Heterocyclic Building Blocks-piperazine

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

General procedure: To a stirred solution of compound 13a-b, 17a-b (1.0 mmol) inCH3CN (20 mL) were added N-Boc-piperazine (180.9 mg,0.9 mmol), K2CO3 (205.9 mg, 1.5 mmol), KI (166.0 mg, 1.0 mmol)and 18-crown-6 (26.4 mg, 0.1 mmol) at room temperature. Themixture was stirred overnight at 80 C and filtered. The filtrate wasdiluted by DCM and washed by brine. The organic layer was concentrated for next step. To a stirred solution of the abovecompounds in DCM (20 mL) was added TFA (3 mL) at room temperature.The mixture was stirred for 3e4 h and concentrated toafford the crude products 15a-o and 19a-f in a yield of 35%e42%. Toa stirred solution of above crudes in anhydrous MeOH (10 mL) wasadded BTZ core compound 11 (403.2 mg, 1.0 mmol) and Et3N(0.2 mL, 1.5 mmolj) at room temperature. The mixture was stirredfor 1e3 h at 40 C and concentrated. The residue was purified bysilica gel column (DCM: MeOH 20: 1) to give 1a-f and 2a-e (25%e41% for two steps)., 639068-43-2

639068-43-2 tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 22219990, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Wang, Apeng; Lv, Kai; Tao, Zeyu; Gu, Jian; Fu, Lei; Liu, Mingliang; Wan, Baojie; Franzblau, Scott G.; Ma, Chao; Ma, Xican; Han, Bing; Wang, Aoyu; Xu, Shijie; Lu, Yu; European Journal of Medicinal Chemistry; vol. 181; (2019);,
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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.

To a solution of 4,6-dichloro-2-methylpyrimidine (3.00 g) in dichloromethane (35 mL) was added 2-(piperazin-1-yl)ethanol (4.51 mL) at room temperature, and the mixture was stirred for 4 hr. To the reaction mixture was added triethylamine (0.513 mL) at room temperature, and the reaction mixture was stirred overnight. The resulting solid was collected by filtration, washed with dichloromethane, and dried under reduced pressure to give the title compound (4.08 g). 1H NMR (400 MHz, CDCl3) delta 2.48 (3H, s), 2.55-2.63 (6H, m), 3.63-3.73 (6H, m), 6.34 (1H, s)

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

Reference£º
Patent; Takeda Pharmaceutical Company Limited; NAGAMIYA, Hiroyuki; YOSHIDA, Masato; SETO, Masaki; MARUI, Shogo; ODA, Tsuneo; ISHICHI, Yuji; SUZUKI, Hideo; KUSUMOTO, Tomokazu; YOGO, Takatoshi; RHIM, Chul Yun; YOON, Cheolhwan; LEE, Gil Nam; KANG, Hyun Bin; KIM, Kwang Ok; JEON, Hye Sun; EP2818473; (2014); A1;,
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59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, EXAMPLE 202; 4-{7-[2-(4-Methyl-3-oxo-piperazin-1-yl)-ethoxy]-quinazolin-4-yl}-piperidine-1-carboxylic acid (4-pyrrolidin-1-yl-phenyl)-amide; To a solution of 4-[7-(-hydroxy-ethoxy)-quinazolin-4-yl]-piperidine-1-carboxylic acid tert-butyl ester (0.5 mmol), prepared as described in Example 169a, in anhydrous DCM, was added Et3N (1 mmol) and methanesulfonyl chloride (1 mmol) and the mixture was stirred at rt for 2 h. It was then washed with water (3.x.), dried over anhydrous MgSO4, filtered and concentrated in vacuo to obtain crude 4-[7-(3-methanesulfonyloxy-ethoxy)-quinazolin-4-yl]-piperidine-1-carboxylic acid tert-butyl ester. This (0.1 mmol) was dissolved in anhydrous DMSO together with 1-methyl-piperazin-2-one (0.2 mmol) and the mixture was stirred at 100¡ã C. for 2 h and then diluted with water and extracted with DCM. The DCM extract was washed with water (3.x.), dried over anhydrous MgSO4, filtered and concentrated in vacuo. To this was added 3M HCl/MeOH (1 mL) and the mixture was stirred at rt for 2 h and then concentrated in vacuo and the residue was dissolved in a 1:1 mixture of DCM:MeOH, neutralized with excess Et3N and treated with (4-pyrrolidin-1-yl-phenyl)-carbamic acid 4-nitrophenyl ester hydrochloride (0.11 mmol), as prepared by the method outlined in Example 74a. The mixture was stirred at rt overnight and then concentrated in vacuo and partitioned between water and DCM. DCM layer was drawn off, washed with water thrice, then dried over anhydrous MgSO4, filtered and concentrated in vacuo. The residue was purified by Preparative TLC (silica gel; DCM:MeOH, 95:5) followed by a further purification by Preparative HPLC to obtain 5.6 mg (6percent) of the title compound. 1H-NMR (300 MHz, CD3OD): 9.10 (s, 1H), 8.44 (d, 1H), 7.59-7.31 (m, 6H), 4.62 (t, 2H), 4.37 (m, 2H), 4.04-3.93 (m, 4H), 3.78-3.54 (m, 8H), 3.21 (m, 2H), 3.03 (s, 3H), 2.30-2.18 (m, 5H), 2.11-1.91 (m, 4H). LC/MS (ESI): 558.3 (MH)+.

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Baindur, Nand; Gaul, Michael David; Kreutter, Kevin Douglas; Baumann, Christian Andrew; Kim, Alexander J.; Xu, Guozhang; Tuman, Robert W.; Johnson, Dana L.; US2006/281772; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.393781-70-9,(R)-1-Boc-2-Ethylpiperazine,as a common compound, the synthetic route is as follows.

Step A: To a solution of (R)-tert-butyl 2-ethylpiperazine-l-carboxylate (0.208 g, 0.971 mmol, Eq: 1.00) and triethylamine (0.135 ml, 0.971 mmol, Eq: 1.00) in DMF (2ml) was added methyl 2,6- dichloronicotinate (0.200 g, 0.971 mmol, Eq: 1.00) and the reaction mixture stirred at 30C for 4.5 hrs. The reaction mixture was diluted with EtOAc and washed with water and brine, the organic phase was dried over Na2S04 and the solvent evaporated. The crude was purified by column chromatography (Si02, EtOAc/Heptane, 1/4) to give 160 mg (43%) of tert-butyl (2R)-4- (6-chloro-5-methoxycarbonyl-2-pyridyl)-2-ethyl-piperazine-l-carboxylate as a white solid. MS (m/e): 384.2 (M+H+)., 393781-70-9

As the paragraph descriping shows that 393781-70-9 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; GREEN, Luke; PINARD, Emmanuel; RATNI, Hasane; WILLIAMSON, Patrick; (95 pag.)WO2015/197503; (2015); A1;,
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31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 250 ml round bottomed flask 5-(3-(1-hydroxyethyl)-1-oxo-1H-isochromen-4-yl)thiophene-2-carbaldehyde (Intermediate B37) (780 mg, 2.60 mmol) was dissolved in 30 ml of DCM then acetic acid (0.446 ml, 7.79 mmol) and benzyl piperazine-1-carboxylate (1.503 ml, 7.79 mmol) were added. After few minutes sodium triacetoxyhydroborate (2.75 g, 12.99 mmol) was added and the mixture was stirred at r.t. The mixture was poured into 100 ml of DCM and 100 NaHCO3 sat. sol. then phases were separated and the organic one was concentrated to dryness to leave a brown oil that was immediately purified by chromatography eluting with HexaneEtOAc mixtures to leave the title compound (903 mg, 1.790 mmol, 68.9percent yield) as a yellow oil.UPLC-MS: 0.79 min, 505.12 [M+H]+, method 9, 31166-44-6

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; CHIESI FARMACEUTICI S.p.A.; Biagetti, Matteo; Capelli, Anna Maria; Accetta, Alessandro; Carzaniga, Laura; US2015/166549; (2015); A1;,
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75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,75336-86-6

Step IA: A mixture of (R)-2-methyl-piperazine (25.0 g, 250 mmol), 2-bromo 5- fluoro benzotrifluoride (55.1 g, 227 mmol), tris(dibenzylidineacetone)dipalldium (0) (2.08g, 2.27 mmol), rac-2,2′-bis(diphenylphosphino)-l,r-binaphthyl (4.24 g, 6.81 mmol) and sodium tert-butoxide (27.3 g, 280 mmol) was mixed and purged with N2. Anhydrous toluene (500 mL) was added and purged with N2 again. The resulting mixture was heated in an oil bath at 105 0C under N2 for 3.5 hours. After cooling, the reaction mixture was concentrated and then filtered through a pad of Celite, washed with Et2O. The organic layer was concentrated, diluted with Et2O (500 mL), filtered through a pad of Celite again, and washed with IN aq. HCl (2 x 150 mL). The aqueous layer was basified with NaOH at 0 0C (pH = -10) and then was extracted with Et2O (3 x 200 mL). The combined organic layer was dried over MgSO4 and concentrated under vacuum to give (3i?)-l-[4- fluoro-2-(trifluoromethyl)phenyl]-3-methylpiperazine as a brown oil (58.5 g, 98percent), which was used without further purification.

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

Reference£º
Patent; WYETH LLC; WAN, Zhao-Kui; CHENAIL, Eva; IPEK, Manus; LI, Huan-Qiu; MANSOUR, Tarek, Suhayl; SURI, Vipin; XIANG, Jason, Shaoyun; SAIAH, Eddine; WO2010/141550; (2010); A2;,
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438631-77-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.438631-77-7,(R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a de-gassed solution of 78 THF (325 ml) and 56 DIPEA (12.74 ml, 73.14 mmol) under a nitrogen atmosphere was added 113 7-bromo-4,6-dichloro-8-fluoro-3-nitroquinoline (26.59 g, 66.49 mmol) and 272 1-(tert-butyl) 3-methyl (R)-piperazine-1,3-dicarboxylate (17.05 g, 69.81 mmol). The resultant brown solution was heated at 61 C. (internal temperature) under a nitrogen atmosphere for 18 hours. Additional DIPEA (5.8 ml, 33.24 mmol) and 1-(tert-butyl) 3-methyl (R)-piperazine-1,3-dicarboxylate (8.12 g, 33.24 mmol) was then added and the resultant reaction mixture was heated at 61 C. (internal) for 4 hours. The reaction mixture was concentrated in vacuo, and the crude product was purified by flash silica chromatography, elution gradient 0 to 50% 57 ethyl acetate in 58 heptane. Pure fractions were evaporated to dryness to afford 273 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6-chloro-8-fluoro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (32.1 g, 88%) as an orange solid. 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 2.52-2.53 (1H, m), 3.29-3.34 (1H, m), 3.56 (3H, s), 3.61-3.77 (2H, m), 3.78-3.93 (1H, m), 4.04-4.21 (1H, m), 4.33-4.4 (1H, m), 8.36 (1H, d), 9.16 (1H, s). m/z: ES+ [M+H]+ 547. 97% ee.

As the paragraph descriping shows that 438631-77-7 is playing an increasingly important role.

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;,
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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.

2,3,7-Trichloropyrido[2,3-b]pyrazine (200.0 mg, 0.85 mmol) and TEA (1180.0 muL, 8.53 mmol) were dissolved in DCM (8.5 mL), and (S)-tert-butyl 2-methylpiperazin-1-carboxylate (187.8 mg, 0.94 mmol) diluted in DCM (0.5 mL) was slowly added thereto at -20 C. The reaction mixture was stirred at -20 C. for 12 hours, and it was poured into saturated NH4Cl aqueous solution and extracted with DCM (30.0 mL). The organic layer was washed with brine, dried over anhydrous Na2SO4, filtered and then distilled under reduced pressure. The residue was purified by column chromatography (EtOAc:n-Hex=30:70) on silica. The fractions containing the product were collected and evaporated to obtain yellow solid compound of (S)-tert-butyl 4-(2,7-dichloropyrido[2,3-b]pyrazin-3-yl)-2-methylpiperazin-1-carboxylate (233.0 mg, 67%). [0544] LCMS ESI(+): 398 (M+1), 400 (M+3) [0545] 1H-NMR (300 MHz, DMSO-d6); delta: 8.96 (d, 1H, J=2.7 Hz), 8.54 (d, 1H, J=2.7 Hz), 4.30 (m, 1H), 4.09 (m, 2H), 3.88 (m, 1H), 3.20 (m, 2H), 3.04 (m, 1H), 1.43 (s, 9H), 1.24 (d, 3H, J=6.6 Hz)

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

Reference£º
Patent; C&C RESEARCH LABORATORIES; Ho, Pil Su; Yoon, Dong Oh; Han, Sun Young; Lee, Won Il; Kim, Jung Sook; Park, Woul Seong; Ahn, Sung Oh; Kim, Hye Jung; US2014/315888; (2014); A1;,
Piperazine – Wikipedia
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1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoic acid (5) was synthesized by the method reported. [Nat Med. 2013, 19(2): 202-8] To a solution of compound 5 (100 mg, 0.175 mmol) in anhydrous dichloromethane, compound 4g (68 mg, 0.175 mmol), EDCI (167 mg, 0.875 mmol) and DMAP (25.6 mg, 0.21 mmol) were added. Afterwards, the mixture solution was stirred for 24 h at room temperature. Completion of the reaction was confirmed by TCL. The reaction mixture was washed with HCl (1 M), NaHCO3 saturated solution and brine, concentrated and purified to afford 6g (160 mg, 85% yield) as a yellow solid., 1235865-77-6

1235865-77-6 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid 66713100, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Zhou, Ruolan; Fang, Shaoyu; Zhang, Minmin; Zhang, Qingsen; Hu, Jian; Wang, Mingping; Wang, Chongqing; Zhu, Ju; Shen, Aijun; Chen, Xin; Zheng, Canhui; Bioorganic and Medicinal Chemistry Letters; vol. 29; 3; (2019); p. 349 – 352;,
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129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (500 mg, 2.04 mmol) and an ammonia methanol solution (7 M, 10mL) in a 100 mL of sealing tube was stirred at 60 for 72 h and concentratedto give the title compound as a white solid (200 mg, 42) . 1H NMR (400 MHz, CD3OD): delta ppm 5.47-5.76, 6.11-6.36 (m, 0.5H, 0.5H) , 4.51-4.68 (m, 1H) , 3.44-3.57(m, 1H) , 2.89-3.02 (m, 2H) , 2.66-2.80 (m, 2H) , 1.47 (m, 9H) and MS-ESI:m/z 230.30 [M+H] +., 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
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