Heterocyclic Building Blocks-piperazine

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,694499-26-8

To a solution of 3-ethynyl-4-methylbenzoic acid (500 mg, 3.12 mmol, 1.05 eq) in DCM, HATU (1.42 g, 3.74 mmol, 1.2 eq) and DIPEA (806 mg, 6.24 mmol, 2.0 eq) was added. The mixture was stirred at room temperature for 30 min or so. Then to the solution 3-trifluoromethyl-4-[(4-methylpiperazin-1-yl) methyl]aniline (812 mg, 2.97 mmol, 1.0 eq) was added and the temperature was raised to 45 C. The reaction is completed after 20 h and the solvent was evaporated to dryness under reduced pressure to afford the residue extracted twice with DCM and saturated sodium bicarbonate aqueous solution. The DCM layer was evaporated to dryness to afford yellow oil which was purified by column chromatogram to give intermediate 74 as a yellowish brown solid (807 mg, 65.4% yield). 1H NMR (400 MHz, CDCl3) delta 8.33 (s, 1H), 7.91 (s, 1H), 7.86 (d, J=13.7 Hz, 2H), 7.73 (t, J=7.1 Hz, 2H), 7.28 (s, 1H), 3.60 (s, 2H), 3.32 (s, 1H), 2.48 (br.s, 11H), 2.30 (s, 3H). MS m/z (ESI): 416.3 [M+H].

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Si Chuan University; Yang, Shengyong; Wei, Yuquan; (168 pag.)US2017/305920; (2017); A1;,
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630125-91-6,630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-Bromophenoxyacetic acid (1.20 g, 4.66 mmol) in anhydrous dichioromethane (10 mL) was added oxalyl chloride (0.59 g, 4.66 mmol)followed by a few drops of N,N-dimethylformamide at 0 C. After stirring at room temperature for one hour, a solution of 4-[(4-ethylpiperazin-1-yl)methyl]-3- (trifluoromethyl)aniline (2.50 g, 8.69 mmol) and triethylamine (2.63 g, 26.0 mmol) in anhydrous dichloromethane (10 mL) was added dropwise at 0 C and warmed to room temperature. After 16 h, the reaction mixture was partitioned between water (200 mL)and dichloromethane (100 mL). The aqueous layer was further extracted with dichloromethane (100 mL). The combined organic extracts were washed with brine (400 mL), dried (Na2SO4), the solvent evaporated and the residue purified by flash chromatography (Redisep silica gel, 97:3 CH2C12/MeOH) to afford 2-(4-bromophenoxy)- N- {4-[(4-ethylpiperazin- 1 -yl)methyl] -3 -(trifluoromethyl)phenyl } -acetamide (2.60 g). 1HNMR (400 MHz, DMSO-d6): 10.37 (s, 1H), 8.06 (s, 1H), 7.85-7.83 (dd, J= 8.4, 1.7Hz, 1H), 7.69-7.66 (a, J 8.5 Hz, 1H), 7.49-7.47 (d, J 9.2 Hz, 2H), 6.99-6.97 (d, J8.8 Hz, 2H), 5.75.(s, 2H), 4.72 (s, 2H), 3.53 (s, 2H), 2.37-2.27 (m, 1OH), 0.99-0.95 (t, J= 7.2 Hz, 3H); ESI MS, m/z 499 [M-H].

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference：
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH (A*STAR); CHERIAN, Joseph; DURAISWAMY, Athisayamani Jeyaraj; NACRO, Kassoum; WO2014/88519; (2014); A1;,
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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.,13754-38-6

Manufacturing Example 10 1-(4-benzoylpiperazine-1-yl)propan-2-one 0.10 g (0.53 mmol) 1-benzoylpiperazine and potassium carbonate 0.22 g (1.58 mmol, 3.0 eq.) were added to 5 ml acetonitrile and 0.05 g (0.53 mmol, 1.0 eq.) chloroacetone was added dropwise slowly at room temperature. After mixing for one hour, 5 ml purified water was added, and the reaction mixture was extracted with 10 ml ethylacetate three times. After collecting organic layer, drying with anhydrous magnesium sulfate, and concentrating with decompression, residues obtained were purified with silicagel chromatography (mobile phase: dichloromethane/methnol=10:1) and 0.11 g (83%) target compound as yellow serup were yielded. 1H NMR (400 MHz, CDCl3) 2.18 (3H, s), 2.41-2.69 (4H, m), 3.27 (2H, s), 3.42-3.54 (2H, m), 3.81-3.93 (2H, m), 7.40-7.46 (5H, m)

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference：
Patent; YANG JI CHEMICAL CO., LTD.; US2012/190689; (2012); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

General procedure: In a schlenk-type flask, a mixture of Pd2(dba)3 (0.023 g, 0.025mmol) and XantPhos (0.015 g, 0.025 mmol) in dry dioxane wasstirred at room temperature for 5 min. Then, NHR (2 mmol) andCs2CO3 (0.24 g, 0.75 mmol) were added and stirred for another 5min at ambient temperature. Afterwards, E-6 (F-4) (0.5 mmol)was added, and the flask was evacuated and backfilled with nitrogenfor three times. The reaction mixture was stirred at 100 C for9 h and followed by TLC until completion. After cooling, the solventwas removed under reduced pressure. The residue was purified byflash column chromatography with ethyl acetate/petroleum etherto afford compounds E-a?E-k (F-a?F-j). White solid, yield 31percent, mp: 144?146 C; 1H NMR (400 MHz,CDCl3) d: 7.51 (d, J = 1.6 Hz, 4H, PhH), 7.33 (d, J = 16 Hz, 1H, CH),7.20 (s, 2H, PhH), 6.96 (s, 1H, NH), 5.83 (d, J = 16.6 Hz, 1H, CH),5.62 (s, 1H, pyridine-H), 5.35 (s, 1H, pyridine-H), 3.34 (s, 2H,CH2), 2.80 (s, 4H, CH2), 2.68 (s, 2H, CH2), 2.45 (s, 3H, CH3), 2.14(s, 6H, CH3), 1.89 (s, 2H, CH2), 1.25 (s, 2H, CH2); 13C NMR (100MHz, CDCl3) d: 152.7, 149.8, 133.2, 132.3, 128.2, 117.9, 96.0,86.2, 51.7, 44.9, 16.3; ESI?MS: 508.2 [M+H+]. C30H33N7O (507.27)., 934-98-5

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

Reference：
Article; Lu, Xueyi; Yang, Jiapei; Kang, Dongwei; Gao, Ping; Daelemans, Dirk; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong; Bioorganic and Medicinal Chemistry; vol. 26; 8; (2018); p. 2051 – 2060;,
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883554-88-9, 4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The white solid from step A in ethanol (50 mL) was cooled to 0 C., and a pre-mixed solution of NaOCl (10-13% active chlorine, 43.4 mL) and 15% NaOH (78.0 mL) was added dropwise via an addition funnel. The ice bath was removed and the resulting mixture was stirred at room temperature for 1 h. 1N HCl was added to the resulting mixture until the pH of the solution was about pH 1, and the resulting mixture was stirred at room temperature for an additional 15 min. The pH of the solution was made basic with saturated aqueous potassium carbonate, and the resulting solution concentrated in vacuo to half the volume, then extracted three times with EtOAc, the combined organics were dried with Na2SO4, and concentrated in vacuo to yield the title compound, which was used in the next step without further purification. MS 202 (M+1)+, 883554-88-9

883554-88-9 4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester 17750351, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MACIELAG, Mark J.; Tennakoon, Manomi; US2009/275594; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55112-42-0,4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride,as a common compound, the synthetic route is as follows.

4-Methyl-l-piperazinecarbonyl chloride hydrochloride (19.9 mg, 0.1 mmol) was added to a solution of 4 (20 mg, 0.05 mmol) and anhydrous pyridine (25 muml, 0.3 mmol) in 3% allyl alcohol in dry methylene chloride (4 ml) and the mixture was stirred for 16 h. Purification of the crude product on silica gel yielded 5 (23.6 mg, 91%). ?NMR DMSO-d6) 8 12.03 (s, 1H), 8.41 (s, 1H), 8.21 (s, 1H), 8.01 (d, 1H, J=8.4 Hz), 7.88 (d, 1H, J=8.4 Hz), 7.82 (dd, 1H, J=8.4 Hz), 7.58 (t, 1H, J=8.1 Hz), 7.51 (d, 1H, J=8.4 Hz), 7.46 (t, 1H, J=7.6 Hz), 7.37 (s, 1H), 4.86 (t, 1H, J=10.8 Hz), 4.57 (dd, 1H, J=10.8 Hz), 4.38 (m, 1H), 4.06 (dd, 1H, J=10.8 Hz), 3.86 (dd, 1H, J=11 Hz), 3.41 (br, 4H), 3.29 (br, 4H), 2.82 (s, 3H), 2.57 (s, 3H). Synthesis of Compound (7). A solution of 5 (13 mg, 24 umol) and linker 6 (16.9 mg, 31 umol) in 5% acetic acid in dry methylene chloride (1 ml) was stirred for 30 min at 25 C. The solvent was completely removed in vacuo and purified by HPLC (SymmetryPrep C18, 7mum, 19 x 150 mm column) to give 7 (18.5 mg, 81%). MS: calcd for C48H57ClN8O11 (M+H) m/z 958.38, found 958.10., 55112-42-0

The synthetic route of 55112-42-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MEDAREX, INC.; WO2005/112919; (2005); A2;,
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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 56 4-(4-tert-Butoxycarbonylpiperazin-1-yl)benzaldehyde 4-(oxazol-5-yl)phenylhydrazone 4-(4-tert-Butoxycarbonylpiperazin-1-yl)benzaldehyde (363 mg) was added to an ethanol solution (10 ml) of 4-(oxazol-5-yl)phenylhydrazine (200 mg), followed by heating overnight under reflux. Dichloromethane was added to the residue obtained by evaporating the solvent, and the thus precipitated solid was collected by filtration, washed with diethyl ether and then dried to obtain the title compound (427 mg) as a yellow solid. 1H-NMR (400 MHz, CDCl3) delta: 1.49 (9H, s), 3.21 (4H, bs), 3.58 (4H, bs), 6.91 (2H, d, J=8.8 Hz), 7.13 (2H, d, J=8.8 Hz), 7.26 (1H, s), 7.55 (2H, d, J=8.8 Hz), 7.57 (2H, d, J=8.8 Hz), 7.62 (1H, s), 7.66 (1H, s), 7.85 (1H, s). ESI-MS m/z: 448 (M+H)+.

197638-83-8, As the paragraph descriping shows that 197638-83-8 is playing an increasingly important role.

Reference：
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1612204; (2006); 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.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

74879-18-8, In a sealed tube, 7-fluoro-2-(2-methylimidazo[l,2-b]pyridazin-6-yl)-4H-pyrido[l,2- a]pyrimidin-4-one (Intermediate 1; 50 mg, 0.169 mmol), and (S)-2-methylpiperazine (68 mg, 0.677 mmol, 4.0 eq.) were stirred in DMSO (2 mL) at 110C overnight. The solvent was removed under high vacuum. The residue was taken up in CH2CI2and washed with an aqueous saturated solution of NaHC03. The organic layer was separated and dried over Na2S04and concentrated in vacuo. The crude was purified by column chromatography (S1O2,CH2Cl2/MeOH=95/5 to 90/10) to afford the title product (40 mg, 63%) as a light yellow solid. MS m/z 376.2 [M+H+].

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; MCCARTHY, Kathleen Dorothy; METZGER, Friedrich; RATNI, Hasane; (76 pag.)WO2017/81111; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-methyl-5-oxiran-2-yl-2-benzofuran-1(3H)-one (3.00 g, 15.8 mmol) and (S)-4-N-BOC-2-hy-droxymethylpiperazine (5.12 g. 23.7 mmol) were suspended in ethanol (10 mL) in a 20 mL microwave tube. Thereaction mixture was degassed and heated in a microwave apparatus for 30 min at 150C. The reaction mixturewas evaporated to dryness, then chromatographed through a 330g Redi-sep column and eluted with a solventsystem of 1:1 EtOAc/ hexane to 100% EtOAc to yield the title compound. LC-MS : M+1= 407.

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; 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;,
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Piperazines – an overview | ScienceDirect Topics

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

Example 1; Preparation of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid; Racemic ulifloxacin (105 g) was dissolved in DMSO (1500 mL). D-tartrate (27 g) solution in DMSO (405 mL) was added to the racemic ulifoxacin solution with agitation. Cloudiness and precipitation appeared. After 20 hours of agitation at an ambient temperature, the mixture was filtered. The solid was dried under vacuum to yield 86 g of solid. The solid was recrystallized in DMSO to yield 37 g of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid-D-tartrate salt; elemental analysis indicated: C 49.08%, H 5.06%, N 9.50%, and S 7.44% (corresponding to: C16H16FN3O3S.1/2C4H6O6.H2O, calculated value: C 48.86%, H 4.78, N 9.50%, and S 7.25%). The salt was dispersed in water and the dispersion was neutralized with 2% NaOH aqueous solution to a pH value of 7 to 8. The precipitate was filtered and dried to yield 24.5 g of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. It had a rotation [alpha]D20=-143.4 (c=0.15, 0.1 mol/L NaOH), 1H-NMR (DMSO-d6) delta2.11 (3H, d, j=6.2 Hz), 2.85-3.20 (8H, m), 6.40 (1H, q, j=6.2 Hz), 6.89 (1H, d, j=7.4 Hz), 7.79 (1H, d, j=13.9 Hz), optical purity e.e.>95%., 112984-60-8

As the paragraph descriping shows that 112984-60-8 is playing an increasingly important role.

Reference：
Patent; Chen, Mao; Zhu, Shaoxuan; Zheng, Lizhen; Liu, Xuebin; Wang, Yuping; Xu, Shuwen; US2011/28444; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics