Heterocyclic Building Blocks-piperazine

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, To a solution of (R)-methylpiperazine (400 mg) in dichloromethane (20 mL) at 0 0C was added di-tert-butyl dicarbonate (871 mg). The reaction was stirred at room temperature for 4 h and then quenched with water (20 mL) and extracted into dichloromethane (2 x 40 mL). The combined organics were washed with saturated aqueous brine solution (40 mL), dried (MgSO4) and concentrated to give (R)-3-methyl-piperazine-l- carboxylic acid tert-butyl ester as a white solid (669 mg, 84%).

As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference：
Patent; PIRAMED LIMITED; GENENTECH, INC.; BAYLISS, Tracy; CHUCKOWREE, Irina; FOLKES, Adrian; OXENFORD, Sally; WAN, Nan, Chi; CASTANEDO, Georgette; GOLDSMITH, Richard; GUNZNER, Janet; HEFFRON, Tim; MATHIEU, Simon; OLIVERO, Alan; STABEN, Steven; SUTHERLIN, Daniel, P.; ZHU, Bing-Yan; WO2008/70740; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-12-2, tert-Butyl 4-(2-bromoacetyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of Example 53, N-[(2R)-i-amino-3-(4-cyanophenyl)propan-2-yl]- 2-chloro-5-[5 -( { [(1 R)- 1 -(4-methylphenyl)ethyl] amino }methyl)-2-furyl]benzamide, 125 mg (0.237 mmol) in acetonitrile (5.0 mL) was added triethylamine, 50 iL (0.356 mmol,1.5 eq) and tert-butyl 4-(bromoacetyl)piperazine-1-carboxylate, 95 mg (0.31 mmol, 1.3 eq.). The mixture was stirred at r.t, for 24 h, The mixture was diluted with ethyl acetate (20 mL) and the organic layer was washed successively with aq. sat, sodium hydrogen carbonate, water, brine, dried over sodium sulfate and concentrated. The residue was purified by preparative TLC (eluent: dichloromethane/ ammonia 7N in methanol, 97/3)to give an impure fraction that was purified by preparative TLC (eluent:dichloromethane/ ammonia 7N in methanol, 97.5/2.5) to give the pure product, 52 mg(29%) as an off-white solid.LC-MS (Method 1): R = 2,50 mm; MS (ES+): mlz = 753/755 (M+H), 535/537 (M+H21 8) ?H-NMR (500 MHz, DMSO-d6) d [ppm] = 1.25 (d, 3H), 1.40 (s, 9H), 2.27 (s, 3H), 2.65-2.72 (m, 2H), 2.80 (dd, 1H), 3.05 (dd, 1H), 3.24-3.35 (m, 5H), 3.35-3,48 (m, 5H),3.50 & 3.58 (2 d, AB, 2H), 3.70 (m, 1H), 4.27 (m, 1H), 6.32 (d, 1H), 6.92 (d, 1H), 7.12 (d, 2H), 7.24 (d, 2H), 7.44-7.51 (m, 4H), 7.66 (dd, 1H), 7.76 (d, 2H), 8.40 (d, 1H)., 112257-12-2

The synthetic route of 112257-12-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; BERGER, Markus; HUeBNER, Jan; TER LAAK, Antonius; GORJANNACZ, Matyas; FERNANDEZ-MONTALVAN, Amaury Ernesto; RODESCHINI, Vincent; ROCHE, Didier; (248 pag.)WO2017/93272; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-60-6, (R)-1-Boc-Piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Trimethylsilyl diazomethane (2M in hexane, 14 ml) was added dropwise to a solution of (2R)-L-(TERT-BUTOXYVARBONYL) piperazine-2-carboxylic acid (5 g) in methanol (100 ml) and DCM (115 ml), and the solution stirred at room temperature for 16 hours. The solvent was concentrated in vacuo and the residue purified by chromatography, eluting with ethyl acetate then 5% methanol / 7N ammonia in ethyl acetate, to give 1-tert-butyl 2-methyl (2R)- PIPERAZINE-1, 2-dicarboxylate as an oil (2.55 g, 48%); NMR spectrum (DMSO-d6) 1.40 (s, 9H), 2.10 (bs, 1H), 2.52 (m, 1H), 2.72 (dd, 1H), 2.82 (d, 1H), 2.97 (m, 1H), 3.29 (d, 1H), 3.61 (d, 1H), 3.67 (s, 3H), 4.43 (m, 1H) ; Mass spectrum MH+ 245.

278788-60-6, As the paragraph descriping shows that 278788-60-6 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/26152; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,2, 2-Trifluoroethyl trifluoromethanesulphonate (8.2 g) was added to a stirred mixture of 1-tert-butoxycarbonylpiperazine (6 g), potassium carbonate (5.77 g) and acetonitrile (30 ml) and the resultant mixture was stirred at ambient temperature for 16 hours. The mixture was filtered and the filtrate was evaporated. The residue was purified by column chromatography on silica using increasingly polar mixtures of petroleum ether (b. p 40-60C) and ethyl acetate as eluent. There was thus obtained tert-butyl 4- (2, 2, 2-trifluoroethylpiperazine-1-carboxylate as a solid (8.1 g); NMR Spectrum: (CDC13) 1.45 (s, 9H), 2.6 (m, 4H), 2.95 (q, 2H), 3.4 (m, 4H), 57260-71-6

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/41829; (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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.,485841-52-9

75 mg (0.16 mmol) of 3-[(chloroacetyl)amino]-N-[6-(2-fluorophenyl)pyridin-3-yl]-4- (trifluoromethoxy)benzamide (intermediate 14) were dissolved in 0.69 mL of anh DMF. 4.1 mg (0.025 mmol) of potassium iodide, 0.042 mL (0.24 mmol) of N-ethyl-N-isopropylpropan-2-amine and 27.5 mg (0.24 mmol) of (2S)-l,2-dimethylpiperazine were added. It was stirred at rt overnight. The reaction mixture was concentrated to dryness under vacuum. The residue was purified by HPLC (method 2) yielding 34.5 mg (39%) of the title compound. XH-NMR (400 MHz, DMSO-d6): delta [ppm]= 1.01 – 1.12 (m, 3H), 2.09 – 2.45 (m, 5H, partly overlapping with the DMSO signal), 2.77 – 3.02 (m, 3H), 3.25 (br. s, 2H), 7.30 – 7.39 (m, 2H), 7.44 – 7.52 (m, 1H), 7.64 – 7.70 (m, 1H), 7.82 – 7.91 (m, 2H), 7.94 – 8.00 (m, 1H), 8.31 (dd, 1H), 8.75 – 8.81 (m, 1H), 9.07 (d, 1H), 9.91 (s, 1H), 10.75 (s, 1H). LC-MS (method 4): Rt = 0.99 min; MS (ESIpos): m/z = 546 [M+H]+.

As the paragraph descriping shows that 485841-52-9 is playing an increasingly important role.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; THEDE, Kai; BENDER, Eckhard; SCOTT, William J.; RICHTER, Anja; ZORN, Ludwig; LIU, Ningshu; MOeNNING, Ursula; SIEGEL, Franziska; GOLZ, Stefan; HAeGEBARTH, Andrea; LIENAU, Philip; PUEHLER, Florian; BASTING, Daniel; SCHNEIDER, Dirk; MOeWES, Manfred; WO2014/147021; (2014); A2;,
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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.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

630125-91-6, Example 69 Preparation of ethyl6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate To a stirred solution of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzeneamine (30.6 mg) in 1,4-dioxane (1 Ml), was added 4-nitrophenylchloroformate (21.6 mg) at room temperature. After 60 C. at 1 h, them mixture was cooled to rt and ethyl 6-(3-aminophenyl)-1H-indazole-3-carboxylate (30 mg) was added. The mixture was stirred at 90 C. for 12 h. Ethyl acetate and water were added and the aqueous layer was extracted with ethyl acetate three times. The combined organic layer was dried over magnesium sulfate and concentrated under reduced pressure. The residue was triturated in ethyl acetate/hexane to give 6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate (16.2 mg). 1H NMR (400 MHz, DMSO-d6) delta13.98 (s, 1H), 9.09 (s, 1H), 8.93 (s, 1H), 8.15 (8.4 Hz, 1H), 7.99 (s, 1H), 7.93 (s, 1H), 7.81 (s, 1H), 7.62 (m, 3H), 7.43 (br d, J=4.4 Hz, 2H), 7.28 (m, 1H), 4.41 (q, J=7.2 Hz, 2H), 3.54 (s, 2H), 2.49 (m, 10H), 1.39 (t, J=7.2 Hz, 3H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Sim, Tae Bo; Son, Jung Beom; Kim, Hwan; Park, Dong Sik; Choi, Hwan Geun; Ham, Young Jin; Hah, Jung Mi; Yoo, Kyung Ho; Oh, Chang Hyun; Lee, So Ha; Ha, Jae Du; Cho, Sung Yun; Kwon, Byoung Mog; Han, Dong Cho; US2012/130069; (2012); A1;,
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Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 511A 3-(4-cyclopentyl-1-piperazinyl)-1-propanamine A mixture of N-(3-bromopropyl)phthalimide (0.8 g, 3.0 mmol), 1-cyclopentylpiperazine (0.46 g, 3.0 mmol), and K2CO3 (1.66 g, 12.0 mmol) in CH3CN (30 mL) was heated to reflux for 3 hours, cooled to room temperature, and filtered through diatomaceous earth (Celite). The filtrate was concentrated, treated with 6N HCl (9.0 mL) and acetic acid (18.0 mL), heated to reflux overnight, and concentrated. The residue was treated with potassium carbonate (1.66 g) in CH3CN (30 mL) for 1 hour. After filtration of the solid, the solvent was evaporated to provide the desired product. MS (DCI/NH3) m/e 212 (M+H)+; 1H NMR (300 MHz, DMSO-d6) delta 8.04 (br s, 2H), 3.68 (m, 4H), 3.41 (m, 4H), 3.21 (m, 2H), 2.91 (m, 2H), 2.0 (m, 4H), 1.84-1.73 (m, 4H), 1.55 (m, 2H).

21043-40-3, The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Comess, Kenneth M.; Erickson, Scott A.; Henkin, Jack; Kalvin, Douglas M.; Kawai, Megumi; Kim, Ki H.; BaMaung, Nwe Y.; Park, Chang Hoon; Sheppard, George S.; Vasudevan, Anil; Wang, Jieyi; Barnes, David M.; Fidanze, Steve D.; Kolaczkowski, Lawrence; Mantei, Robert A.; Park, David C.; Sanders, William J.; Tedrow, Jason S.; Wang, Gary T.; US2004/157836; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4-(3 -hydroxypropyl)piperazine- 1 -carboxylate (1.52 g, 6.2 mmol), Ph3P (2.46 g, 9.4 mmol), 12 (2.40 g, 9.4 mmol) and imidazole (1.28 g, 18.6 mmol) in DCM (100mL) was stirred at room temperature for 5 h and then diluted with DCM (200 mL). The organic layer was washed with brine, dried over anhydrous sodium sulfate, filtered and evaporated. The residue was purified by chromatography (PE : EtOAc = 5 : 1) to provide tert-butyl 4-(3- iodopropyl)piperazine- 1 -carboxylate (1 .10 g, 50%) as a colorless oil.

132710-90-8, As the paragraph descriping shows that 132710-90-8 is playing an increasingly important role.

Reference：
Patent; PRINCIPIA BIOPHARMA, INC.; VERNER, Erik; BRAMELD, Kenneth Albert; WO2015/120049; (2015); A1;,
Piperazine – Wikipedia
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

39539-66-7, EXAMPLE 1 4-(5-Chloropyridin-2-yl)-3-methyl-5-[(4-methylpiperazin-1-yl)carbonyl]oxy-1,2,4-triazole 50 g (0.24 mol) of 4-(5-chloropyridin-2-yl)-5-hydroxy-3-methyl-1,2,4-triazole are dissolved or suspended in 1 litre of absolute tetrahydrofuran. The sodium hydride, degreased with toluene, is added thereto from 10.8 g of a 55% sodium hydride dispersion and the mixture is stirred for 1 hour at ambient temperature. Then 39 g (0.24 mol) of freshly distilled 1-chlorocarbonyl-4-methyl-piperazine (Bp17: 120-124 C.) are added dropwise thereto and the mixture is stirred for a further 5 hours whilst moisture is excluded. The resulting suspension is concentrated by evaporation in vacuo and the residue is carefully mixed with water and neutralised. The solution containing the carbamate is extracted several times with methylene chloride and the organic phase is washed with water, dried and concentrated. The residue is triturated with ether and 55 g (68% of theory) of the title compound are obtained in the form of crystals, m.p. 121-122 C. 12.5 g of this base are dissolved in 100 ml of methanol and 4.3 g of fumaric acid are added hot. On cooling, the hemifumarate crystallises out, m.p. 173-175 C. (yield: 17 g). The compound is highly water-soluble; pH of the solution 3.5. The starting compound, 4-(5-chloropyridin-2-yl)-5-hydroxy-3-methyl-1,2,4-triazole, is obtained as follows:

39539-66-7 4-Methylpiperazine-1-carbonyl chloride 3016935, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Boehringer Ingelheim KG; US4732900; (1988); 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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

Stage 3: methyl 4-[2-[4-(4-methylpiperazin-1-yl)benzyl]amino-4-oxoquinazolin-3(4H)-yl]butanoateTriethylamine (0.4 mL) and [4-(4-methylpiperazin-1-yl)benzyl]amine (300 mg) are successively added to a solution of methyl 4-(2-chloro-4-oxoquinazolin-3(4H)-yl)butanoate (140 mg) in tetrahydrofuran (3 mL). The mixture is stirred at ambient temperature for 24 hours then water and ethyl acetate are added. After decantation and extractions, the combined organic phases are washed with salt water, dried over Na2SO4 then concentrated under reduced pressure at 40 C. Purification by flash chromatography on silica gel (eluent: dichloromethane/methanol 95:5) produces the expected compound in the form of beige crystals (131 mg, 58% yield from Stage 1).MS/LC: calculated MM=449.2; m/z=450.2 (MH+)NMR (1H, 400 MHz, DMSO-d6): delta 1.85 (t, 2H), 2.21 (s, 3H), 2.40 (m, 6H), 3.08 (m, 4H), 3.54 (s, 3H), 4.05 (t, 2H), 4.54 (d, 2H), 6.86 (AB, 2H), 7.08 (t, 2H), 7.18 (AB, 1H), 7.25 (AB, 2H), 7.48 (t, 1H), 7.52 (t, 1H), 7.89 (AB, 1H).

216144-45-5, The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SOCIETE DE CONSEILS DE RECHERCHES ET D’APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.); US2010/144714; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics