Heterocyclic Building Blocks-piperazine

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

To a mixture of piperazine-2-one (1.037 g, 10.4 mmol) in 52 mL of CH2Cl2, was added BOC20 (2.5 g, 11.4 mmol). The reaction became homogeneous after 3 hours when the starting material was completely consumed. The reaction was diluted with CH2Cl2 and the organic layer was washed with water. The solvent was removed in vacuo to yield quantitative amount of product 33 as a white solid. ?H NMR (300 MHz, CDCl3) 8 1.48 (s, 9H), 3.35-3.44 (m, 2H), 3.64 (t, 2H, J= 5 Hz), 4.10 (s, 2H), 6.41 (br s, 1H).

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GILEAD SCIENCES, INC.; CAI, Zhenhong, R.; CHEN, Xiaowu; FARDIS, Maria; JABRI, Salman, Y.; JIN, Haolun; KIM, Choung, U.; METOBO, Sanuel, E.; MISH, Michael, R.; PASTOR, Richard, M.; WO2005/117904; (2005); A2;,
Piperazine – Wikipedia
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109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

109-07-9, 2-Methylpiperazine (3.19 g) was added at 0°C to 2-(tert-butylcarbonyloxyimino)-2-phenylacetonitrile (7.87 g) in tetrahydrofuran (100 mL), and the mixture was stirred for 2 hours. The reaction solvent was removed under reduced pressure, and the residue was purified through silica gel column chromatography (chloroform – 7N ammonia/methanol), to thereby give the title compound as an oil (5.70 g, 89percent). 1H-NMR(400MHz,CDCl3)delta:1.05(3H,d,J=6.4Hz), 1.46(9H,s), 2.40 (1H,br), 2.65-2.84(3H,m), 2.90-3.00 (1H,br), 3.94(2H,br). MS(ESI)m/z:201(M+H)+.

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1621537; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Description 4; Methyl-3-(4-{[(3R,5S)-3,5-dimethyl-1-piperazinyl]methyl}phenyl)-2-pyridine carboxylate (D4); To a solution of D3 (260 mg, 1.08 mmol) in dry DCM (30 ml) was added (2R,6S)-dimethylpiperazine (185 mg, 1.62 mmol) at 0° C. under argon. The reaction mixture was then warmed to 25° C. and stirred for 1 h. After this period, sodium (triacetoxy)borohydride (343 mg, 1.62 mmol) was added portionwise and the reaction mixture stirred at 25° C. under argon for 18 h. The reaction was then quenched with saturated NaHCO3 solution (50 ml) and extracted with DCM (3.x.50 ml). The organic layers were combined, washed with water, dried (Na2SO4) and concentrated in vacuo. The crude oil was purified by column chromatography on silica eluting with a 0-10percent [(9:1)MeOH:ammonia]/EtOAc gradient to afford the title compound (213 mg, 58percent). deltaH (CDCl3, 250 MHz) 1.04 (6H, d), 1.64 (2H, t), 2.79 (2H, m), 2.89-2.99 (2H, m), 3.54 (2H, s), 3.79 (3H, s), 7.28-7.50 (5H, m), 7.77 (1H, dd), 8.66 (1H, dd). MS (ES): C20H25N3O2 requires 339. found 340 (MH+), 21655-48-1

The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Glaxo Group Limited; US2008/312209; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

150407-69-5, (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

150407-69-5, A mixture of (S)- 1 -((benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine- 2- carboxylic acid (500 mg, 1.372 mmol, 1.0 eq), 6-chloro-pyridin-2-ylamine (265 mg, 2.058 mmol, 1.5 eq), and EDCI (790 mg, 4.116 mmol, 3.0 eq) in pyridine (25 mL) was stirred at r.t. for 6 h. The reaction was monitored by LC-MS and TLC. The mixture was concentrated and the resulting residue was purified by chromatography on silica gel column (PE/EA = 5/1, v/v) to give the crude (S)- 1-b enzyl 4-tert-butyl 2-((6-chloropyridin-2-yl)carbamoyl)piperazine- 1,4-dicarboxylate (400 mg, 61%) as a white solid.

As the paragraph descriping shows that 150407-69-5 is playing an increasingly important role.

Reference：
Patent; LIFESCI PHAMACEUTICALS, INC.; MCDONALD, Andrew; QIAN, Shawn; (241 pag.)WO2017/98328; (2017); 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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

N-tert-butyloxycarbonyl-N’-(4-aminophenyl)-piperazine (138 mg) and 5-chloro-2-methoxyphenyl isocyanate (138 mg) were dissolved in anhydrous tetrahydrofuran (5 mL) and stirred at room temperature for 14.5 hours. After methanol was added to the reaction solution, the mixed solution was concentrated. The obtained solid was vigorously stirred in hexane/isopropyl ether (5:1), collected by filtration and dried under reduced pressure, and 206 mg (89%) of the title compound was obtained as a pale pink crystal. 1H-NMR spectrum (400MHz,DMSO-d6):delta(ppm)=9.15(1H, s), 8.27(1H, s), 8.21(1H, d, J=2.3Hz), 7.29(2H, d, J=9.0Hz), 7.00(1H, d, J=9.0Hz), 6.94(1H, dd, J=8.6 and 2.8Hz), 6.95(2H, d, J=2.8Hz), 3.87(3H, s), 3.44(4H, t, J=4.9Hz), 2.99(4H, t, J=5.1Hz), 1.42(9H, s). MS(FAB) m/z:461 (M + H)+. Melting point: 205C.

170911-92-9, 170911-92-9 tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate 11011301, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Sankyo Company, Limited; EP1764360; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

EtOH (250 mL) was added to a mixture of 5-bromo-2-chloropyrimidine (5 g, 25.8 mmol) and (R)-2- methylpiperazine (2.74 g, 27.4 mmol) followed by the addition of TEA (9.98 mL, 71.6 mmol) under a nitrogen atmosphere. The reaction was stirred at about 78 °C for about 8 h. The reaction was cooled to about rt and concentrated under reduced pressure. The residue was triturated with 20: 1 DCM/MeOH (150 mL) and stirred for 30 min. The solid was collected by filtration and dried under vacuum to afford title compound (5 g, 75 percent) as the HC1 salt; lH NMR (400MHz, DMSO-t/6) delta 9.66 (br. s., 2H), 8.53 (s, 2H), 4.53 (d, J=13.7 Hz, 2H), 3.34 – 3.20 (m, 3H), 3.18 – 3.08 (m, 1H), 3.03 – 2.92 (m, 1H), 1.29 (d, J=6.2 Hz, 3H)

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference：
Patent; ABBVIE INC.; BREINLINGER, Eric, C.; COX, Phil, B.; DAANEN, Jerome; DIETRICH, Justin; DJURIC, Stevan; DOMBROWSKI, Amanda, W.; FRANK, Kristine, E.; FRIEDMAN, Michael, M.; GOMTSYAN, Arthur; LI, Huan-Qui; LONGENECKER, Kenton; OSUMA, Augustine; ROWLEY, Ann, Marie; SCHMIDT, Robert; VASUDEVAN, Anil; WILSON, Noel; (378 pag.)WO2016/168641; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

1-(4-Trifluormethyl-phenyl)-piperazine (283 mg, 1 mmol) and triethylamine (220 muL, 2 mmol) were dissolved in dichloromethane (8 mL). Chloroacetyl chloride (110 muL, 1 mmol) was then slowly added under stirring. After stirring for an additional 10 min at room temperature, the mixture was diluted with dichloromethane (10 mL), washed with water (10 mL), and washed with saturated aqueous sodium hydrogencarbonate (10 mL). The organic layer was collected, dried over magnesium sulfate, filtered, and concentrated under vacuum. The desired product was isolated as a light yellow oil (292 mg, 95% yield).

30459-17-7, The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; INTERVET INTERNATIONAL B.V.; WO2009/77527; (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.57184-25-5,1-(Cyclopropylmethyl)piperazine,as a common compound, the synthetic route is as follows.,57184-25-5

The cis-isomer may be prepared analogously. cis- and trans-4-(4-cyclopropylmethyl-piperazin-1-yl)-cyclohexylamine 9.8 g (33.4 mmol) of 4-dibenzylcyclohexanone is dissolved in 100 mL dichloromethane and stirred with 5.6 g (40 mmol) of N-cyclopropylmethylpiperazine and 8.5 g (40 mmol) of NaBH(OAc)3 for 12 h at RT. Then the mixture is combined with water and potassium carbonate, the org. phase is separated off and dried and the solvent is eliminated in vacuo. The residue is purified on a silica gel column (approx. 50 mL silica gel, approx. 3 L ethyl acetate 95/methanol 5+0.25% conc. ammonia). The desired fractions are evaporated down in vacuo. The faster eluding cis compound crystallises from ethyl acetate. The trans compound is crystallized from ethanol+conc. HCl. Yield: 8.5 g (61%) cis-isomer and 2.2 g (13%) trans-isomer.

The synthetic route of 57184-25-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Boehringer Ingelheim International GmbH; US2006/35903; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5521-39-1, 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5521-39-1, To a stirred solution of 21 3-(2,6-dichlorophenyl)-7-(methylthio)-2,3-dihydro-4H-pyrimido[5,4-e][1,3]oxazin-4-one (0.2 g, 0.58 mmol, 1.0 eq) in 5 mL 24 toluene 25 m-CPBA (0.251 g, 1.46 mmol, 2.5 eq) was added under stirring and resulting mixture was allowed to stir at rt for 30 min. Further, 604 2-(4-(4-aminophenyl)piperazin-1-yl)ethan-1-ol (0.129 g, 0.58 mmol, 1.0 eq) and 27 DIPEA (0.302 g, 2.33 mmol, 4 eq) were added and the reaction was allowed to stir at rt for 12 h. The reaction was monitored by LCMS. After completion reaction was quenched with 7 water and extracted with ethyl acetate (5 mL×3). The combined organic layer was washed with brine solution (10 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford crude product which was purified by flash chromatography (MeOH: CH2Cl2 1-10%) to afford 607 3-(2,6-dichlorophenyl)-7-((4-(4-(2-hydroxyethyl)piperazin-1-yl)phenyl)amino)-2,3-dihydro-4H-pyrimido[5,4-e][1,3]oxazin-4-one (0.008 g, 10%) as white solid. (0628) LCMS: 515 [M+1]+ (0629) 1H NMR (400 MHz, DMSO-d6): delta 10.18 (s, 1H), 8.78 (s, 1H), 8.20 (s, 1H), 7.65 (d, J=8.33 Hz, 2H), 7.51 (d, J=7.45 Hz, 2H), 6.92 (d, J=8.33 Hz, 2H), 5.71 (br s, 2H), 4.43 (br s, 2H), 3.53 (d, J=6.14 Hz, 2H), 3.17 (d, J=5.26 Hz, 1H), 3.09 (br s, 1H), 1.23 (br s, 1H), 1.16 (d, J=10.09 Hz, 1H).

5521-39-1 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol 767100, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (2019); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (250 mg, 1.25 mmol) , cyclopropanecarboxylic acid (130 mg, 1.50 mmol) , EDCI (480 mg, 2.50 mmol) and HOAT (254 mg, 1.87 mmol) in DCM (10 mL) was stirred at 0 , and DIPEA (0.65 mL, 3.74 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 10 h and washed with water (10 mL × 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4- (cyclopropanecarbonyl) -3-methylpiperazine-1-carboxylate as colorless oil (310 mg, 93) .1H NMR (400 MHz, CDCl3) : delta ppm 4.24-4.50 (m, 1H) , 3.78-4.07 (m, 2H) , 2.90-3.41 (m, 3H) , 2.81 (s, 6H) , 1.50 (s, 9H) , 1.12-1.36 (m, 4H) , 0.96-1.05 (m, 2H) , 0.74-0.82 (m, 2H) and MS-ESI: m/z 213.10 [M-55] +.

163765-44-4, The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference：
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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics