Heterocyclic Building Blocks-piperazine

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,115761-79-0

To a solution of l-(2,4-difluorophenyl)piperazine [C.A.S. 115761-79-0] (0.088 g, 0.446 mmol) in DCE (2.14 ml) stirred at r.t. was added D88 (0.1 g, 0.371 mmol) and the resulting mixture was stirred at r.t. overnight. Then, acetic acid (0.037 ml) was added and stirred at r.t. for 4 h more. Then, sodium triacetoxy-borohydride (0.87 g, 0.409 mmol) was added and stirred at r.t. overnight. The reaction mixture was neutralized with Na2CO3 (aqueous sat. solution) and extracted with DCM. The organic layer was dried (Na2SO4) and concentrated in vacuo. The crude product thus obtained was purified by column chromatography (silica gel; DCM/EtOAc from 100/0 to 50/50 as eluent). The desired fractions were collected and concentrated in vacuo. The residue obtained was triturated with DIPE to yield final compound E224 (0.107 g, 64%).

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; ADDEX PHARMA S.A.; CID-NUNEZ, Jose, Maria; OEHLRlCH, Daniel; TRABANCO-SUAREZ, Andres, Avelino; TRESADERN, Gary, John; VEGA RAMIRO, Juan, Antonio; MACDONALD, Gregor, James; WO2010/130424; (2010); A1;,
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132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of tert-butyl 4-(3-hydroxypropyl)piperazine-l-carboxylate (7.0 g, 28.64 mmol) in THF (50 mL), was added triethylamine (8 mL, 57.29 mmol) at room temeperature. After 5 min, benzoyl chloride (3.66 mL, 31.51 mmol) was added dropwise at 0 C under inert atmoshphere. After addition, the resultant reaction mixture was stirred at room temperature for 1 h. After completion of reaction (monitored by TLC), the reaction was quenched with water (100 mL) and extracted with ethyl acetate (3 X 250 mL). The combined organic layer was dried over anhydrous sodium sulphate and concentrated – – under reduced pressure to afford 43 (7.8 g) as a off-white solid. *H NMR (400 MHz, CDC13): delta 8.06 – 8.00 (m, 2H), 7.59 – 7.52 (m, 1H), 7.48 – 7.40 (m, 2H), 4.38 (tj = 6.6 Hz, 2H), 3.50 – 3.39 (m, 4H), 2.53 (t, / = 7.3 Hz, 2H), 2.43 (br t, / = 4.9 Hz, 4H), 1.98 (quin, / = 6.8 Hz, 2H), 1.46 (s, 9H); LCMS (M+H) = m/z 349.7 [M+H+]; purity~83%., 132710-90-8

132710-90-8 1-Boc-4-(3-hydroxypropyl)piperazine 16217800, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; TOPADUR PHARMA AG; NAEF, Reto; TENOR, Hermann; (135 pag.)WO2017/85056; (2017); A1;,
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Piperazines – an overview | ScienceDirect Topics

502649-29-8, 1-Boc-3-Benzylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

502649-29-8, A solution of l-benzyl-2-methyl-lH-pyrrole-3-carboxylic acid (150 mg) , tert-butyl 3-benzylpiperazine-l-carboxylate(193 mg) , WSC-HCl (174 mg) , HOBt (139 mg) and DMF (10 ml) was stirred at room temperature for 12 hr. Then, the mixture was poured into a saturated aqueous sodium bicarbonate solution and extracted with ethyl acetate. The extract was washed successively with water and brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated in vacuo. The residue was subjected to silica gel column chromatography, and the fraction eluted with ethyl acetate-hexane (1:9 to 1:3) was concentrated in vacuo to give an amorphous solid (140 mg) . 110 mg of the resulting amorphous was dissolved in dichloromethane (2 ml), and TFA (2 ml) was added thereto. After stirring at room temperature for 2 hr,. the mixture was poured into a saturated aqueous sodium bicarbonate solution (50 ml) and extracted with ethyl acetate. The extract was washed with brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated in vacuo. The residue was subjected to silica gel column chromatography, and eluted with ethyl acetate-methanol (1:1). The target fraction was concentrated, and then the residue was dissolved in ethyl acetate. The mixture was acidified with a 4 N hydrogen chloride-ethyl acetate solution, and then concentrated in vacuo to give the desired product (45 mg) as an amorphous solid. MS (ESI+, m/e) 374 (M+l)

The synthetic route of 502649-29-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2007/94513; (2007); A2;,
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Piperazines – an overview | ScienceDirect Topics

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

28 grams of ulifloxacin dissolved at room temperatureIn a 14 ml volume ratio of 5:1 acetic acid in acetonitrile,Dissolve and filter at 10CThen add 16ml of 10M hydrochloric acid to the filtrate.And stirred at 10 C for 4 hours to complete the reaction.After filtration, the precipitate was collected and washed with acetonitrile and dried under vacuum at 20C.The collected crystals were dissolved in methanol,After heating and stirring, cool in an ice bath and stir to crystallize.Precipitated crystals were collected and vacuum dried at 20C.That is, ulifloxacin hydrochloride crystal A is obtained.

112984-60-8, As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; Zhaoke Pharmaceutical (Hefei) Co., Ltd.; Li Xiaoyi; Dai Xiangrong; Zhou Guanqun; (18 pag.)CN107501298; (2017); A;,
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55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

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

Reference：
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

182618-86-6, 1-Boc-4-(4-Nitrophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A. 4-(4-Amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester To a suspension of 1-fluoro-4-nitrobenzene (1.4 mL, 13 mmol) and potassium carbonate (2.5 g, 18 mmol) in DMSO (10 mL) was added 1-Boc-piperazine (2.75 g, 14.8 mmol). The mixture was stirred at 100 C. for 2 hours. After cooing down, the mixture was diluted with water (50 mL) and extracted with EtOAc (3*50 mL). The combined organic layers were washed with brine, dried with sodium sulfate (Na2SO4), and concentrated in vacuo to afford a yellow solid. Recrystallization from EtOAC/hexanes gave 4.0 g of 1-(4-Boc-piperazin-1-yl)-4-nitrobenzene, which was reduced via hydrogenation to give the title compound (purple solid, 3 g). 1H NMR (400 MHz, CDCl3) delta (ppm): 6.68 (d, J=8.8 Hz, 2H), 6.64 (d, J=8.8 Hz, 2H), 3.56 (t, J=5.0 Hz, 4H), 2.96 (t, J=5.0 Hz, 4H), 1.46 (s, 9H).

182618-86-6, 182618-86-6 1-Boc-4-(4-Nitrophenyl)piperazine 3380696, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Player, Mark R.; Huang, Hui; Hutta, Daniel A.; US2007/60577; (2007); 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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Diisopropylethylamine (156 mL, 894 mmol) was added to a stirred, room temperature mixture of 3-(2-Bromo-acetyl)-6-fluoro-2-methyl- benzonitrile (176 g, 688 mmol) and (i?)-4-N-Boc-2-hydroxymethyl-piperazine (149 g, 688 mmol) in THF (3500 mL) and the mixture was stirred at room temperature for 18 h. The reaction was diluted with 3 L EtOAc, washed 2x with 1500 mL 10%> w/w NaHC03 aqueous solution, dried over MgS04, filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80% EtOAc/Hexanes, linear gradient), to provide the title compound ., 278788-66-2

As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics

314741-39-4, (S)-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

EXAMPLE 9; f8aS)-7V-Biphenyl-2-yl-2-[^r°?s-2-f4-chlorophenyl)cvclopropyll-l,3- dioxohexahydroimidazo [ 1 ,5-al pyrazine-7( lHVcarboxamide ( Eta5); Step 1 : ferf-Butyl (8a61-l,3-dioxohexahydroimidazo[l,5-alphalpyrazine-7(lH)-carboxylate (Hl); To a stirred solution of l-tert-buty 3-methyl (35)-piperazine-l,3-dicarboxylate (AA3) (1.0 eq.) and 6 N aq. HCl sol. (1.0 eq.) in 1,4-dioxane (1 M) was added a sol. of KOCN (2.0 eq.) in H2O (2 M). The reaction mixture was stirred at RT for 2 h, then the organic solvent was removed under reduced pressure. The desired product precipitated from H2O: it was filtered off, washed with cold water and dried at the high vacuum pump. Mother liquors were extracted with EtOAc, the organic phase was washed with brine, dried (Na2SO4), filtered and concentrated to dryness. The crude product was purified by flash chromatography on silica gel eluting with 10-100% EtO Ac/petroleum ether to afford the desired product (Hl) as a white powder which was combined with the previously isolated precipitate. 1H-NMR (300 MHz, DMSO-de, 300K) delta10.95 (IH, bs), 4.15-4.00 (2H, m), 3.97-3.75 (2H, m), 2.97-2.67 (3H, m), 1.42 (9H, s). MS (ES)CnHi7N3O4 requires: 255, found: 256 (M+H)+., 314741-39-4

The synthetic route of 314741-39-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.; BRANCA, Danila; FERRIGNO, Federica; HERNANDO, Jose, Ignacio, Martin; JONES, Philip; KINZEL, Olaf; MALANCONA, Savina; MURAGLIA, Ester; PALUMBI, Maria, Cecilia; PESCATORE, Giovanna; SCARPELLI, Rita; WO2010/23480; (2010); 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

To a suspension of Example 1285A (0.091 g, 0.21 1 mmol) and l-(methylsulfonyl)piperazine hydrochloride (0.057 g, 0.284 mmol) in 1,4-dioxane (1 mL), N-ethyl-N-isopropylpropan-2-amine (0.2 mL, 1.145 mmol) was added. The mixture was stirred for 72 hours at room temperature. The solvent was removed and the product was purified by flash chromatography on silica gel (AnaLogix IntelliFlash) eluting with a gradient of 0-50% ethyl acetate in heptanes to afford the title compound. MS (ESI+) m/z: 40.3.8 (M+H)+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference：
Patent; ABBVIE INC.; ABBVIE PHARMACEUTICAL TRADING (SHANGHAI) CO., LTD.; TONG, Yunsong; BRUNCKO, Milan; CLARK, Richard F.; CURTIN, Michael L.; FLORJANCIC, Alan S.; FREY, Robin R.; GONG, Jianchun; HANSEN, Todd M.; JI, Zhiqin; LAI, Chunqiu; MASTRACCHIO, Anthony; MICHAELIDES, Michael; MIYASHIRO, Juliem; RISI, Roberto M.; SONG, Xiaohong; TAO, Zhi-fu; WOODS, Keith W.; ZHU, Guidong; PENNING, Thomas; SOUERS, Andrew; GOSWAMI, Rajeev; IQUTURI, Omprakash Reddy; DABBEERU, Madhu Babu; WO2014/139328; (2014); 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.5521-38-0,2-(4-(4-Nitrophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

REFERENCE EXAMPLE 19b 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol. 2-[4-(4-amino-phenyl)-piperazin-1-yl]-ethanol is prepared by catalytic hydrogenation of 2[4-(4-nitrophenyl)piperazine-1-yl]-ethanol (prepared as in Reference Example 19a) as described in Reference Example 13b, 5521-38-0

The synthetic route of 5521-38-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chapdelaine, Marc; Davenport, Timothy; Haeberlein, Markus; Horchler, Carey; McCauley, John; Pierson, Edward; Sohn, Daniel; US2004/87575; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics