Month: March 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Phenyl (4-chloro-3-fluorophenyl)carbamate (441 mg, 1.659 mmol) and tert-butyl 3-(2- hydroxyethyl)piperazine-l-carboxylate (382 mg, 1.659 mmol) were suspended in EtOH (5 niL) and heated in a Biotage Initiator using initial high setting to 100 C for 7 min. The reaction was concentrated under a stream of nitrogen at 50 C then dissolved in DCM (3 niL) and TFA (3 niL, 38.9 mmol). After 30 minutes the reaction was concentrated under a stream of nitrogen at 50 C. The residue was dissolved in DCM/MeOH and loaded onto a SCX-3 cartridge (2 g). The cartridge was washed with 3 volumes of MeOH, then eluted with 3 volumes of 2N NH3MeOH. The eluants were concentrated under a stream of nitrogen at 50 C followed by high vacuum, resulting in the isolation of N-(4-chloro-3-fluorophenyl)-2-(2 -hydro xyethyl)piperazine-l-carboxamide (494 mg, 1.637 mmol, 99 % yield) as a white solid.LC/MS (ESI): m/z 302.0 (M+H)+, 0.39 min (ret. time)

1188265-73-7, 1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BAILEY, James; CHEN, Yao; HURLE, Mark; LEACH, Craig; TURUNEN, Brandon; (103 pag.)WO2018/134731; (2018); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, EXAMPLE 3 4-((4-methyl-1-piperazinyl)methyl)aniline (I-c) Crude I-a (8.5g, 36.2mmol), FeO(OH)/C, 2.0 g as catalyst and 95% ethanol (100 ml) were added into a 500 mL single neck flask, which was refluxed. Into the reaction system were added slowly and dropwise a mixture of 25 mL hydrazine hydrate and 20 mL 95% ethanol. The depletion of the starting materials was confirmed by TLC (methanol: chloroform = 1:15). Suction filtration was performed while the reaction mixture was hot. The filter cake was washed with hot ethanol twice (30 ml *2). After removal of the solvent under reduced pressure, white solid was obtained, which was dried under vacuum to give 6.7 g (I-c); Yield: 90.3%. The product was used for subsequent reaction without further purification. 1H-NMR[300MHz, DMSO-d6]: delta2.1 (3H, s, -CH3), 2.3-2.5 (8H, m, -CH2-*4), 3.5 (2H, s, -CH2-), 4.0(2H, s, -NH2), 7.5 (2H, d, J = 8.7 Hz, ArH), 8.1 (2H, d, J = 8.7 Hz, ArH).

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference£º
Patent; China Pharmaceutical University; LU, Tao; WANG, Yue; CHEN, Yadong; LU, Yi; WANG, Zhanwei; JIN, Qiaomei; YANG, Taotao; LIN, Guowu; GUO, Qinglong; ZHAO, Li; EP2955185; (2015); 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

[7261 Step 1: Synthesis of (3R.55?)- 1 -benzyl-3 .5-dimethvlpiperazine [7271 (2S,6R)-2,6-dimethylpiperazine (1.000 g, 8.757 mmol) and K2C03(1.724 g, 13.136 mmol) were dissolved in acetonitrile (5OmL), and benzylbromide (1.092 mL, 9.195 mmol) was added thereto at 0 ¡ãC, and the mixture was stuffed at the same temperature for 1 hour and 30 minutes. Water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with a saturated aqueous solution of sodium chloride, dried with anhydrous magnesium sulfate, and then concentrated under reduced pressure. The concentrate was purified by column chromatography (silicon dioxide; methanol/methylene chloride = 5 percent) and concentrated to afford the desired compound (1.170 g, 65.4 percent) as a yellow oil., 21655-48-1

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

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; SONG, Hyeseung; LEE, Changgon; KWAK, Dalyong; LEE, Jaeyoung; BAE, Suyeal; KIM, Yuntae; BAE, Daekwon; HA, Nina; BAE, Miseon; KIM, Jihyun; WO2015/137750; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (8-((5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)carbamoyl)-2-(dimethoxymethyl)-5,6 ,7 ,8-tetrahydro-1 ,8-naphthyridin-3-yl)methyl methanesu Ifonate (intermediate170, 368 mg, 0.657 mmol) in DCM (2.7 ml) at room temperature was added NEt3 (0.319 ml, 2.301mmol) followed by 1-methylpiperazin-2-one (120 mg, 1.052 mmol). The reaction mixture was stirred at room temperature for 2 h and partitioned between DCM and water. The water layer was extracted multiple times with DCM, the combined organic layers were dried using Na2504, filtered and evaporated. The crude product was purified by silica gel column chromatography usinggradient of MeOH (0-3percent) in DCM to yield the title compound as a white solid. (UPLC-MS 3) tR 0.87mm; ESl-MS 553.3 [M+H].1H NMR (600 MHz, CDCI3)5 13.75 (s, IH), 8.20 (s, IH), 7.64 (brs, IH),7.58 (s, I H), 5.56 (s, I H), 5.23 (d, I H), 4.06 ? 4.01 (m, 2H), 3.70 (br s, 2H), 3.63 (t, 2H), 3.503.42 (m, 8H), 3.40 (s, 3H), 3.31 (br s, 2H), 3.14 (br s, 2H), 2.96 (br s, 3H), 2.87 ?2.80 (m, 2H), 2.71(br s, 2H), 2.03 ? 1.96 (m, 2H)., 59702-07-7

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

Reference£º
Patent; NOVARTIS AG; BUSCHMANN, Nicole; FAIRHURST, Robin Alec; FURET, Pascal; KNOePFEL, Thomas; LEBLANC, Catherine; MAH, Robert; NIMSGERN, Pierre; RIPOCHE, Sebastien; LIAO, Lv; XIONG, Jing; ZHAO, Xianglin; HAN, Bo; WANG, Can; WO2015/59668; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 1-(3-hydroxypropyl)-4-methylpiperazine used as a starting material was prepared as follows: A mixture of 3-bromopropanol (20 ml), N-methylpiperazine (29 ml), potassium carbonate (83 g) and ethanol (200 ml) was stirred and heated to reflux for 20 hours. The mixture was cooled to ambient temperature and filtered. The filtrate was evaporated and the residue was triturated under diethyl ether. The resultant mixture was filtered and the filtrate was evaporated. The residue was purified by distillation to give the required starting material as an oil; NMR Spectrum: (CDCl3) 1.72 (m, 2H), 2.3 (s, 3H), 2.2-2.8 (m, 8H), 2.6 (t, 2H), 3.8 (t, 2H), 5.3 (br s, 1H)., 109-01-3

109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Hennequin, Laurent Francois Andre; Crawley, Graham Charles; McKerrecher, Darren; Ple, Patrick; Poyser, Jeffrey Philip; Lambert, Christine Marie Paul; US2003/225111; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

438631-77-7, (R)-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

To degassed solution of 68 1,4-dioxane (71.6 mL) and 56 DIPEA (5.65 mL, 32.46 mmol) at rt was added 505 7-bromo-4-chloro-6,8-difluoro-3-nitroquinoline (3.5 g, 10.82 mmol) followed by 272 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (3.96 g, 16.23 mmol). The reaction was heated at 100 C. for 16 h. The reaction was cooled to rt and the solvent removed in vacuo. The resulting residue was diluted with EtOAc (300 mL), washed with water (2¡Á250 mL) and brine (100 mL). The organic layer was dried (phase separator) and concentrated in vacuo to afford crude material which was purified by flash silica chromatography (0 to 50% 57 EtOAc in 58 heptane) to give 507 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6,8-difluoro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (3.89 g, 68%) as an orange dry film; 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.18-3.29 (2H, m), 3.54 (3H, s), 3.57-3.66 (1H, m), 3.72-3.95 (2H, m), 4.05 (1H, s), 4.33 (1H, s), 8.06 (1H, dd), 9.13 (1H, s); m/z: ES+ [M+H]+ 530.9.

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); 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

Intermediate 66: (3R*,5Si:)-3,5-Dimethyl-piperazin-l-yl)-(l-m-tolyl-lH-[l ,2,4]triazol-3-yl)- methanone A mixture of 610 mg (3.00 mmol) l-m-tolyl-lH-[l,2,4]triazole-3-carboxylic acid, 350 mg (3.00 mmol) cz’s-2,6-dimethyl-piperazine, 1.06 g (3.30 mmol) TBTU and 770 mu, (4.50 mmol) DIPEA in 5.0 mL DMF was stirred with at RT for 12 h. The reaction mixture was poured into ice water and extracted with EtOAc. The combined organic phases were washed with saturated NaHC03 solution, dried over sodium sulfate, filtered and concentrated in vacuo. Yield: 520 mg (58 percent) ESI-MS: m/z = 300 (M+H)+ Rt(HPLC): 0.80 min (method 8), 21655-48-1

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

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

639068-43-2, tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,639068-43-2

A solution of compounds of general structure 1 (1 equiv), Boc protected amine (1-3 equiv) and DIPEA (3 equiv) in DMSO were reacted at 100-110 ¡ãC. The reaction mixture was cooled to room temperature and quenched by addition of water and crude residue extracted with EtOAc. Combined organic layers were washed with brine, dried over Na2S04, filtered and concentrated under reduced pressure to provide crude compound of general strucutre 2, which was used in the following step without further purification. To a solution of compounds of general structure 2 in CH2C12 was added HCl/dioxane (4 N) or TFA. The reaction was stirred at room temperature for 2 hrs and mixture was concentrated under reduced pressure. The residue was purified by reverse phase preparative HPLC to afford final compounds of general structure 3.

The synthetic route of 639068-43-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KADMON CORPORATION, LLC; SKUCAS, Eduardas; LIU, Kevin, G.; KIM, Ji-In; POYUROVSKY, Masha, V.; MO, Rigen; (345 pag.)WO2019/45824; (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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of Intermediate 13b (1.15 g, 5.0 mmol), 2-(4-methyl- piperazin-l -yl)-ethanol (864 mg, 6.0 mmol) and triphenylphosphine (2.62 g, 10.0 mmol) in THF (10 mL) was added diisopropyl azodicarboxylate (2.0 g, 10.0 mmol) dropwise and stirred for 75 min. The mixture was diluted with diethyl ether (50 mL) and extracted with 10percent aqueous citric acid soln (2 x). The combined aqueous layers were basified with solid potassium carbonate until pH = 9. The aqueous layer was then extracted with ethyl acetate (3 x). The combined ethyl acetate layers were washed with brine, dried (NaSO4) and evaporated in vacuo. Purification by FCC using 0- 12percent [9: 1 MeOH/880 ammonia] in DCM. The resulting product was crystallised (diethyl ether) to give the title compound (270 mg, 0.756 mmol, 15percent). LCMS (Method 1): Rt 2.31 , 1.72 min, m/z 358/359 [MH+].

5464-12-0, The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHIESI FARMACEUTICI S.P.A.; VAN NIEL, Monique Bodil; RAY, Nicholas Charles; ALCARAZ, Lilian; PANCHAL, Terry Aaron; JENNINGS, Andrew Stephen Robert; ARMANI, Elisabetta; CRIDLAND, Andrew Peter; HURLEY, Cristopher; WO2013/83606; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3 4-[4-(4′-{2-[(S)-1-((S)-2-Methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-1H-imidazol-4-yl}-biphenyl-4-ylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester To a solution of 4-(4-(tert-butoxycarbonyl)piperazin-1-yl)benzoic acid (24.7 mg, 0.081 mmol) in dichloromethane (0.89 mL, 14 mmol) and N,N-dimethylformamide (0.4 mL, 6 mmol) was added N,N-diisopropylethylamine (0.071 mL, 0.407 mmol) and methyl chloroformate (0.006 mL, 0.081 mmol). The reaction mixture was stirred for 15 min at room temperature, then ((S)-1-{(S)-2-[4-(4′-amino-biphenyl-4-yl)-1H-imidazol-2-yl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (25.0 mg, 0.054 mmol) was added and the mixture was allowed to stir overnight. The reaction mixture was concentrated and then dissolved in DCM (5 mL) and washed with saturated aqueous sodium bicarbonate (2 mL). The organic layer was concentrated. Approximately 15 mg of the crude material was concentrated, dissolved in 1:1 acetic acid:water (1.5 mL), and purified by preparative HPLC to provide the trifluoroacetic acid salt of the title compound (7.3 mg). (m/z): [M+H]+ calcd for C42H51N7O6 750.39 found 750.4., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; THERAVANCE, INC.; US2012/114600; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics