Heterocyclic Building Blocks-piperazine

112984-60-8, 6-Fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of DCC (0.9 g, 4.3 mmol)in DMF (20 ml), BOC-glycine (0.5 g, 2.85 mmol) and hydroxybenzotriazole (HOBt, 0.5 g, 4.3mmol) were added at 0 C and the mixture was allowed to stir for 4 h, followed by addition of 6-fluoro- 1 -methyl-7-(4-((5-nitro- 1H-benzo[d]imidazol-2-yl)methyl)piperazin- 1 -yl)-4-oxo- 1H,4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (0.9 g, 2.85 mmol) and triethylamine (0.4 g, 0.6 ml 4.3 mmol) at 0 C. The reaction mixture was allowed to stir for overnight at room temperature. After completion, the final solution was then concentrated under reduced pressure to obtain the crudeproduct which was purified by flash column chromatography over silica gel using 3% methanolDCM as eluent to afford compound A as pale yellow solid (0.75g, yield: 65%).1H NMR (DMSO-d6):oe 14.62 (brs, 1H, COOH), 7.84 (d, 1H, JAB = 14.0 Hz, ArH), 6.95 (d, 1H, JAB = 7.0 Hz, ArH), 6.81 (t, 1H, JAB = 6.0 Hz, NH), 6.39 (q, 1H, JAB = 6.5 Hz, SCHN), 3.85 (d, 2H, JAB = 6.0 Hz, CH2), 3.64-3.56 (m, 4H, CH2N), 2.12 (d, 3H, JAB = 6.0 Hz, CH3). ESI-MS (mlz): 495.16 (M+H).

112984-60-8, The synthetic route of 112984-60-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; VYOME BIOSCIENCES PVT. LTD.; SENGUPTA, Shiladitya; GHOSH, Shamik; GHOSH, Sumana; SINHA, Mau; SADHASIVAM, Suresh; BHATTACHARYYA, Anamika; MAVUDURU, Siva Ganesh; TANDON, Nupur; KUMAR, Deepak; (149 pag.)WO2017/17631; (2017); A2;,
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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

109-01-3, The 1-(3-hydroxypropy)-4-methylpiperazine used as a stating material was prepared as follows: [00740] A mixture of 3-bromopropanol (20 ml), N-methylpiperzine (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).

The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AstraZeneca UK Limited; US6806274; (2004); B1;,
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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

A mixture 2,3-dichloro-pyrazine (5.0 g, 34 mmol), 1-isopropylpiperazine (6.5 g, 51 mmol) and potassium carbonate (7.0 g, 51 mmol) in acetonitrile (100 mL) was stirred at ambient temperature for 2 h. Addition of hexane, followed by filtration and concentration of the filtrate gave 9.5 g of crude material as an orange liquid. Purification by filtration through silica using heptane/EtOAc (3: 1), followed by EtOAc/acetone (1: 1), provided 6.5 g (79percent) of the title compound as a yellow oil which solidified upon cooling. HPLC purity: 98percent. MS m/z 241 (M+H) +. HRMS m/z calcd for C11H17ClN4 (M) + 240.1142, found 240.1138.

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

Reference：
Patent; BIOVITRUM AB; WO2004/9586; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5464-12-0,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.

A 250 ml three-necked flask equipped with a thermometer, a condenser, a bubble counter and a dropping funnel, and with magnetic stirring, is charged with 60 ml of THF and 7.9 g (50.94 mmol) of 2-(4-methylpiperazin-1 -yl)ethanol. The solution obtained is cooled to zero degrees and 2.04 g (50.94 mmol) of sodium hydride are gently added at this temperature. Stirring is continued at zero degrees for 1 hour. A solution of 7.9 g (42.45 mmol) of 1 -fluoro-2,4-dinitrobenzene and of 70 ml of THF, cooled beforehand to zero degrees, is then added dropwise to the previous medium. The reaction is monitored by TLC, elution being carried out with MeOH/CH2CI2. After stirring overnight at ambient temperature, the solvent is eliminated by evaporation under vacuum until a brown-yellow solid is obtained which, via purification by silica column flash chromatography (CH2Cl2/MeOH) gives, after evaporation of the solvent, a brown solid with a mass of 8.39 g (63.7percent yield) corresponding to the expected compound.

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

Reference：
Patent; L’OREAL; FADLI, Aziz; WO2014/26952; (2014); 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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

70261-82-4, A. 8-Indan-5-yl-2-[4-(4-methyl-piperazin-1-ylmethyl)-phenylamino]-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester 8-indan-5-yl-2-methanesulfonyl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester (0.098 g, 0.24 mmol) and 4-(4-methyl-piperazin-1-ylmethyl)-phenylamine (0.049 g, 0.24 mmol) were combined in i-PrOH (2 mL) and heated to 90 C. After 3 h, the reaction mixture was concentrated and purified by preparative HPLC (30 mL/min 5-100% MeCN/H2O gradient over 10 min) and lyophilized to provide 20 mg of 8-Indan-5-yl-2-[4-(4-methyl-piperazin-1-ylmethyl)-phenylamino]-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester. 1H NMR (400 MHz, CDCl3) delta (ppm): 9.36 (s, 1H), 8.54 (s, 1H), 7.43 (d, 2H, J=7.9 Hz), 7.29 (m, 2H), 7.18 (dd, 2H, J=2.0 Hz, J=7.9 Hz), 7.03-7.05 (m, 1H), 4.38 (q, 2H, J=7.1 Hz), 3.44 (s, 2H), 3.08 (t, 2H, J=7.4 Hz), 3.01 (t, 2H, J=7.5 Hz), 2.52 (br s, 8H), 2.36 (s, 3H), 2.19-2.29 (m, 2H), 1.39 (t, 3H, J=7.1 Hz).

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Player, Mark R.; Huang, Hui; Hutta, Daniel A.; US2007/60577; (2007); A1;,
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Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of 3-iodo-4-methylbenzoyl chloride obtained above in dry DCM (10mL) at 0C was added Et3N (0.28mL, 2.0mmol) and 4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) aniline (328mg, 1.2mmol). The mixture was stirred at room temperature for 5h, and then the solvent was removed under reduced pressure. The residue was purified by using column chromatography to afford the corresponding product 6-1 (439mg, 2 steps yield: 85%)., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Liu, Yang; Peng, Xia; Guan, Xiaocong; Lu, Dong; Xi, Yong; Jin, Shiyu; Chen, Hui; Zeng, Limin; Ai, Jing; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 122 – 132;,
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Piperazines – an overview | ScienceDirect Topics

77279-24-4,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.77279-24-4,tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Weigh the compound 10 (8.7 g, 37.8 mmol) in anhydrous tetrahydrofuran (THF)Then, dimethylaminopyridine DMAP (0.23 g, 1.9 mmol) and triethylamine (4.9 g, 49 l lm) were added; methanesulfonyl chloride (5.2 g, 45.3 mml) was added dropwise to the ice bath After the completion of the solution slowly rose to room temperature for 5h; TLC detection, iodine cylinder color; until the raw material disappeared after adding a small amount of ice water quenching, recovery solvent was crude, silica gel column chromatography (petroleum ether / ethyl acetate) 3.9 g)

As the paragraph descriping shows that 77279-24-4 is playing an increasingly important role.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Yang Chunhao; Miao Zehong; Yue Zhizhou; Liang Yukun; Feng Jianming; Li Jiaxin; He Qian; (30 pag.)CN104250246; (2017); B;,
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.

To a solution of tert-butyl (2S)-2- methylpiperazine-l-carboxylate (400 mg, 2.00 mmol) in dichloromethane (6 mL) was added acetic acid (120 mg, 2.0 mmol) and 5-cyclopropyl-3-(2,6-dichlorophenyl)-l,2-oxazole-4- carbaldehyde (562 mg, 1.99 mmol). After the mixture was stirred for 30 min, NaBH(OAc)3 (1.3 g, 6.13 mmol) was added. The resulting solution was stirred overnight at room temperature. The solids were filtered out. The resulting mixture was concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (30:70). This resulted in 670 mg (72%) of the title compound as a white solid. LC-MS (ESI, m/z): [M+H]+ = 466.2., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; HEPAGENE THERAPEUTICS, INC.; XU, Xiaodong; (104 pag.)WO2018/85148; (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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of terf-butyl 4-carbamothioylpiperazine-1-carboxylate (synthesized according to Example 5, Step 1, 3.0 g, 12 mmol) in dioxane (10 mL), TEA (2.6 mL, 16 mmol) and 3-bromo-ethyl pyruvate (2.1 mL, 16 mmol) were added at rt and the mixture was stirred at 90 C for 16 h. The completion of the reaction was monitored by TLC. The reaction mixture was quenched with water and extracted with EtOAc. The organic layer was dried over anhydrous Na2SO4, concentrated under vacuum and the resulting crude product was taken as such for next step. Yield: 95% (4 g, black solid).

196811-66-2, As the paragraph descriping shows that 196811-66-2 is playing an increasingly important role.

Reference：
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(c) 4-Methyl-N-(4-((4-methylpiperazin-l-yl)methyl)phenyl)-3-(4-phenylpyrimidin-2- ylamino)benzamide[0071] DIEA (50muL, 0.204mmol) was added into a solution of 3-bromo-4- methylbenzoic acid (15mumg, 0.049mmol), 4-((4-methylpiperazin-l-yl)methyl)benzenamine (9mg, 0.04mmol), BOP (25mg, 0.057mmol) in DMF. The reaction mixture was stirred at rt under argon atmosphere overnight. The reaction mixture was then purified by a semi- preparative HPLC to give pure product as white powder. MS (ESI+) m/z 493.2 [M+H]+.

70261-82-4, As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference：
Patent; INTRA-CELLULAR THERAPIES, INC.; WO2008/153959; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics