Category: piperazines

934-98-5,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.

00106] Step 6. To a solution of 4-((lH-indol-3-yl)methyl)-3-ethylaniline (0.8 g, 3.2 mmol) and 4-nitrophenyl carbonochloridate (0.64 g, 3.2 mmol) in THF was added diisopropylethylamine (0.4 g, 3.2 mmol) (16 mL) at 20 ¡ãC and the resulting solution was stirred for 30 min. Then 2-(4-methylpiperazin-l-yl)ethanamine (0.9 g, 6.4 mmol) was added to the solution. After the addition was complete, the mixture was stirred at 20 ¡ãC for 12 h. The mixture was concentrated and purified by preparative HPLC to give l-(4-((lH-indol-3- yl)methyl)-3-ethylphenyl)-3-(2-(4-methylpiperazin-l-yl)ethyl)urea (0.33 g, 26percent) as a yellow solid. 1H NMR (400 MHz, MeOD) delta: 1.13-1.17 (t, 3H), 2.25 (s, 3H), 2.48-2.71 (m, 10H), 3.29- 3.32 (m, 2H), 4.01 (s, 2H), 6.73 (s, 1H), 6.92-6.96 (m, 1H), 7.02-7.08 (m, 3H), 7.18 (s, 1H), 7.29-7.31 (d, J = 8.0 Hz, 1H), 7.39-7.41 (d, J = 7.6 Hz, 1H); MS (M+l+): 220.3.

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; WO2013/148365; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

[4990] A solution of N-(4-(chloi methyl)phenyl)thiomotpholine-4-carboxamide 1,1-dioxide (l.OOOg.3.303 mmol), tert-butyl (3S,5R)-3.5-dimethylpipeiazine-l-carboxylate (1.416 g.6.606 mmol) and potassium carbonate (1.369 g, 9.909 mmol) in acetonitrile (50 mL) prepared at the room temperature was stirred at the same temperature for 18 hr and concentrated under the reduced pressure. Then, water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous MgS0 , filtered, and concentrated in vacuo. The residue was diluted with diethylether (15 mL) and stirred. The resulting precipitates were collected by filtration, washed by diethylether, and dried to give tert-butyl (2S,6R)-4-(4-(l,l-dioxidothiomorpholine-4-carboxamido)benzyl)-2,6-dimethylpiperaz ine-l-carboxylate as pale yellow solid (1.580 g, 99.5 ).

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; KIM, Yuntae; LEE, Chang Sik; SONG, Hyeseung; GWAK, Dal-Yong; LEE, Jaeyoung; OH, Jung Taek; LEE, Chang Gon; KIM, II Hyang; (1041 pag.)WO2017/23133; (2017); A2;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

A solution of methyl 4-((N-phenylvinylsulfonamido)methyl)benzoate (0.300 g, 0.905 mmol), (2S,6R)-2,6-dimethylpiperazine (0.207 g, 1.811 mmol) and N,N-Diisopropylethylamine (0.189 mL, 1.086 mmol) in tetrahydrofuran (5 mL) was stilTed at the room temperature for 5 hr. Then, water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with aqueous saturated ammonium chloride solution, dried with anhydrous MgSO4, filtered, and concentrated in vacuo. The residue was chromatographed (Si02, 4 g cartridge; methanol / dichloromethane =0 percent to 10 percent) to give methyl4-(((2-((3S,5R)-3 ,5-dimethylpiperazin- 1 -yl)-N-phenylethyl) sulfonamido)methyl)benzo ate as white solid (0.403 g, 99.9 percent).

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.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; CHOI, Daekyu; MIN, Jaeki; BAE, Miseon; YANG, Hyunmo; KIM, Dohoon; (644 pag.)WO2017/18803; (2017); A1;,
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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.

To a stirring solution of 2-methylpiperazine 7 (3 g, 30.00 mmol) in CH2C12 (100 mL) under argon atmosphere were added triethylamine (9 mL, 90.00 mmol) and Boc-anhydride (7.2 mL, 33.00 mmol) at 0 ¡ãC; warmed to RT and stirred for 16 h. The reaction was monitored by TLC; after completion of the reaction, the volatiles were removed in vacuo. The crude was washed with -pentane (2 x 20 mL) and dried in vacuo to afford compound 9 (5 g, 83percent) as off- white solid. TLC: 5percent MeOH/ CH2C12 (R/. 0.4); 1H-NMR (OMSO-d6, 400 MHz): delta 3.80- 3.62 (m, 2H), 3.27-3.09 (m, 2H), 2.83-2.71 (m, 2H), 2.37-2.17 (m, 1H), 1.39 (s, 9H), 0.92 (d, J= 6.3 Hz, 3H)., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION; ARNOLD, Lee Daniel; MAAG, Hans; TURNER, JR., William W.; (274 pag.)WO2016/168619; (2016); A1;,
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109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture of 2a (1.9 g, 8.8 mM), morpholine (1.1 mL, 13.2 mM) and triethylamine (1.8 mL, 13.2 mM) were heated to reflux in THF for 2 h. The mixture was partitioned between ethyl acetate (60¡Á2 mL) and water (40¡Á2 mL), the organic layer was evaporated. The oily residue 3a utilized as materials without further purification., 109-01-3

As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Article; Wang, Lu; Zhang, Qing; Zhu, Gaoyuan; Zhang, Zhimin; Zhi, Yanle; Zhang, Li; Mao, Tianxiao; Zhou, Xiang; Chen, Yadong; Lu, Tao; Tang, Weifang; European Journal of Medicinal Chemistry; vol. 130; (2017); p. 86 – 106;,
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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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

The product was prepared according to General Procedure 1 using 8-tert-butyl- 6-(4,4-difluorocyclohexyl)imidazo [1 ,2-b]pyridazine-2-carboxylic acid (500 mg, 1.482 mmol), DMF (10 mL), HATU (845.3 mg, 2.223 mmol), Huenig?s base (775 tL, 4.449 mmol) and tert-butyl 3,3-dimethylpiperazine-1-carboxylate (476.4 mg, 2.223 mmol Purification by flash chromatography on silica gel was carried out under standard condition to afford title compound tert-butyl 4-[8-tert-butyl-6-(4,4-difluorocyclohexyl)imidazo [1 ,2-b]pyridazine-2- carbonyl]-3,3-dimethyl-piperazine-1-carboxylate (766 mg, 1.435 mmol, 96.85%) as a white solid. ?H NMR (400 MHz, Chloroform-cl) oe 8.23 (s, 1H), 6.72 (s, 1H), 4.31 (t, J= 6.3 Hz, 2H), 3.68-3.34 (m, 4H), 2.81 (t, J= 10.9 Hz, 1H), 2.24 (dt, J= 12.3, 7.2 Hz, 2H), 2.12 -1.72 (m, 6H), 1.59 (s, 6H), 1.52 (t, J= 1.9 Hz, 9H), 1.47 (d, J= 1.7 Hz, 9H). LC-MS: 534.26 (M+Hj., 259808-67-8

259808-67-8 1-Boc-3,3-Dimethylpiperazine 22710387, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; VERTEX PHARMACEUTICALS INCORPORATED; FARMER, Luc J.; FOURNIER, Pierre-Andre; LESSARD, Stephanie; LIU, Bingcan; ST-ONGE, Miguel; STURINO, Claudio; SZYCHOWSKI, Janek; YANNOPOULOS, Constantin; WO2015/48245; (2015); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

A suspension of 2-chloro-/V-methyl-/V-(4-nitrophenyl)acetamide (1.0 g, 4.37 mmol) in ethyl acetate (10 mL) was heated to 40 C for 30 min and added l-methylpiperazine (1.2 mL, 10.9 mmol) at the same temperature. The mixture was stirred at 50 C for 2 h. The reaction mixture was cooled to RT and diluted with ethyl acetate. The solution was washed with water and dried over anhydrous sodium sulfate. The solution was filtered, concentrated and diluted with methanol. The solution was subjected to hydrogenation in the presence of palladium on carbon as catalyst under 25 bar of hydrogen pressure at 25 C for 2 h. The catalyst was removed by filtration and the solvent was evaporated at 60 C to yield 400 mg of the desired compound. 1 H NMR (400 MHz, DMSO-de) d 1.88 (s, 3H), 2.14-2.19 (m, 4H), 2.63-2.68 (m, 4H), 2.80 (s, 2H), 3.01 (s, 3H), 5.20 (br s, 2H), 6.53 (d, J= 8.1 Hz, 2H), 6.88 (d, J= 8.7 Hz, 2H)., 109-01-3

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

Reference£º
Patent; ICHNOS SCIENCES S.A.; CHAUDHARI, Sachin, Sundarlal; GHARAT, Laxmikant, Atmaram; IYER, Pravin; DHONE, Sachin, Vasantrao; ADIK, Bharat, Gangadhar; WADEKAR, Prashant, Dilip; GOWDA, Nagaraj; BAJPAI, Malini; (233 pag.)WO2020/70331; (2020); A1;,
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Piperazines – an overview | ScienceDirect Topics

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

General procedure: A suitable commercial phenylpiperazine (2.00-5.10 mmol), K2CO3 (0.9-2.00 g) and acetone (7-16 mL) were stirred and refluxed for 30 min. Then, correspondingly substituted bromopentyl 3-benzyl-5,5-hydantoin derivatives 37-39 (2.20-5.70 mmol) in acetone (9-20 mL) were added and the mixture was refluxed for 6 h, left at room temperature overnight and separated from the inorganic precipitate by filtration. The solvent was evaporated from the filtrate. The pure product (14a-24a) was obtained from the residue using method C or D.

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

Reference£º
Article; Handzlik, Jadwiga; Bojarski, Andrzej J.; Sata?a, Grzegorz; Kubacka, Monika; Sadek, Bassem; Ashoor, Abrar; Siwek, Agata; Wi?cek, Ma?gorzata; Kucwaj, Katarzyna; Filipek, Barbara; Kie?-Kononowicz, Katarzyna; European Journal of Medicinal Chemistry; vol. 78; (2014); p. 324 – 339;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 10 RRN No.442(R)-tert-Butyl 4-(4-amino-1-methyl-1H-pyrazol-5-yl)-3-methylpiperazine-1-carboxylate [0401] 5-chloro-1-methyl-4-nitro-1H-pyrazole from Example 1 (355 mg, 2.2 mmol) and potassium fluoride (511 mg, 8.8 mmol) in dry DMSO (20 mL) was added (R)-tert-butyl 3-methylpiperazine-1-carboxylate (507 mg, 2.53 mmol) and the mixture was heated in the microwave at 100 C. for 10 hr. The mixture was partitioned between water (40 mL) and EtOAc (100 mL) and the organic layer passed through a phase separation cartridge and concentrated under reduced pressure. Purification via silica gel column chromatography (0-100% EtOAc/isohexane) gave (R)-tert-butyl 3-methyl-4-(1-methyl-4-nitro-1H-pyrazol-5-yl)piperazine-1-carboxylate as an orange gum (627 mg). To a solution of this gum (179 mg, 0.55 mmol) and ammonium formate (256 mg, 4.4 mmol) in MeOH (10 mL) under nitrogen was added 10% palladium on carbon (59 mg, 0.55 mmol). The mixture was heated at 70 C. for 4 hr before being cooled, filtered and concentrated under reduced pressure. The residue was partitioned between water (20 mL) and DCM (60 mL) and the organic layer separated, passed through a phase separation cartridge and concentrated under reduced pressure to give (R)-tert-butyl 4-(4-amino-1-methyl-1H-pyrazol-5-yl)-3-methylpiperazine-1-carboxylate as a brown gum (150 mg, 80% over two steps). LCMS (ES+) m/z 296 (M+1)., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; GENENTECH, INC.; Hodges, Alastair James; Matteucci, Mizio; Sharpe, Andrew; Sun, Minghua; Wang, Xiaojing; Tsui, Vickie H.; US2013/79321; (2013); A1;,
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Piperazines – an overview | ScienceDirect Topics

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 5; Preparation of Quetiapine from ll-piperazinyldibenzo[b,f][l,4]thiazepine; [0040] 33.1 g of extra fine potassium carbonate is added to the r¡ã-butanol solution of 1 l-piperazinyldibenzo[b,fj[l54]thiazepine with continuous stirring. Then, 16.48 g of sodium iodide and 35.97 g of 2-(2-chloroethoxy)ethanol are respectively added with stirring. With continued mixing, the reaction mixture is heated to a temperature of 102 C and maintained at that temperature for 12 – 16 hours. The conversion of 11- piperazinyldibenzo[b,fj[l,4]thiazepine to quetiapine can be monitored by HPLC analysis. Once the conversion of is complete, the reaction mixture is cooled to a temperature of less than about 80 0C and about 500 g of water is added to adjust the reaction mixture to a temperature of about 40 – 50 C and the mixing is continued for at least about 30 minutes. The biphasic mixture is transferred to a separatory funnel and the aqueous and organic phases are allowed to separate. The lower aqueous phase is isolated and discarded. The upper organic phase containing crude quetiapine is transferred to a flask. Another 25O g of water is added to the quetiapine solution and the reaction mixture is stirred at a temperature of about 40 – 50 C for at least 30 additional minutes. The biphasic mixture is again transferred to a separatory funnel and the aqueous and organic phases are allowed to separate. The lower aqueous phase is removed and discarded. The upper organic phase containing crude quetiapine is recovered and transferred to a flask and distillation setup suitable for vacuum distillation to azeotropically remove water. Vacuum is applied to the distillation setup as the solution is heated, possibly to a temperature as high as 55 – 65 C at the end of the distillation, to remove water. The distillation is continued until no more water is observed collecting in the collection trap. The still bottoms may be checked by KF moisture analysis; the amount of KF water should be less than 0.5% by weight. Once the distillation is complete, the crude quetiapine solution is cooled to a temperature of less than 30 0C., 5747-48-8

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CAMBREX CHARLES CITY, INC.; WO2006/135544; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics