Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, EXAMPLE 2 4-Amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline N-(Cyclopropylcarbonyl)piperazine (3.08 g., 0.02 mole) and 2-chloro-4-amino-6,7-dimethoxyquinazoline (4.74 g., 0.02 mole) are reacted according to the procedure of Example 1(a). The crude product crystallized from ethanol affords analytically pure 4-amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline, m.p. 283.5-285.5 C. (corr.). Analysis. Calcd. for C18 H23 N5 O3 (percent): C, 60.49; H, 6.49; N, 19.59. Found (percent): C, 60.56; H, 6.46; N, 19.41.

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

Reference：
Patent; Mead Johnson & Company; US4060615; (1977); A;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7365-45-9,2-(4-(2-Hydroxyethyl)piperazin-1-yl)ethanesulfonic acid,as a common compound, the synthetic route is as follows.

7365-45-9, General procedure: Larger Scale Production of Nucleotide Analogs. (0230) The process described for small-scale batches is scalable to larger batches by using proportionate amounts of compounds. As an alternate to the small-scale batches described above, larger scale batches were prepared. Here, reaction mixtures having a total volume of 0.25 ml (>10× the volume of the small-scale batch) and containing 40 mM of a reagent from Table 1, 10 mM magnesium acetate, 80 muM dATP, 50 mug/ml BSA, and 5.84 muM p41 subunit (containing 0.64 M glycerol following dilution in the glycerol diluent described above) were incubated for 30 min at 70 C. Incubation with the p41 subunit and TLC analysis on PEI plates showed greater than 60% conversion of starting material (i.e., the reagent and dNTP) into nucleotide analog products (dNMP derivatives). Experiments were also performed using heavy isotopes incorporated in dNTP, but the presence of a heavy isotope did not alter the utilization of dNTP in the reaction. (0231) Samples from reaction mixtures were analyzed using a capillary reverse phase liquid chromatography system coupled to an Orbitrap Discovery mass spectrometer in negative mode. Negative mode nanospray mode was set to -1.5 kV, and chromatographic flow rate was <20 nl/min. Fragmentation was achieved using high collision dissociation at 45% energy. Isotope-labeled samples were run both individually and combined. By analyzing the mass difference between heavy and light fragmentation pattern, the identity of each fragmentation peak was established. As the paragraph descriping shows that 7365-45-9 is playing an increasingly important role. Reference：
Patent; THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY OF COMMERCE; MEMORIAL SLOAN KETTERING CANCER CENTER; UNIVERSITY OF MARYLAND; Marino, John P.; Kelman, Zvi; Hurwitz, Jerard; Giulian, Gary G.; (45 pag.)US9534243; (2017); B2;,
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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 9: 2,2-Dimethyl-piperazine-l-carboxylic acid benzyl ester trifluoro acetate 9.1 : 2,2-Dimethyl-piperazine- 1 ,4-dicarboxylic acid 1 -benzyl ester 4-tert-butyl ester To a solution of 18.5 g (82.0 mmol) 3,3-dimethyl-piperazine-l-carboxylic acid tert-butyl ester in 150 mL DCM at RT was added 30.0 mL (174 mmol) DIPEA. The mixture was cooled with ice and a solution of 14.0 mL (93.2 mmol) benzyl chloroformate in 60 mL DCM was added drop wise. The reaction mixture was stirred at RT over night and quenched with saturated aqueous sodium bicarbonate solution. The product was extracted with DCM. The organic layers were combined, dried over sodium sulfate and concentrated in vacuo. Yield: 23.0 g (81%) ESI-MS: m/z = 249 (M-BOC+H)+ Rt(HPLC): 1.60 min (method 1)

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of ferf-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (S)-4-N-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford ferf-butyl (S)-3-(((ferf-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NMR (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, 1H), 3.41 (dd, 1H), 3.52 (s, 1H), 3.85 (s, 2H)., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (2019); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (500 mg, 2.50 mmol) , propionic acid (0.22 mL, 3.00 mmol) , EDCI (718 mg, 3.74 mmol) and HOAT (850 mg, 6.24 mmol) in DCM (15 mL) was stirred at 0 , and DIPEA (1.7 mL, 9.99 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 16 h and washed with water (10 mL × 2) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 3-methyl-4-propionylpiperazine-1-carboxylate as colorless oil (630 mg, 95) .1H NMR (400 MHz, CDCl3) : delta ppm 4.76, 4.36 (m, m, 0.5H, 0.5H) , 4.00-3.94 (m, 1H) , 3.85-3.76 (m, 1H) , 3.53, 3.29 (m, m, 0.5H, 0.5H) , 2.98-2.96 (m, 1H) , 2.83-2.74 (m, 2H) , 2.34-2.26 (m, 2H) , 1.45 (s, 9H) , 1.13 (t, J 7.0 Hz, 6H) .

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference：
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;,
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.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 24 te/t-Butyl 4-(4-(6-bromo-7-(4-(4-chlorobenzyl)piperazin-1-yl)-3H-imidazo[4,5- C6H4CI), 7.41 (m, 4H, C6H4CI), 7.07 (d, J = 8.9 Hz1 2H) and 8.04 (d, J = 8.9 Hz, 2H)(2,6-C6H4 and 3,5-C6H4), 8.17 (s, 1H, imidazo[4,5-/b]pyridine 5-H), 13.23 (br s, 1H, imidazo[4,5-b]pyridine N-H);LC (Method B) – MS (ESI, m/z): Rt = 4.55 min – 666, 668, 670 [(M+H)+, BrCI isotopic pattern]., 197638-83-8

The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHROMA THERAPEUTICS LTD.; WO2009/1021; (2008); A1;,
Piperazine – Wikipedia
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

To asolution of 3-(chloroacetyl)-2-methylbenzonitrile (1.7 g, 8.8 mmol) in THF (17.6 mL) was added (R)-4-N-boc-2-hydroxymethyl-piperazine (2.279 g, 10.54 mmol) and DIPEA (3.07 mL, 17.56 mmol) at rt. The reaction mixture wasstirred at rt over the weekend. After concentration, the residue was partitioned between EtOAc and aqueous NaHCO3(saturated). The aqueous layer was extracted with EtOAc (2x). The combined organic phase was washed with brine,dried over anhydrous MgSO4, and filtered. Concentration was followed by purification by prep TLC (silica gel; 10%MeOH/DCM) to give the title compound: LC/MS (M+1)+ = 374.14

278788-66-2, The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
Piperazine – Wikipedia
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

Preparation of Lambda^2-benzyl-6-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(lH)-yl)-Lambda^-(2- (4-methylpiperazin-l-yl)ethyl)-l,3,5-triazine-2,4-diamineTo the above reaction solution of N-benzyl-4-chloro-6-(6,7-dimethoxy-3,4- dihydroisoquinolin-2(lH)-yl)-l,3,5-triazin-2-amine (0.126 mmol, 1 equivalent) in CEta3CNu/Eta2O (1/1, 2 ml) was added 2-(4-methyl-piperazin-l-yl)-ethylamine (36 mg, 0.252 mmol, 2 equivalents), followed by adding IN NaOH (126 mul, 0.126 mmol, 1 equivalent). The reaction mixture was heated at 8O0C overnight. The solvent was evaporated and the residue was acidified and purified with RP-HPLC (Luna, 5mu C8(2), 100x21mm, 10-60percent CH3CN/H2O, 0.1percent TFA, 17 min) to give the desired product. MS: cacld for C28H38N8O2+H+ 519.32, found 519.4., 934-98-5

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference：
Patent; PRAECIS PHARMACEUTICALS INC; DING, Yun; WO2010/85246; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of starting material (27 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-1-yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in t-BuOH (1.5 mL) was heated at 100 C. in a seal tube for 4 h. The reaction was then filtered through celite, eluted with dichloromethane, and concentrated in vacuo. The residue was then purified by reverse-phase prep-HPLC to afford the title compound as the TFA salt (21.5 mg, 47%).

122833-04-9, 122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (2016); 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.21091-98-5,(4-Methylpiperazin-1-yl)(4-nitrophenyl)methanone,as a common compound, the synthetic route is as follows.

(4-Methyl-piperazin- l-yl)-(4-nitro-phenyl)-methanone (2.12 g, 8.51 mmol) was dissolved in Methanol (35 mL, 860 mmol) and the solution was carefull added to a Parr vessel containing 10% Palladium on Carbon (0.650 g, 48.7 mmol) under nitrogen. The mixture was then placed on a Parr hydrogenation apparatus and was allowed to shake at 55 psi until uptake of hydrogen ceased. The catalyst was then filtered to afford 1.86 g of (4-Amino-phenyl)-(4-methyl-piperazin-l-yl)-methanone without further purification. (M+H) = 220.6. 1H NMR (400 MHz, DMSO, d6) delta 7.09 (d, 2H, J = 8.41 Hz), 6.53 (d, 2H J = 8.41 Hz), 5.48 (s, 2H), 3.46 (m, 4H), 2.28 (m, 4H), 2.17 (s, 3H).

21091-98-5, As the paragraph descriping shows that 21091-98-5 is playing an increasingly important role.

Reference：
Patent; CEPHALON, INC.; BRESLIN, Henry J.; CHATTERJEE, Sankar; DIEBOLD, James L.; DORSEY, Bruce D.; DUNN, Derek; GINGRICH, Diane E.; HOSTETLER, Greg A.; HUDKINS, Robert L.; HUNTER, Rachael; JOSEF, Kurt; LISKO, Joseph; MESAROS, Eugen F.; MILKIEWICZ, Karen L.; OTT, Gregory R.; SUNDAR, Babu G.; THEROFF, Jay P.; THIEU, Tho; TRIPATHY, Rabindranath; UNDERINER, Theodore L.; WEINBERG, Linda; WELLS, Gregory J.; ZIFICSAK, Craig A.; WO2010/71885; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics