Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,655225-01-7

Example 7Q ethyl (7R,20S)-16-{2-[4-(tert-butoxycarbonyl)piperazin-1-yl]ethyl}-18-chloro-1-(4-fluorophenyl)-19-methyl-15-oxo-10-{[2-(3,3,3-trifluoropropoxy)pyrimidin-4-yl]methoxy}-7,8,15,16-tetrahydro-14H-17,20-etheno-13,9-(metheno)-6-oxa-2-thia-3,5,16-triazacyclooctadeca[1,2,3-cd]indene-7-carboxylate A 4 mL vial equipped with stir bar and septum was charged with Example 7P (9.5 mg), tert-butyl 4-(2-bromomethyl)piperazine-1-carboxylate (6.8 mg) and cesium carbonate (11.3 mg). N,N-dimethylformamide (116 muL) was added, and the mixture was stirred at ambient temperature. After completion of the reaction as indicated by LC/MS (?30 minutes), the mixture was poured into water and extracted with three portions of ethyl acetate. The combined organic layers were washed with brine, dried over anhydrous magnesium sulfate, filtered and concentrated. Purification by preparative thin-layer chromatography (0.5 mm thick, 20*20 cm, eluting with 100percent ethyl acetate) provided the title compound. LC/MS (APCI) m/z 1034.4 (M+H)+.

As the paragraph descriping shows that 655225-01-7 is playing an increasingly important role.

Reference：
Patent; AbbVie Inc.; AbbVie Deutschland GmbH & Co. KG; Brady, Patrick B.; Braje, Wilfried; Dai, Yujia; Doherty, George A.; Gong, Jane; Jantos, Katja; Ji, Cheng; Judd, Andrew S.; Kunzer, Aaron R.; Lai, Chunqiu; Mastracchio, Anthony; Risi, Roberto M.; Song, Xiaohong; Souers, Andrew J.; Sullivan, Gerard M.; Tao, Zhi-Fu; Teske, Jesse A.; Wang, Xilu; Wendt, Michael D.; Yu, Yiyun; Zhu, Guidong; Penning, Thomas D.; (218 pag.)US2019/55264; (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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

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

Reference：
Article; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
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Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of 2-chloro-N-(3-chlorobenzyl)-6-(3,5-dimethylisoxazol-4-yl)quinazolin-4-amine (Example 1, 39.9 mg, 0.1 mmol) and 2-(4-methylpiperazin-1-yl)ethanamine (143 mg, 1.0mmol) was added EtOH (1 ml). The tube was sealed and heated at 90 00 for 16 h. After cooling to rt, the mixture was filtered through a filter, and submitted for purification to give N4-(3- chlorobenzyl)-6-(3,5-dimethylisoxazol-4-yl)-N2-(2-(4-methylpiperazin- 1 -yl)ethyl)quinazoline-2,4- diamine, 2TFA (28.6 mg, 0.039 mmol, 39.0 percent yield). 1H NMR (400 MHz, DMSO-d6) O 12.81 (5,1H), 10.07 (5, 1H), 9.62 (d, J= 141.1 Hz, 1H), 8.23 (d, J= 1.8 Hz, 1H), 7.82 (dd, J= 8.4, 1.7 Hz,1 H), 7.52 (d, J = 8.5 Hz, 1 H), 7.46 (t, J = 1.9 Hz, 1 H), 7.42 ? 7.27 (m, 3H), 4.83 (d, J = 5.7 Hz,2H), 4.43?2.67 (m, 15H), 2.42 (5, 3H), 2.25 (d, J= 1.4 Hz, 3H). (including 1 salt NH); MS(M+H)= 506., 934-98-5

The synthetic route of 934-98-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; STROVEL, Jeffrey William; YOSHIOKA, Makoto; MALONEY, David J.; YANG, Shyh Ming; JADHAV, Ajit; URBAN, Daniel Jason; (334 pag.)WO2017/91661; (2017); A1;,
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Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

R)-l-Boc-3-(Hydroxymethyl)piperazine (10 g, 46.2 mmol) was dissolved in a mixture of DCM (180 ml) and sat. NaHC03 (180 ml). CBZ-C1 (6.60 ml, 46.2 mmol) was dissolved in DCM (15 ml) and added dropwise with vigorous stirring. The mixture was stirred for 2.5 hours. The layers were separated and the aqueous phase was extracted with DCM. The combined organic phases were washed with brine, dried over Na2S04 and the solvent was removed in vacuo to give an oil which was used in the next step without purification.

278788-66-2, As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; MSD R&D (CHINA) CO. LTD.; WILLIAMS, Peter, D.; MCCAULEY, John, A.; BENNETT, David, J.; BUNGARD, Christopher, J.; CHANG, Lehua; CHU, Xin-Jie; DWYER, Michael, P.; HOLLOWAY, M. Katherine; KEERTIKAR, Kartik, M.; LOUGHRAN, H. Marie; MANIKOWSKI, Jesse, J.; MORRIELLO, Gregori, J.; SHEN, Dong-Ming; SHERER, Edward, C.; SCHULZ, Jurgen; WADDELL, Sherman Tim; WISCOUNT, Catherine, M.; ZORN, Nicolas; SATYANARAYANA, Tummanapalli; VIJAYASARADHI, Sivalenka; HU, Bin; JI, Tao; ZHONG, Bin; WO2015/17393; (2015); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture of 13a (151 mg, 0.423 mmol) and 4 N HCl in 1,4-dioxane solution (1.38 ml) was stirred at room temperature overnight. After concentration, the residue was crystalized with etherto afford the white precipitation. The resulting solid was collected by filtration to afford 14a (121 mg, 98.0%) as the white solid. MSESI (m/z) = 257 [M+H]+. To a solution of 4a (116 mg, 0.35 mmol)in DMF (2.3 ml) was added 14a (120 mg, 0.42 mmol), COMU (225 mg, 0.525 mmol) and Et3N (177 mg, 1.75 mmol) at room temperature.The reaction mixture was stirred at same temperature for 1.5 h. The reaction mixture was diluted with sat. NaHCO3 solution to afford the pale yellow precipitation. The resulting solid was collected by filtration to 16a, 169447-70-5

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

Reference：
Article; Tsuno, Naoki; Yukimasa, Akira; Yoshida, Osamu; Suzuki, Shinji; Nakai, Hiromi; Ogawa, Tomoyuki; Fujiu, Motohiro; Takaya, Kenji; Nozu, Azusa; Yamaguchi, Hiroki; Matsuda, Hidetoshi; Funaki, Satoko; Yamanada, Natsue; Tanimura, Miki; Nagamatsu, Daiki; Asaki, Toshiyuki; Horita, Narumi; Yamamoto, Miyuki; Hinata, Mikie; Soga, Masahiko; Imai, Masayuki; Morioka, Yasuhide; Kanemasa, Toshiyuki; Sakaguchi, Gaku; Iso, Yasuyoshi; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2177 – 2190;,
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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A solution of 2-chloroalkyl/aryl substitutedwith or without N-substitution as well as with or without 5 and/or 6-substituted benzimidazole derivative (1.75g,0.01051mol) and 1-[(4-phenyl)carbonyl]piperazine (3g,0.0105mol) in N, N dimethylformamide was taken in a RBF.K2CO3(2gm,) was added to the reaction mixture. The reaction mixture was stirred for 8h at 80C on a magnetic stirrer (heat + stirring). The progress of the reaction was monitored by thin layer chromatography (TLC).Upon completion of the reaction, water was added to the reaction mixture and the product extracted by shaking the reaction mixture with dichloromethane in a separating funnel.The dichloromethane layer was washed successively with water and brine, dried over anhydrous sodium sulfate. Evaporation of the solvent gave theproduct. 11a-l Recrystallized with various solvent like chloroform, ethanol, methanol.

13754-38-6, The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Kankate, Rani S.; Gide, Parag S.; Belsare, Deepak P.; Oriental Journal of Chemistry; vol. 30; 4; (2014); p. 1855 – 1863;,
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Piperazines – an overview | ScienceDirect Topics

39539-66-7, 4-Methylpiperazine-1-carbonyl chloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 4′-OH was protected using methyl pipirazine carbonyl chloride (11 mg, 0.054 mMoles) in 2mL DCM, 200 muL Allyl alcohol and pyridine (21 muL) for 2 hours. The product was purified by silica gel column chromatography and Identified by Mass Spec, MS+1 = 654, 39539-66-7

As the paragraph descriping shows that 39539-66-7 is playing an increasingly important role.

Reference：
Patent; MEDAREX, INC.; WO2005/112919; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The mixture of Pd2(dba)3 (377 mg, 0.410 mmol), piperidine (500 mg, 5.87 mmol), t-BuOK (851 mg, 7.58 mmol), X-Phos (418 mg, 0.877 mmol) and intermediate M-2 (1000 mg, 3.35 mmol) in toluene (40 mL) was heated under a nitrogen atmosphere at 110 C until complete by TLC. Upon completion, the reaction solution was cooled to ambient temperature, concentrated under vacuum, and purified by flash chromatography (3:1 petroleum ether: ethyl acetate eluent) to yield N-(2,6-dimethyl-4-(piperidin-1-yl)phenyl)-3,3-dimethylbutanamide (293mg, 29% yield)., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Yang, Shaoning; Lu, Dingqiang; Ouyang, Pingkai; Bioorganic and Medicinal Chemistry Letters; vol. 28; 10; (2018); p. 1731 – 1735;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

To 188 (10 mg, 0.026 mmol) in DMF (800 mu) was added 1- methylpiperazin-2-one (14.8 mg, 0.130 mmol) and the reaction mixture was heated at 90 °C for 2 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH-NH3 (7 N), 20: 1 to afford 10 mg (83percent) of 189t. MS (m/z): [M+H]+ 462.1.

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

Reference：
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; CHIOSIS, Gabriela; KANG, Yanlong; PATEL, Hardik J.; PATEL, Maulik; OCHIANA, Stefan; RODINA, Anna; TALDONE, Tony; SHRESTHA, Liza; (288 pag.)WO2015/175707; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

170911-92-9, Step 3. 4-[4-(6-Bromo-imidazo[1,2-a]pyrazin-8-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester [0167] A mixture of 6, 8-dibromoimidazo [1, 2-a] pyrazine (12. 5 MMOL), 4- (4-AMINO- PHENYL)-PIPERAZINE-L-CARBOXYLIC acid tert-butyl ester (12) (13. 1 mmol), potassium carbonate (25 mmol), acetonitrile (50 ML) and N, N-DIMETHYLACETAMIDE (20 mL) is heated at 65 C for 16 hrs. The mixture is cooled to room temperature, treated water (100 mL), and extracted with ethyl acetate (3 x 80 mL). The extracts are washed with water (3 x 60 mL) and brine (1 x 60 mL), dried over magnesium sulfate, and concentrated in vacuo. The residue is’ chromatographed over silica gel, eluting with ethyl acetate, to give 4- [4- (6-bromo- imidazo [1, 2-a] pyrazin-8-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester (13) as a light brown foam.

As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference：
Patent; CELLULAR GENOMICS, INC.; WO2005/14599; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics