Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 80; 4-{2-[4-(4-Mcthancsulfonylphcnyl)pipcrazin-l-yl]-2-oxocthyl}pipcridinc-l- carboxylic acid ferf-butyl ester; To a solution of l-(4-methanesulfonylphenyl)piperazine (0.22 g, 0.91 mmol), 4-carboxy methylpiperidine-1-carboxylic acid tert-butyl ester (0.20 g, 0.80 mmol), HOBT.H2O (0.14 g, 0.91 mmol) and DIPEA (0.47 mL, 2.72 mmol) in DMF (5mL) was added EDCI (0.19 g, 0.99 mmol) and the mixture was stirred for 18h. The solvent was removed under vacuum and the resulting residue was partitioned between EtOAc and saturated NaHCO3 solution. The aqueous phase was re-extracted with EtOAc, the organic extracts were combined, washed with brine, dried (MgSO4) and adsorbed onto SiO2. The adsorbed sample was purified by flash chromatography eluting with 50:50 EtOAc:hexane to afford the title compound: RT = 3.26 min; m/z (ES+) = 466.33 [M+H]+., 187669-60-9

The synthetic route of 187669-60-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-31-7,1-Ethylpiperazine-2,3-dione,as a common compound, the synthetic route is as follows.

To Boc-Asp-OBzl 5 g (15.5 mmol) in dichloromethane (50 mL) was added triethylamine 6.43 mL (46.4 mmol), followed by HATU 7 g (18.6 mmol) and the mixture was stirred at RT for 30 min.1-Ethylpiperazine-2,3-dione 2.6 g (18.6 mmol) was added to the reaction in one portion, stirred at RT for 1 h and diluted with dichloromethane. The solution was washed with water/brine, dried over sodium sulfate, concentrated and purified using silica gel chromatography (70-80% ethyl acetate/hexanes) to give the desired compound, 5.64 g. ESI-MS m/z 448 (MH)+.

59702-31-7, The synthetic route of 59702-31-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VENATORX PHARMACEUTICALS, INC.; BURNS, Christopher J.; DAIGLE, Denis; CHU, Guo-Hua; HAMRICK, Jodie; BOYD, Steven A.; ZULLI, Allison L.; MESAROS, Eugen F.; CONDON, Stephen M.; TROUT, Robert E. Lee; MYERS, Cullen L.; XU, Zhenrong; (327 pag.)WO2019/226931; (2019); A1;,
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278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (prepared as described above for I-17A and I-17B, Method1, Steps A-C) (4.80 g, 27.1 mmol) and (R)-4-N-BOC-2-hydroxymethyl-piperazine (commercially available, e.g. fromAcesys Pharmatech, catalog A1612R; and also described in J. Org. Chem, 2007, 72(22), p. 8591-8592) (8.79g.40.6 mmol) were suspended in EtOH (30mL) and heated in a microwave apparatus at 150 C for 1 h. The reactionmixture was cooled and evaporated to dryness. The residue was purified by chromatography through a 330 g ISCORedi-sep column eluting with ethyl acetate to 5% MeOH/ ethyl acetate gradient to yield the title compound. LC-MS:M+1 = 394;

278788-66-2, 278788-66-2 (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820286, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
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118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-hutyl 4-aminopiperazine-l-carboxylate (0.200 g, 0.99 mmol, 1.0 equiv) in DMF (05 mL) was added HATU (0.753 g, 1.98 mmol, 2.0 equiv) at RT and stirred for 10 minutes. Then 6-chloroquinoline-2-carboxylic acid (0.206 g, 0.99 mmol, 1.0 equiv) was added followed by the addition of DIPEA (0.6 mL, 2.97 mmol, 3.0 equiv). The resulting reaction mixture was allowed to stir at RT for overnight. Product formation was confirmed by LCMS The reaction mixture was diluted with water (50 mL) and extracted with EtOAc (50 mL * 2). The combined organic layer was washed with water (30mL x 3), brine solution (30 ml, c 2), dried over anhydrous sodium sulfate and concentrated under reduced pressure, to obtain tert-butyl 4-(6-chloroquinoline-2-carboxamido)piperazine-l-carboxylate (0.140 g, 36 % Yield) as a brown solid. LCMS 390 ] M 1 1 | : NMR (400MHz, DMSO-de) d 9.95 (br. s., 1 H), 8.53 (d, ./ 8.3 Hz, 1 H), 8.24 (br. s., 1 H), 8.15 (d, J= 5.3 Hz, 2 H), 7.88 (d, J = 7.5 Hz, 1 H), 3 45 (br. s., 4 H), 2.90 (d, J= 1 1.0 Hz, 4 H), 1.42 (s, 9 H).

118753-66-5, The synthetic route of 118753-66-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRAXIS BIOTECH LLC; DELGADO OYARZO, Luz Marina; URETA DIAZ, Gonzalo Andres; PUJALA, Brahmam; PANPATIL, Dayanand; BERNALES, Sebastian; CHAKRAVARTY, Sarvajit; (0 pag.)WO2019/236710; (2019); A1;,
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55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

55276-43-2, (S)-Epichlorohydrin (48.0 mL, 0.612 mol) was added to a stirred solution of piperazine N-methylsulfonamide (87.3 g, 0.532 mol) in ethanol (1.33 L) at room temperature. The reaction mixture was stirred for 18 h and the white solid precipitate which formed was collected by filtration and washed with ethanol to afford (S)-1-chloro-3-(4-methylsulfonyl-1-piperazinyl)-2-propanol (107.76 g) as a white solid which was used without further purification. (m/z): [M+H]+ calcd for C8H17ClN2O3S, 257.07; found, 257.2. 1H-NMR (DMSO): delta (ppm) 2.37 (dd, 1H), 2.45 (dd, 1H), 2.50-2.58 (m, 4H), 2.86 (s, 3H), 3.09 (m, 4H), 3.55 (dd, 1H), 3.65 (dd, 1H), 3.84 (m, 1H), 5.09 (d, 1H).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference£º
Patent; THERAVANCE, INC.; US2006/100426; (2006); A1;,
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Piperazines – an overview | ScienceDirect Topics

611225-86-6, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

611225-86-6, 104 mg (0.35 mMol) triphosgene are ^j-n’ ^ dissolved in13 ml ice-cooled CH2CI2. ^-/ ~~” Then a solution of 230 mg (1.05mMol) 4-(4-ethylpiperazin-1-O Hylmethyl)~aniline and 209 i (1.50 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 3 additional minutes, the mixture is warmed up to rt by a water bath and then a solution of 1.0 mMol 5-(6-chloro-pyrimidin-4-yioxy)-2,3-dihydro-1H-indole (Step 14.1) and 139 jll. (1.00 mMol) Et3N in 6 ml CH2CI2 is added during 8 min. After 2 h at rt, the mixture is diluted with sat. Na2C03 solution / water 1:1 and EtOAc, the aqueous phase separated off and extracted twice with EtOAc. The organic layers are washed with water and brine, dried (Na2S04) and concentrated. Crystallization from DIPE gives the title compound: MS: [M+1]+= 493 / 495; TLC(CH2CI2/MeOH/NH3conc- 90:10:1): Rf = 0.24; HPLC: et_ = 10.5.

The synthetic route of 611225-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/34833; (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.112257-12-2,tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-(2-bromoacetyl)piperazine-1-carboxylate (9.77 mmol, 1 eq.) in methanol (26 ml) at 0C. The reaction vial was sealed and the mixture stirred vigorously overnight at room temperature. The solvent was subsequently evaporated, the residue dissolved in hydrogen chloride (aqueous soln., 0.1 N, 100 ml) and extracted with ethyl acetate (3 x 100 ml). The pH of the recovered aqueous layer was adjusted to 10 by addition of sodium hydroxide (aqueous soln., 1 N), then the organics extracted with ethyl acetate (3 x 100 ml). The combined organic layers were dried over magnesium sulfate, filtered and the solvent evaporated under vacuum to give a light yellow crude product. Further trituration in diethyl ether conducted to the desired amine as a white solid used for the next step without additional purification. C11 H21N3O3; yield 58%; white solid; m.p. 159-160 C; M = 243.30 g/mol; IR (ATR): v = 2974 (w), 1675 (s), 1627 (s), 1417 (m), 1360 (m), 1235 (m), 1172 (m), 1123 (m), 990 (m), 759 (m) cm – ; H NMR (250 MHz, CDCI 3) delta 3.71-3.41 (m, 10H), 1.46 (s, 9H); C NMR (63 MHz, CDCI 3) delta 169.5 (C q), 154.6 (C q), 80.5 (C q), 50.4 (CH 2), 44.6 (2CH 2), 41.7 (2CH 2); HRMS: calcd. for CHH21 3O3 244.1661 , found. 244.1657;, 112257-12-2

The synthetic route of 112257-12-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTON UNIVERSITY; GRIFFIN, Martin; RATHBONE, Daniel; BADARAU, Leonas Eduard; WO2014/57266; (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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

A solution of (i?)-3-(6-(2- fluorophenyl)-5,6-dihydrobenzo[h]quinazolin-2-ylamino)phenethyl methanesulfonate (5.37 g, 11.00 mmol), l-(2-methoxyethyl)piperazine (3.32 niL, 22.34 mmol) and triethylamine (1.5 niL, 11.17 mmol) in JV,JV-dimethylacetamide (30 mL) was heated at 90 0C for 20 h. After cooling to room temperature, water (200 mL) was added while stirring. The suspension was stirred for 15 min. and filtered. Solid was taken into dichloromethane (200 mL), dried over sodium sulfate and concentrated. Product was purified by flash column chromatography on silica gel (120 g silica gel column, 0-10% 7N NH3 in methanol-dichloromethane, over 80 min.) to afford the title compound as a yellow solid (5.50 g, 93% yield). 1H-NMR (DMSO- d6): delta 9.53 (s, 1 H), 8.37-8.34 (m, 1 H), 8.33 (s, 1 H), 7.81 (s, 1 H), 7.62-7.60 (m, 1 H), 7.51- 7.46 (m, 2 H), 7.30-7.19 (m, 3 H), 7.08-7.02 (m, 2 H), 6.82-6.79 (m, 2 H), 4.67 (t, J= 7.2 Hz, 1 H), 3.41 (t, J= 5.6 Hz, 2 H), 3.22-3.08 (m, 2 H), 3.33 (s, 3 H), 2.74-2.70 (m, 2 H), 2.59- 2.42 (m, 12 H). LCMS m/e 539 [M+H].

13484-40-7, As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference£º
Patent; ARQULE, INC.; ALI, Syed, M.; ASHWELL, Mark; TANDON, Manish; YANG, Rui-yang; LIU, Yanbin; VENSEL, David; EATHIRAJ, Sudharshan; PALMA, Rocio; LAPIERRE, Jean-marc; WESTLUND, Neil; WU, Hui; NAMDEV, Nivedita; KELLEHER, Eoin; KELLEHER, Eugene; WO2010/78421; (2010); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, A solution of N [5-bromo-7- (3-methoxyprop-1-yn-1-yl)-1, 3-benzodioxol-4-yl]-7- (3- chloropropoxy) -6-methoxyquinazolin-4-amine (0.14g, 0. 26mmol), 1-methylpiperazin-2-one (0. 15g, 1. 3mmol) and triethylamine (0. 18ml, 1. 3mmol) in 2-methoxy ethanol (2ml) was heated at 80 C overnight and then further heated at 100 C for 24 hours. The solvent was evaporated under reduced pressure and the residue was partitioned between dichloromethane and water. The organic layer was separated, dried over magnesium sulfate and evaporated under reduced pressure. Flash chromatography on silica eluting with increasingly polar solutions of methanol (0-8percent) in dichloromethane followed by trituration with diethyl ether gave the product as a cream coloured solid (0. 042g). NMR Spectrum: (d6DMSO) 1.93-2. 03 (m, 2H), 2.50-2. 57 (m, 2H), 2.63-2. 70 (m, 2H), 2.82 (s, 3H), 3.01 (s, 2H), 3.25-3. 29 (m, 2H), 3.35 (s, 3H), 3.94 (s, 3H), 4.16-4. 22 (m, 2H), 4.37 (s, 2H), 6.16 (s, 2H), 7.19 (s, 1H), 7.30 (s, 1H), 7.84 (s, 1H), 8.32 (s, 1H), 9.50 (s, 1H). Mass Spectrum: M+H+ 612/614.

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/4732; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

197638-83-8, 1-Boc-4-(4-Formylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

te/f-Butyl 4-(4-(6-chloro-7-(4-(2-oxo-2-(thiazol-2-ylamino)ethyl)piperazin-1-yl)-3H- imidazo[4,5-iotab]pyridin-2-yl)phenyl)piperazine-1-carboxylate To a mixture of 2-[4-(2-amino-5-chloro-3-nitro-pyridin-4-yl)-piperazin-1-yl]-lambda/-thiazol-2- yl-acetamide (0.048 g, 0.12 mmol) and EtOH (5 ml_) was added tert-butyl 4-(4- formylphenyl)piperazine-1-carboxylate (0.045 g, 0.16 mmol) followed by a freshly prepared aqueous solution of Na2S2O4 (1 M; 0.48 ml_, 0.48 mmol). The reaction mixture was stirred at 80 0C for 18 h, then allowed to cool to room temperature and concentrated in vacuo. The residue was absorbed on silica gel, the free-running powder was placed on a 10 g isolute silica column, and elution with a gradient of methanol (0 to 3%) in ethyl acetate / dichloromethane (v:v; 1 :1 ) afforded the title compound as a pale yellow solid (0.040 g, 53%).1 H-NMR (500 MHz, DMSO-d6) 1.43 (s, 9H, C(CHs)3), 2.77 (br t, 4H), 3.26 (br t obscured by water peak), 3.48 (br t, 4H), and 3.71 (br s, 4H) (piperazine N(CH2)2), 3.40 (s, 2H, NCH2CONH), 7.06 (d, J = 9.3 Hz, 2H) and 8.04 (d, J= 8.2Hz, 2H) (2,6-C6H4 and 3,5-C6H4), 7.23 (d, J = 3.5 Hz, 1 H) and 7.49 (d, J = 3.5 Hz, 1H), (thiazole 4-H, 5-H), 8.05 (s, 1 H, imidazo[4,5-]pyridine 5-H)1 11.87 (br s, 1H, CONH), 13.18 (br s, 1 H, imidazo[4,5-197638-83-8

197638-83-8 1-Boc-4-(4-Formylphenyl)piperazine 2795509, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics