Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

38. 159 mg of 4-{[4-((4-methylpiperazin-1-yl)methyl)phenyl]hydrazono}-4H-pyrazole-3,5-diamine was prepared in two steps starting with 205 mg (1.00 mmol) of 4-(4-methylpiperazin-1-yl)methylphenylamine. Yield 50.6%. MS (m/z, ES+): 315 (M+1, 20%). 1H NMR (ppm, 200 MHz, DMSO-d6) delta 2.1 (s, 3H), 2.2-2.5 (br m, 4H), 3.15-3.25 (br m, 4H), 3.45 (s, 2H), 5.5-6.5 (br m, 4H), 7.25 (d, 2H), 7.55 (d, 2H), 10.75 (s,1H)., 70261-82-4

70261-82-4 4-(4-Methylpiperazin-1-ylmethyl)phenylamine 3153996, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhang, Zaihui; Daynard, Timothy Scott; Sviridov, Serguei V.; Chafeev, Mikhail A.; Wang, Shisen; US2003/60453; (2003); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE D rac-3-Methyl-4-(4-trifluoromethyl-phenyl)-piperazine-1-carboxylic acid tert-butyl ester To a solution of 3-Methyl-piperazine-1-carboxylic acid tert-butyl ester (1.0 g, 5.3 mmol) and of 1-Bromo-4-trifluoromethyl-benzene (1.0 g, 4.4 mmol) in toluene (10 ml) were added sodium-tert butylate (0.6 g, 6.2 mmol), 2-(dicyclohexylphosphino)biphenyl (31. mg,89 mmol), and tris(dibenzylideneacetone)dipalladium-chloroform complex (23 mg, 22 mmol). The reaction mixture was then stirred for 16 hours at 80¡ã C. After allowing to cool to room temperature the reaction mixture was concentrated in vacuo and purified by column chromatography (SiO2, 70 g, heptane/ethyl acetate 0-30percent) to give the title compound as a light brown solid (0.47 g); MS (m/e): 345.2 (M+H+, 100percent)., 120737-59-9

Big data shows that 120737-59-9 is playing an increasingly important role.

Reference£º
Patent; Alberati-Giani, Daniela; Jolidon, Synese; Narquizian, Robert; Nettekoven, Matthias Heinrich; Norcross, Roger David; Pinard, Emmanuel; Stalder, Henri; US2005/59668; (2005); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: An ethanolic solution (10 mL) of sodium hydroxide (10 mmol, 0.4 g) was added to an ethanolicsolution (10 mL) of the secondary amine (10 mmol). The mixture was cooled in an ice bath; additionally,carbon disulfide (100 mmol, 6.0 mL) was added dropwise with continuous stirring for 1 h at roomtemperature. The precipitates were filtrated and washed with diethyl ether to obtain a white topale-yellow-colored product in 70-90% yield

103-76-4, 103-76-4 N-(2-Hydroxyethyl)piperazine 7677, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Hussein, Weiam; Sa?lik, Beguem Nurpelin; Levent, Serkan; Korkut, Bue?ra; Ilgin, Sinem; Oezkay, Yusuf; Kaplancikli, Zafer Asim; Molecules; vol. 23; 8; (2018);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

77279-24-4,77279-24-4, tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 63; l-{2-[4-(3,5-dimethoxybenzyl)piperazin-l-yl]ethyl}-3,3-bis(4-fluorophenyl)pyrrolidin-2- one; Example 63A; tert-butyl 4-(2-bromoethyl)piperazine-l-carboxylate; tert-Butyl 4-(2-hydroxyethyl)piperazine-l-carboxylate (5.76 g, 25.0 mmol) was dissolved in dry tetrahydrofuran (100 mL) and carbon tetrabromide (9.12 g, 27.5 mmol). A solution of triphenyl phosphine (6.62 g, 25.3 mmol) in dry tetrahydrofuran (25 mL) was added dropwise, and the mixture was stirred for 20 hours. The reaction was diluted with n- hexane (100 mL) and washed with a saturated NaHCO3 solution, water and brine, dried with MgSO4, filtered and concentrated. Silica gel chromatography eluting with ethyl acetate/hexanes 1 :4 gave the title compound. MS (DCI) m/z 295(M+H)+.

The synthetic route of 77279-24-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBOTT LABORATORIES; BHATIA, Pramila, A.; DOHERTY, George, A.; DRIZIN, Irene; MACK, Helmut; PERNER, Richard, J.; STEWART, Andrew, O.; ZHANG, Qing Wei; WO2010/39947; (2010); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2762-32-5,Piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

2-PIPERAZINECARBOXYLIC acid and 2-CHLORO-1, 3-pyrimidine were stirred with triethylamine and MeOH. After stirring overnight at reflux, the mixture was filtered and concentrated in vacuo to give the desired compound which was used directly in Step B (MH+ = 209).

2762-32-5, 2762-32-5 Piperazine-2-carboxylic acid 2723758, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PHARMACOPEIA, INC.; WO2004/33440; (2004); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Step A: Preparation of 2a; According to general procedure C, 2a was obtained with 1a (0.25 mL, 5.18 mmol, 1.0 eq.), EDC (324 mg, 10.36 mmol, 2.0 eq.), DMAP (317 mg, 10.36 mmol, 2.0 eq.) and N-methylpyrrole-2-carboxylic acid (329 mg, 10.36 mmol, 2.0 eq.). The mixture was washed first with a saturated solution of ammonium chloride, then with 1 N HCl and at the end with a saturated solution of sodium carbonate. The residue was purified by flash chromatography on silica gel, eluting with cyclohexane-ethyl acetate (8:2 to 1:1) to afford 2a (420 mg, 98percent) as a colorless oil.MS (ESI+) (+0.1percent HCOOH): 328.12 [C18H21N3O3+H]+ (m/z); “General method C” (peptide coupling) consists of adding 1.2 to 2.0 equivalents of EDCl and 1.2 to 2.0 equivalents of HOBt or DMAP and 1.2 to 2.0 equivalents of heteroaryl carboxylic acid, at 0¡ã C., to a 0.2 to 0.6M solution within DMF of protected amino(piperidine) derivative N-Boc or N-CBz. The mixture is maintained under stirring at ambient temperature for 16 to 18 hours, then diluted with ethyl acetate and washed with water. The solution is then dried and concentrated to dryness under reduced pressure, then the residue is purified by chromatography over silica eluting with the cyclohexane-ethyl acetate mixture., 31166-44-6

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Vetoquinol SA; US2010/9980; (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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

934-98-5, To a disposable tube with stir bar was added tert-butyl 3-(4-chloro-3-(2-(methylsulfonyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamido)benzamido)-3-phenylpropylcarbamate (100 mg, 153 mumol, Eq: 1.00) (from Example 116 supra), DMF (0.5 mL) and then 2-(4-methylpiperazin-1-yl)ethanamine (437 mg, 3.05 mmol, Eq: 20). The reaction was heated at 75¡ã C. in a pre-heated oil bath for 3 hours, after which it was cooled to room temperature. The reaction was then diluted with water, the solid was filtered off and then rinsed with water and then diethyl ether to provide after drying tert-butyl 3-(4-chloro-3-(2-(2-(4-methylpiperazin-1-yl)ethylamino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamido)benzamido)-3-phenylpropyl-carbamate. (Yield 74 mg, 68percent).LR-MS [M+H]+: 718.

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference£º
Patent; Anderson, Kevin; Chen, Yi; Chen, Zhi; Luk, Kin-Chun; Rossman, Pamela Loreen; Sun, Hongmao; Wovkulich, Peter Michael; US2012/184542; (2012); 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.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

a) To a solution of (R)-N-(l-(2,4-dichlorophenyl)ethyl)-5-fluoro-2-nitroaniline (prepared from Example 14 step a, 1.6 g, 4.9 mmol) and (5)-2-(hydroxymethyl)piperazine-l- carboxylic acid ?-butyl ester (0.99 g, 4.9 mmol) in anhydrous DMSO (10 mL) was added K2CO3 (1.88 g, 14.6 mmol). The reaction mixture was heated with stirring at 125 C for 2 h. After cooling to room temperature, the mixture was diluted with deionized water (10 mL) and stirred for 30 min. The aqueous layer was extracted with dichloromethane. The organic layer was dried (MgS04), filtered, and concentrated in vacuo. The crude oil was dried under vacuum to give the desired compound (1.9 g, 3.5 mmol, 73%).

1030377-21-9, 1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHEMOCENTRYX, INC.; LELETI, Manmohan Reddy; LI, Yandong; MALI, Venkat Reddy; POWERS, Jay; YANG, Ju; WO2013/82429; (2013); 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.118753-66-5,tert-Butyl 4-aminopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 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 2-(4-chloro-3-fluorophenoxy)acetic acid (0.201 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), brine solution (30 mL x 2), dried over anhydrous sodium sulfate and concentrated under reduced pressure, to obtain tert-butyl 4-(2-(4-chloro-3-fluorophenoxy)acetamido)piperazine-l -carboxylate (0.150 g, 38 % Yield) as a semi solid. LCMS 388 2 | M H | ; NMR (400MHz, DMSO-de) d 7.57 – 7.36 (m, 1 H), 7.11 – 6.94 (m, 1 H), 6.92 – 6.69 ( m. 1 H), 5.76 (s, 1 H), 5.04 – 4.79 (m, 1 ). 4.48 (s, 1 H), 3.85 (br s, 1 H), 2.92 (br. s., 2 H), 2.70 (d, J= 11.8 Hz, 2 H), 1 40 (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;,
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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

4-(Thiophen-2-yl)butanoic acid (0.05 ml, 0.34 mmol), HOBt (58 mg, 0.43 mmol), TBTU (140 mg, 0.43 mmol), anhydrous triethylamine (0.1 ml, 0.69 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (100 mg, 0.43 mmol) and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 80% yield. H NMR (300 MHz, CDCI3) ? 7.49 (d, 2H), 7.12 (dd, 1 H), 6.90-6.94 (m, 3H), 6.80-6.82 (m, 1 H), 3.76 (t, 2H), 3.56 (t, 2H), 3.24 (t, 4H), 2.91 (t, 2H), 2.38 (t, 2H), 2.0-2.1 1 (m, 2H). MS (+ESI) calcd for C18 H21 F3 N2 O S m/z: [M + H]+, 382.1329; found 383.1399 [Diff(ppm) = 0.61]., 30459-17-7

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

Reference£º
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics