Category: piperazines

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 2-(5-iodomethyl-2-oxo-oxazolidin-3-yl)-N-(6-methoxy-2-methyl-quinolin-4-yl)-acetamide (12, 0.2 g, 0.439 mmol), potassium carbonate (0.151 g, 1.09 mmol), different substituted amines (1.1 mmol) in 10 mL of acetonitrile was heated to 80 °C for 4 h. The reaction completion was monitored by TLC and when the reaction was completed, the reaction mass was filtered through a celite bed, filtrate was concentrated under reduced pressure. The crude residue was purified using biotage parallel column purifier using ethyl acetate in petroleum ether (4:1) to 4-6percent methanol in dichloromethane as eluant. The spectral data for the final compounds, 13a-n is given below.

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Thomas; Adhikari, Airody Vasudeva; Chowdhury, Imran H.; Sandeep; Mahmood; Bhattacharya; Sumesh; European Journal of Medicinal Chemistry; vol. 46; 10; (2011); p. 4834 – 4845;,
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.

DIPEA (84 ml, 480.94 mmol) was added to 53 7-bromo-4,6-dichloro-3-nitroquinoline (60 g, 186.37 mmol) and 55 tert-butyl (R)-3-(hydroxymethyl)piperazine-1-carboxylate (89 g, 410.02 mmol) in 131 i-PrOH (600 ml). The resulting mixture was stirred at 80 C. for 2 hours. The solvent was removed under reduced pressure. The crude product was purified by flash silica chromatography, elution gradient 0 to 20% 57 EtOAc in 148 petroleum ether. Pure fractions were evaporated to dryness to afford 199 tert-butyl (3R)-4-(6-bromo-7-chloro-3-nitroquinolin-4-yl)-3-(hydroxymethyl)piperazine-1-carboxylate (54 g, 58%) as a yellow solid. 1H NMR (DMSO, 300 MHz) 1.16 (1H, t), 1.31-1.46 (9H, m), 1.97 (1H, s), 2.10-2.27 (1H, m), 2.36 (1H, d), 2.66 (1H, s), 3.47 (1H, s), 3.77 (1H, s), 4.01 (1H, q), 4.14 (1H, s), 7.50-7.64 (1H, m), 8.52 (1H, d), 8.62 (1H, s), 11.16 (1H, s). m/z (ES+), [M+H]+=503., 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.889939-92-8,2-(1-Methylpiperazin-2-yl)ethanol,as a common compound, the synthetic route is as follows.

889939-92-8, Method 9 4-[3-(2-Methoxyethyl)-4-methylpiperazin-1-yl]-2-(propan-2-yloxy)aniline 974 mg of N,N-diisopropylethylamine and 724 mg of 2-(1-methylpiperazin-2-yl)ethanol are added to a suspension of 1 g of 4-fluoro-1-nitro-2-(propan-2-yloxy)benzene in 10 ml of acetonitrile. The reaction medium is microwave-heated at 110 C. for 6 hours and then concentrated to dryness under reduced pressure. Purification is carried out by flash chromatography on silica gel (40-63 microns), elution being carried out with a mixture of dichloromethane and methanol (100/0) to (90/10). 1.15 g of 2-{1-methyl-4-[4-nitro-3-(propan-2-yloxy)phenyl]piperazin-2-yl}ethanol are obtained in the form of a yellow oil.

As the paragraph descriping shows that 889939-92-8 is playing an increasingly important role.

Reference：
Patent; SANOFI; CARRY, Jean-Christophe; CHATREAUX, Fabienne; DEPRETS, Stephanie; DUCLOS, Olivier; LEROY, Vincent; MALLART, Sergio; MELON-MANGUER, Dominique; MENDEZ-PEREZ, Maria; VERGNE, Fabrice; US2013/261106; (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 5-chlorobenzofuran-2 -carboxylic acid (0.100 g, 0.50 mmol, 1.0 equiv) in DMF (05 mL) was added HATH (0.380 g, 1.01 mmol, 2.0 equiv) at RT and stirred for 10 minutes. Then tert-butyi 4-aminopiperazine-l -carboxylate (0.112 g, 0.55 mmol, 1.1 equiv) was added followed by the addition of DIPEA (0 2 mL, 1.52 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 c 2). Tire 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-(5-chlorobenzofuran-2-carboxamido)piperazine-l-carboxylate (0.140 g, 66 % Yield) as an off-white solid. LCMS 380.3 [M+H]+; NMR (400MHz, DMSO-de) d 9.90 (s, 1 H), 7.87 (s, 1 H), 7.70 (d, J= 8 8 Hz, 1 H), 7.57 – 7.44 (m, 2 H), 3 42 (br. s, 4 H), 2.83 (br. s ,4 H), 1.50 – 1.29 (m, 9 H)., 118753-66-5

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference：
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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: Synthesis of (S)-tert-butyl-2-methyl-4-(pyrimidin-2-yl)piperazine-1-carboxylate To the mixture of 2-chloropyrimidine (200 mg, 1.75 mmol), (S)-tert-butyl-2-methylpiperazine-1-carboxylate (350 mg, 1.75 mmol), and DIPEA (677 mg, 5.24 mmol) was added DMF (4 mL). The mixture was stirred at 100 C. for 3 hrs, then extracted with EtOAc/H2O (50 mL/50 mL). The organic phase was dried over anhydrous Na2SO4 and concentrated in vacuo. The residue was purified by chromatography (silica, PE/EtOAc=0-10%) to afford (S)-tert-butyl-2-methyl-4-(pyrimidin-2-yl)-piperazine-1-carboxylate (330 mg, 67.8%). MS (EI+, m/z): 279 [M+H]+., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference：
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (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.

General procedure: The appropriate 1-substituted piperazines (1 mmol)and Et3N (3 mmol) were added to a solution of 6-chloropurines(1mmol) (5, 6) in 5 mL of absolute EtOH. Themixture was refluxed for 8-16 h. The reaction mixture wasconcentrated in vacuo and the residue was purified by columnchromatography (EtOAC-hexane, 1:3 to 1:1).

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

Reference：
Article; Atalay, Rengul Cetin; Guven, Ebru Bilget; Kucukdumlu, Asligul; Tuncbilek, Meral; Acta Chimica Slovenica; vol. 67; 1; (2020); p. 70 – 82;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Ethyl 5-chloro-l ,3,4-thiadiazole-2 -carboxylate (3, 3 g, 15.7 mmol), 2-methoxy-4-(4-methyl piperazin-l -yl)aniline (4, 3.4 g, 15.7 mmol) and p-TSA (3 g, 15.7 mmol) were taken up in IPA (25 mL) and the resultant mixture was stirred at 80 C overnight. The progress of the reaction was monitored by TLC. After completion of the reaction, the solvent was evaporated from the reaction mixture under reduced pressure, and the resultant residue was basified using aq. NaHC03 solution and extracted with ethyl acetate. The organic extract was dried over anhydrous sodium sulfate and evaporated under reduced pressure. The resultant crude product was purified by columnchromatography using 5% MeOH-DCM to afford ethyl 5-((2-methoxy-4-(4-methylpiperazin-l – yl)phenyl)amino)-l ,3,4-thiadiazole-2-carboxylate (5, 1 .5 g, 25%). NMR (400 MHz, CDC13): delta 7.90 (bs, 1 H), 7.43 (d, 1 H), 6.59-6.55 (m, 2H), 4.50 (q, 2H), 3.90 (s, 3H), 3.25-3.22 (m, 4H), 2.65- l .60 (m, 4H), 2.40 (s, 3H), 1.42 (t, 3H)., 122833-04-9

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GATEKEEPER PHARMACEUTICAL, INC.; GRAY, Nathanael, S.; ZHOU, Wenjun; WO2011/79231; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Cyclobutyl-1-cyclohexyl-4-(6-fluoro-pyridin-3-yl)-1H-pyrazolo[3,4-]pyridine-6-carboxylic acid (200 mg, 0.51 mmol) was heated together with 1-cyclopropylpiperazine ([20327- 23-5], 64 muL, 0.53 mmol) and DIPEA (110 muL, 0.64 mmol) in NMP (2 mL) at 100 C for 18 hours. The mixture was diluted with EtOAc and water. Isolation of the organic layer and subsequent concentration yielded the titled compound., 20327-23-5

As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference：
Patent; ABBVIE S.A.R.L; GALAPAGOS NV; AKKARI, Rhalid; ALVEY, Luke Jonathan; BOCK, Xavier Marie; BROWN, Brian S.; CLAES, Pieter Isabelle Roger; COWART, Marlon D.; DE LEMOS, Elsa; DESROY, Nicolas; DUTHION, Beranger; GFESSER, Gregory A.; GOSMINI, Romain Luc Marie; HOUSSEMAN, Christopher Gaetan; JANSEN, Koen Karel; JI, Jianguo; KYM, Philip R.; LEFRANCOIS, Jean-Michel; MAMMOLITI, Oscar; MENET, Christel Jeanne Marie; MERAYO, Nuria Merayo; NEWSOME, Gregory John Robert; PALISSE, Adeline Marie Elise; PATEL, Sachin V.; PIZZONERO, Mathieu Rafael; SHRESTHA, Anurupa; SWIFT, Elizabeth C.; VAN DER PLAS, Steven Emiel; WANG, Xueqing; DE BLIECK, Ann; (1004 pag.)WO2017/60874; (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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Example 9. l-(4-{2-[[l-(3,5-Dichloro-benzyl)-lH-imidazol-2-ylmethyl]-(3-fluoro- benzyl)-amino]-ethyl}-piperazin-l-yl)-ethanone EPO (BoC)2O (2.29 g, 10.5 mmol) was added to a solution l-(2-hydroxyethyl)piperizine (1.30 g, 10 mmol) in THF (10 mL) at 0 0C. The mixture was stirred at ambient temperature for 14 h. The volatiles were removed in vacuo to afford 4-(2-hydroxy-ethyl)-piperazine-l- carboxylic acid tert-butyl ester (2.3Og, 100%) as a colorless oil which solidified on standing: ESI MS m/z 231 [CnH22N2O3 + H]+.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2006/107923; (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.848482-93-9,(S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

848482-93-9, INTERMEDIATE 5 (S)-(4-Methyl-piperazin-2-yl)-methanolTo a stirred suspension of (S)-piperazine-l,3-dicarboxylic acid l-tert-buty ester (5.00 g, 21.7 mmol) in THF (40 mL) was slowly added 1.0 M borane-THF complex solution (32.6 rnL, 32.6 mmol). The reaction was heated to 90 0C and stirred under reflux for 2 hours. The reaction mixture was removed from the heat before a further 1.5 equivalents of 1.0 M borane-THF complex solution (32.6 mL, 32.6 mmol) was added. The reaction was reheated to 90 0C and stirred under reflux for a further 2 hours. The reaction was cooled to 0 0C and quenched by the slow addition of MeOH. The reaction mixture was then concentrated in vacuo. The white solid obtained was dissolved in THF (30 mL), cooled to 0 0C and slowly added a 2.0M solution of LiAlH4 in THF (27 mL, 54.0 mmol). The reaction was heated to 90 0C and stirred under reflux for 2h. A further portion of 2.0M solution of LiAlH4 in THF (27 mL, 54.0mmol) was added and the reaction stirred under reflux for 4h and then at room temperature overnight. The reaction mixture was cooled to O0C and quenched by the slow addition of 1.0M aq NaOH solution until the exothermic reaction subsided. The resulting gel was diluted with THF and the solids filtered off. The filtrate was then concentrated in vacuo to afford (S)-(4-methyl-piperazin-2-yl)-methanol (2.84 g, 101% crude yield) as a colourless oil.

848482-93-9 (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid 1501850, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BIOVITRUM AB (PUBL); WO2009/71658; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics