Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Part II – Synthesis of [(S)-4-(3-chloro-benzenesulfonyl)-2-(4-methyl-3-oxo-piperazin-l- ylmethyl)-3,4-dihydro-2H-benzo[l,4]oxazin-6-yl]-carbamic acid tert-butyl ester [0340] A suspension of 3-chloro-benzenesulfonic acid (i?)-6-tert-butoxycarbonylamino-4-(3- chloro-benzenesulfonyl)-3,4-dihydro-2H-benzo[l,4]oxazin-2-yl methyl ester (63 mg, 0.1 mmol), N, N-diisopropylethylamine (0.2 mmol), l-methyl-piperazin-2-one, hydrochloride salt (30 mg, 0.2 mmol) and potassium iodide (5 mg) in THF (0.5 mL) and N-methyl pyrrolidinone (0.5 mL) was heated in a sealed tube for 12 hours at 80 C. After cooling, the mixture was partitioned between water and ethyl acetate. The organic layer was separated, washed with brine, saturated aqueous NaHC03 and concentrated. The residue was purified by column chromatography on silica gel to provide [(5)-4-(3-chloro-benzenesulfonyl)-2-(4- methyl-3-oxo-piperazin-l-ylmethyl)-3,4-dihydro-2H-benzo[l,4]oxazin-6-yl]-carbamic acid tert-butyl ester. LCMS (ESI) m/z 551., 109384-27-2

The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; LYCERA CORPORATION; AICHER, Thomas; BARR, Kenneth; LAPOINTE, Blair; SIMOV, Vladimir; STEIN, Karin; THOMAS, William; TOOGOOD, Peter; VAN HUIS, Chad; WHITE, Catherine; WO2013/169704; (2013); A2;,
Piperazine – Wikipedia
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59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The appropriate piperazine derivative (1.34mmol) and K2CO3 (180mg, 1.34mmol) were added to a solution of the appropriate 3-(4-(n-iodoalkoxy)phenyl)thiazolidine-2,4-dione (11, 0.67mmol) in MeCN (6mL). The reaction mixture was stirred at room temperature for 9h. The mixture was quenched by addition of water and extracted with DCM. The organic layer was dried over anhydrous MgSO4, filtered and evaporated under reduced pressure. The residue was purified by column chromatography (SiO2, DCM/MeOH= 15/1 v/v including 1% of NH4OH).

59878-57-8, As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference：
Article; Elkamhawy, Ahmed; Kim, Nam youn; Hassan, Ahmed H.E.; Park, Jung-eun; Yang, Jeong-Eun; Oh, Kwang-Seok; Lee, Byung Ho; Lee, Mi Young; Shin, Kye Jung; Lee, Kyung-Tae; Hur, Wooyoung; Roh, Eun Joo; European Journal of Medicinal Chemistry; vol. 157; (2018); p. 691 – 704;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a N-(tert-Butoxycarbonyl)-1-(2-hydroxyethyl)piperazine To a solution of 1-(2-hydroxyethyl)piperazine (5.20 g, 40 mmol) and triethylamine (6 mL) in 1,4-dioxane (100 mL) was added slowly di-tert-butyl dicarbonate (8.72 g, 40 mmol). The reaction mixture was stirred at room temperature for 2 h. The solvent was removed in vacuo and the residue was purified by flash column chromatography (ethyl acetate to 2% methanol in ethyl acetate) to give the title compound as a colorless oil (8.32 g, 90%). 1 H-NMR (300 MHz, CDCl3) delta 1.46 (s, 9H), 2.46 (t, 4H), 2.55 (t, 2H), 2.75 (bs, 1H), 3.44 (t, 4H), 3.63 (t, 2H)., 103-76-4

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

Reference：
Patent; 3-Dimensional Pharmaceuticals, Inc.; US5792769; (1998); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a suspension of methyl (Z)-1-acetyl-3-(ethoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate (6) (500 mg,1.368 mmol) in DMF (3.5 mL) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (14) (395 mg,1.505 mmol, 1.1 equiv.) at RT. After heating the reaction mixture at 80 C for 1 h, it was allowed to cool to RT. Piperidine (297 lL,3.010 mmol, 2.2 equiv.) was then added and stirred for 2 h. Volatiles were removed in vacuo and water was added to the obtained residue and stirred for 15 min. The precipitate was then filtered under suction and cake was washed with water, then with minimum amount of cold methanol, and then ether. The obtained product was purified by column chromatography (neutral Al2O3,0-10% methanol in CH2Cl2) to afford 532 mg (72%) of target molecule 15.

262368-30-9, The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Edupuganti, Ramakrishna; Taliaferro, Juliana M.; Wang, Qiantao; Xie, Xuemei; Cho, Eun Jeong; Vidhu, Fnu; Ren, Pengyu; Anslyn, Eric V.; Bartholomeusz, Chandra; Dalby, Kevin N.; Bioorganic and Medicinal Chemistry; vol. 25; 9; (2017); p. 2609 – 2616;,
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Piperazines – an overview | ScienceDirect Topics

149057-19-2, 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

149057-19-2, Step 4 Synthesis of piperazine-1,2,4-tricarboxylic acid 4-benzyl ester 1-tert-butyl ester 2-methyl ester K2CO3 (910 mg, 6.6 mmol) was added to a stirred solution of piperazine-1,2,4-tricarboxylic acid 4-benzyl ester 1-tert-butyl ester (1.2 g, 3.3 mmol) in DMF (10 mL) at ambient temperature. To the above mixture was added at 0 C., CH3I (1.4 g, 9.9 mmol) and stirred 20 C. for 2 hr. The reaction mixture was diluted with cold water, extracted with ethyl acetate and dried over sodium sulphate, concentrated under reduced pressure to afford 1.2 g(96.4%) of piperazine-1,2,4-tricarboxylic acid 4-benzyl ester 1-tert-butyl ester 2-methyl ester.

149057-19-2 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 2756778, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Bischoff, Alexander; Subramanya, Hosahalli; Sundaresan, Kumar; Sammeta, Srinivasa Raju; Vaka, Anil Kumar; US2010/160323; (2010); A1;,
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Piperazines – an overview | ScienceDirect Topics

548762-66-9,548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (500 mg, 2.33 mmol) in dry acetonitrile (3.0 mL), were added 1-bromo-2-(bromo(4- fluorophenyl)methyl)benzene (883 mg, 2.57 mmol) and DIPEA (1.22 mL, 7.0 mmol) at room temperature. The reaction mixture was heated at 85 C for 24 h. The reaction mixture was cooled to room temperature and concentrated under reduced pressure to obtain the crude product, which was purified by Combi flash 12 g silica gel (2632) chromatography by using 0-100% ethyl acetate/petroleum ether as eluent to obtain tert- butyl (2S,5R)-4-((2-bromophenyl)(4-fluorophenyl)methyl)-2,5-dimethylpiperazine-1- carboxylate (0.45 g, 40 % yield). 1H NMR (300 MHz, CDCl3) d ppm 7.75-7.89 (m, 1H), 7.25-7.60 (m, 4H), 6.91-7.17 (m, 3H), 5.02 (d, J=9.6 Hz, 1H), 4.12 (m, 1H), 3.51-3.72 (m, 1H), 3.30 (m, 1H), 2.93 (m, 1H), 2.57-2.71 (m, 1H), 2.17-2.31 (m, 1H), 1.37-1.65 (m, 9H), 1.14-1.33 (m, 3H), 0.82-1.05 (m, 3H).

548762-66-9 (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate 11745988, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); 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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: Combine the product of Preparation 13, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Schering Corporation; US2004/220194; (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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

Pyrazine-2-carboxylic acid hydrochloride (2 g, 9.8 mmol)And (Boc) 2O (8.6 g, 39.4 mmol)Was dissolved in THF (40 mL) and water (40 mL)Sodium bicarbonate (8.31 g, 79.8 mmol) was added,The reaction mixture was stirred magnetically at room temperature for 4 hours and then added with ethyl acetate.Poured into a separatory funnel, and the separated organic phase was washed with saturated brine, dried over anhydrous sodium sulfate,The solvent was concentrated under reduced pressure and purified by silica gel column chromatography to obtain 2.5 g of 1,4-di-tert-butoxycarbonylpiperazine-2-carboxylic acid (13-2) in a yield of 78%

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Fujian Jinle Pharmaceutical Technology Co., Ltd.; Zhou Zhongxiang; Xing Yuanyuan; Chen Yingzhong; Deng Chengjun; Deng Honggui; Xue Wanhua; Zhang Shuzu; Chen Weipeng; Li Fang; (27 pag.)CN107174584; (2017); A;,
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.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of 6 or 7 (0.68-0.74 mmol) in 3 mL of n-BuOH kept in a PV with stirring, cyclic amines (1.02-1.11 mmol) was added. The sealed PV was placed in an oil bath at 145-150 C and stirred for 50-60 min. The solvent was evaporated in vacuo with the aid of DCM and the residue was re-dissolved in 2:1 EtOAc/DCM and washed successively with saturated NaHCO3 and NaCl solution (1 x 15 mL), respectively. The aqueous layer was washed with EtOAc (3 x 5 mL) and the organic layer was dried over anhydrous MgSO4 then filtered. The solution was evaporated in vacuo and purified using silica gel column chromatography with appropriate eluents (EtOAc/hexanes 3:1 and 1:3 v/v, respectively or 9:1 DCM/EtOAc) to afford either solid or semisolid products., 13484-40-7

As the paragraph descriping shows that 13484-40-7 is playing an increasingly important role.

Reference：
Article; Mohamed, Tarek; Yeung, Jacky C.K.; Rao, Praveen P.N.; Bioorganic and Medicinal Chemistry Letters; vol. 21; 19; (2011); p. 5881 – 5887;,
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 vial was charged with 5-amino-3,6-dichloro-l ,2,4-triazine (495.1 mg, 4.25 mmol) and triethylamine (1.5 mL, 10.76 mmol), 2,6-dimethylpiperazine (0.7054 g, 4.28 mmol) in dioxane (11 mL). The mixture was heated at 95 C for 1.5 h using microwave. The mixture was cooled to room temperature, filtered and the white solid was washed with dichloromethane. The organic solution was concentrated. The residue was dissolved in dichloromethane, washed with saturated potassium carbonate, dried over anhydrous sodium sulfate, concentrated. The residue was purified with flash column chromatography on silica gel using ethyl acetate and 0-10% methanol/ethyl acetate to afford product as solid (0.8916 g, yield: 86%). NMR (500 MHz, Chloroform-i/) delta 5.168 (br, 2H), 4.550 (d, J = 12.5 Hz, 2H), 2.859-2.800 (m, 2H), 2.432 (d, – J= 13.2 Hz, 1 H), 2.406 (d, J= 10.5 Hz, 1H), 1.094 (d, J = 6.5 Hz, 6H). LC-MS: 243.0 (MH+/z).

21655-48-1, As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics