Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture of the 2- (5-amino-2- (furan-2-yl) -8H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-8-yl) -4-methylpentanoic acid (35.5 mg, 0.1 mmol) , 1- (2, 4-difluorophenyl) piperazine (19.8 mg, 0.1 mmol) , HATU (46 mg, 0.12 mmol) and DIPEA (25.8 mg, 0.2 mmol) in DMF (3 mL) was stirred overnight. The reaction mixture was poured into H2O (15 mL) and extracted with EtOAc (20 mL x 3) . The combined organic layers were washed with brine, dried over Na2SO4, concentrated and purified by column chromatography (petroleum ether/EtOAc = 10: 1 3: 1) to give the target compound (20 mg, 37.3%) .1H NMR (400 MHz, DMSO-d6) delta 8.78 (s, 1H) , 7.94 (s, 1H) , 7.65 (s, 2H) , 7.25 -7.17 (m, 2H) , 7.03 (m, 2H) , 6.74 (dd, J = 3.2, 1.6 Hz, 1H) , 5.69 (m, 1H) , 3.76 (s, 2H) , 3.64 (m, 2H) , 3.05-2.93 (m, 2H) , 2.91 -2.79 (m, 2H) , 2.28 -2.17 (m, 1H) , 1.89 -1.78 (m, 1H) , 1.35 (m, 1H) , 0.97 (d, J = 6.4 Hz, 3H) , 0.88 (d, J = 6.4 Hz, 3H) ppm. MS: M/e 536 (M+1)+., 115761-79-0

The synthetic route of 115761-79-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BEIGENE, LTD.; ZHANG, Guoliang; SUN, Hanzi; ZHOU, Changyou; (253 pag.)WO2020/20097; (2020); 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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of 4-(3-(4-cyanophenyl)imidazo[l,2-a]pyridin-6-yl)benzoic acid (100 mg, 0.294 mmol) in DMF (1.5 mL) were added HATU (168 mg, 0.441 mmol), N-methyl morpholine (129 iL, 1.18 mmol) and 1-benzoylpiperazine (67 mg, 0.441 mmol). The reaction mixture was stirred at room temperature under inert atmosphere for 18 h then, was diluted with water (15 mL) and extracted with EtOAc (3×30 mL). The combined organic layer was dried over Na2S04 and was concentrated under reduced pressure. The residue was purified by column chromatography (silica gel, eluent CHCl3/MeOH 92:8) to afford 4-(6-(4- (4-benzoylpiperazine- 1 -carbonyl)phenyl)imidazo[ 1 ,2-a]pyridin-3 -yl)benzonitrile (75 mg, 50%, AUC HPLC 99%) as a white solid. NMR (400 MHz, DMSO- 6) delta 8.75 (s, 1H), 7.95-7.89 (m, 4H), 7.88 (s, 1H), 7.82-7.55 (m, 4H), 7.59 (d, J= 8.0 Hz, 2H), 7.63-7.43 (m, 5H), 4.00-3.40 (m, 8H); 13C NMR (100 MHz, CD3OD): delta 172.90, 172.34, 147.49, 140.29, 136.50, 136.11, 134.87, 134.76, 134.43, 131.43, 129.87, 129.48, 129.22, 128.63, 128.59, 128.21, 127.85, 126.61, 122.92, 119.55, 118.51, 112.76; MS (ESI) m/z 512 [C32H25N50 + H]+..

13754-38-6, 13754-38-6 1-Benzoylpiperazine 762654, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH; NACRO, Kassoum; DURAISWAMY, Athisayamani, Jeyaraj; CHENNAMANENI, Lohitha, Rao; WO2013/147711; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1: Compound 250-2 (1.14 g, 10 mmol) was added into a solution of compound 250-1 (1.71 g, 10 mmol) and K2CO3 (2.78 g, 20 mmol) in DMF (20 mL), the reaction mixture was stirred at 110¡ãC for 2h, monitored by LCMS till completion. Then the mixture was poured into H2O, extracted with EtOAc, the organic phase was dried over anhydrous sodium sulfate, concentrated to give a crude product. The crude product was purified by silica gel column chromatography (PE:EtOAc=1:1) to deliver compound 250-3 (2.3 g, yield 92percent) as oil. MS ESI calcd for C13H19N3O2[M+H]+ 250, found 250., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference£º
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; WU, Hao; LIN, Jun; LI, Yunhui; WEI, Changqing; CHEN, Shuhui; LONG, Chaofeng; CHEN, Xiaoxin; LIU, Zhuowei; CHEN, Lijuan; (212 pag.)EP3124482; (2017); 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.

In a sealed tube, 7-fluoro-2-(2-methylimidazo [1 ,2-b]pyridazin-6-yl)-4H-pyrido [1,2- a]pyrimidin-4-one (Intermediate 1; 50 mg, 0.169 mmol), and (R)-2-methylpiperazine (68 mg, 0.677 mmol, 4.0 eq.) were stuffed in DMSO (2 mL) at 110C overnight. The solvent wasremoved under high vacuum. The residue was taken up in CH2C12 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2504 and concentrated in vacuo. The crude was purified by column chromatography (5i02, CH2C12/MeOH=95/5 to 90/10) to afford the title product (48 mg, 75%) as a light yellow solid. MS m/z 376.3 [M+H?i.

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; ALSENZ, Jochem; GRASSMANN, Olaf; KUEHL, Peter; METZGER, Friedrich; MCCARTHY, Kathleen Dorothy; MORAWSKI VIANNA, Eduardo Paulo; WOODHOUSE, Marvin Lloyd; (130 pag.)WO2017/80967; (2017); 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

109-07-9, Stage-2 : Preparation of 1-CYCLOPROPYL-7- 3-METHYLPIPERAZIN-1-YL)- 6-fluoro-8-methoxy-4-oxo-1, 4-DIHYDRO-3-QUINOLINE carboxylic acid boron difluoride chelate 100 g of Boron difluoride chelate derivative prepared as above in stage-1 is suspended in acetonitrile (800 ml), to that 2-methyl piperazine (44.0 g, 1. 5 mole EQUIV.) IS added and mixed for 15 min to obtain a clear solution. The reaction mass is maintained at 30C – 35C for 12 hrs followed by cooling TO-10C TO-5C. The reaction mass is maintained AT-10C TO-5C for 1 hr. The product is filtered and dried at 45C-50C to constant weight. Dry weight of the product : 116. 0 g (Yield : 93. 9 %).; Stage-2: Preparation of Gatifloxacin (Crude) The boron difluoride chelate derivative (100 g) prepared as above in stage-1 is suspended in acetonitrile (800 ml), 2-methyl piperazine (44 g, 1.5 mole equiv. ) is added and mixed for 15 min to obtain a clear solution. The reaction mass is maintained at 30C- 35C for 12 hrs. Removed the solvent by vacuum distillation. 20% Aq. ethanol (1000 ml) is added, raised the temperature and maintained at 75C to 80C for 2 hrs. The reaction mass is cooled, filtered to remove insolubles. The filtrate is distilled under vacuum to remove solvent completely. Fresh ethanol (250 ml) is added and distilled under vacuum at temperature below 50C. Fresh Ethanol (250 ml) is added to the residue and gradually cooled TO-10C TO-5C. The reaction mass is maintained AT-10C to-5C for 1 hr and filtered. The wet cake is washed with ethanol (30 ML) and dried at 45C-50C to constant weight. The dry weight of the Gatifloxacin is 73.5 g (Yield: 65.4 %)

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

Reference£º
Patent; MATRIX LABORATORIES LTD; WO2005/9970; (2005); 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added at room temperature to piperazin-2-one (2.5 g) in a mixture of tetrahydrofuran (50 mL) and methanol (50 mL), followed by stirring for 4 hours. The reaction solvent was evaporated under reduced pressure. The residue was partitioned between water and ethyl acetate. The organic layer was sequentially washed with water and saturated brine. The aqueous layers obtained through washing were combined, and the combined layer was extracted with ethyl acetate. The organic layers were combined, followed by drying over magnesium sulfate anhydrate. After a filtration step, the solvent was evaporated under reduced pressure. Subsequently, ethyl acetate-hexane was added to the residue, followed by drying to solid, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester (3.6 g, 72%). 1H-NMR(400MHz,CDCl3)delta:1.48(9H,s), 3.37-3.40(2H,m), 3.62-3.65(2H,m), 4.01(2H,s), 6.32(1H,br s). [Referential Example 40] 1-Ethyl-2-oxopiperazine hydrochloride [Show Image] 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Piperazin-2-one (5.07 g) was dissolved in tetrahydrofuran (50 mL) and methanol (50 mL), and, at room temperature, triethylamine (7.76 mL) and di-tert-butyl dicarbonate (12.17 g) were added to the solution, followed by stirring for 4 hours. The reaction solvent was evaporated under reduced pressure, and diethyl ether was added to the residue. The precipitated solid was collected through filtration, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester as a solid product (9.36 g, 92%). 1H-NMR(400MHz,DMSO-d6)delta:1.40(9H,s), 3.15(2H,br), 3.45(2H,br), 3.81(2H,br), 8.03(1H,br). ESI-MS m/z:201(M+H)+.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1762568; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

1-(2-(4-bromo-3-fluorophenoxy)ethyl)-4-methylpiperazine: A flask was charged with 4-bromo-3-fluorophenol (5.00 g, 26 mmol) and triphenylphosphine (10.30 g, 39 mmol). Methylene chloride (120 mL) was added followed by 2-(4-methylpiperazin-1-yl)ethanol (4.61 g, 32 mmol) and the solution was stirred on an ice water bath to cool. After 5 minutes, diisopropyl azodicarboxylate (7.6 ml, 39.1 mmol) was added over 6 to 8 minutes. The reaction was left stirring on the cold bath to slowly warm to room temperature overnight. The reaction was concentrated and the residue purified by flash chromatography (25percent to 100percent EtOAc in hexanes) to provide the product as a colorless oil (2.62 g, 33percent).

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; Hangauer, David G.; US2006/160800; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 25 mL flask was added TEA (177 mg, 244 ).ll, 1.75 mmol), tert-butyl piperazine-1-carboxylate (240 mg, 1.29 mmol), (bromomethyl)benzene (200 mg, 139 ).ll, 1.17 mmol) andDCM (4 mL). The colorless solution was stirred at rt for 3 hrs. The reaction mixture wasconcentrated to give a white solid. Then it was purified by silica gel column chromatography(eluted with EA/PE=15- 30% ), about 177 mg tert-butyl4-benzylpiperazine-1-carboxylate20 (Compound lOA) was obtained as a colorless oil. MS: calc’d 277 (M+Ht, measured 277(M+Ht, 57260-71-6

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; WANG, Lisha; YUN, Hongying; ZHANG, Weixing; ZHU, Wei; ZHANG, Zhiwei; (69 pag.)WO2017/202704; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 4 g (22 mmol) N-(2-chloro-pyridin-4-yl)-N-methyl-acetamide and 3.5 g (23 mmol) l-(cyclopentyl)-piperazine was heated to 120 0C for 24 h. The crude product was purified by flash column chromatography on silica eluting with a gradient formed from heptane and ethyl acetate (0.1% NEt3) to yield after evaporation of the product fractions 3.3 g (50%) of the title compound as light brow oil. MS: (m/e): 303.3 (MH+)., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; WO2006/63718; (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.55112-42-0,4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride,as a common compound, the synthetic route is as follows.

55112-42-0, Example 6: Preparation of Zopiclone in ACN[0069] To a slurry of l-chlorocarbonyl-4-methyl piperazine hydrochloride(CMP) (4.92g) in acetonitrile (ACN) (75 ml), stirred mechanically at Room temperature and under nitrogen, was added tri-ethyl amine (Et^N) (4.42g). After Et3N addition ended, DMAP (0.46g) was added to the slurry, and after 1-2 min of stirring, 7-OH -Py (5g) was added. The slurry changed its appearance at 7-OH addition. The stirring was applied for 2h at about 00C, then at room temperature for 14h.The reaction was completed after an additional heating (about 9h) at 400C. After cooling to the room temperature the solvent was evaporated, to give a yellowish-brown solid, that was dissolved in CH2CI2 (40 ml) and water (50 ml). Phases were separated while the interphase was left in the aqueous phase. The aqueous phase was extracted with CH2CI2 (40 ml). The combined organic phases were washed with water (50 ml), dried over MgSO4 filtered and evaporated to dryness to give zopiclone crude product (6.17g, yield 82.2%; purity 98.24% by HPLC).

The synthetic route of 55112-42-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/2629; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics