiment was carried out as described for Example 9, except that 25.00 g of 1-butanol and 25.00 g of water (water content 50.0 wt%) were used instead of 50.00 g of 1-butanol. As a result, the conversion of 2-methylpiperazine was 81.2%, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 41.8% (reaction yield 33.9%).

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
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129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (500 mg, 2.04 mmol) and an ammonia methanol solution (7 M, 10mL) in a 100 mL of sealing tube was stirred at 60 for 12 h and concentratedto give the title compound as a white solid (450 mg, 95) . 1H NMR (400 MHz, CD3OD): delta ppm 4.01-4.08 (m, 1H) , 3.65-3.88 (m, 1H) , 3.31-3.38 (m, 1H) , 2.90-3.12(m, 3H) , 2.73-2.82 (m, 1H) , 1.47 (s, 9H) and MS-ESI: m/z 130.20 [M+H-100] +.

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various.

Reference£º
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;,
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154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-(2-fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (29.1 g, 89.4 mmol) in MeOH (150 mL) and DCM (10 mL) mixture was added Raney Ni (5.5 g) and the Parr shaker was charged with hydrogen to 50 psi for 1 h. The initial yellow solution became clear and the content was filtered, washed with MeOH and the combined filtrate evaporated to dryness. The residue was dissolved in dry dioxane (20 mL) and a 4M HC1 solution in dioxane (30 mL) was added. The solution was warmed to 45 C in a water bath and stirred vigorously overnight producing a white precipitate. After filtering and washing with cold dioxane and diethyl ether and drying in vacuo, 23.1 g (96%) of the title compound was isolated as a white solid. N1HMR (400 MHz, DMSO-4 delta (ppm): 10.5 (br. s., 1 H), 9.63 (br. s., 2H), 8.0 (br. s., 2H), 7.29 (d, J = 12.6 Hz, 1 H), 7.20 – 7.19 (m, 2H), 3.24 (d, J = 4.8 Hz, 4H), 3.19 (br. s., 4H). 19F NMR (376 MHz, DMSO-d6) delta (ppm): – 120.36 (dd, J = 13.6, 7.2 Hz, IF).

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference£º
Patent; ANACOR PHARMACEUTICALS, INC.; HERNANDEZ, Vincent, S.; DING, Charles; PLATTNER, Jacob; ALLEY, Michael, Richard Kevin; ZHANG, Yong-Kang; ZHANG, Yanchen; WO2011/37731; (2011); 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.

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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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.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.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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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.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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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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