Heterocyclic Building Blocks-piperazine

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4,6-dimethyl-2-(o-tolyl)pyrimidine-5-carboxylic acid (26) (40 mg, 0.17 mmol), tert-butyl 2-methylpiperazine-1-carboxylate45 (50 mg, 0.25 mmol), HOBt(25 mg, 0.18 mmol), EDCI (28 mg, 0.18 mmol) and DIPEA (0.06 mL,0.33 mmol) in DCM (10 mL) was stirred at room temperature for18 h. The solution was then concentrated in vacuo before the residue was purified via silica gel chromatography (1:1 ethyl acetate/hexane) to afford compound 28, a clear oil (45 mg, 65%), as a mixture of conformers. Rf 0.44 (1:1 ethyl acetate/hexane). 1H NMR(CDCl3) d: 7.77e7.74 (m, 1H), 7.34e7.25 (m, 3H), 4.65 (m, 0.5H), 4.51 (m, 0.5H), 4.47 (m, 0.5H), 4.27 (m, 0.5H), 4.02 (m, 0.5H), 3.90 (m,0.5H), 3.40e3.32 (m, 1H), 3.21e2.95 (m, 3H), 2.59 (s, 1.5H), 2.57 (s,1.5H), 2.52 (s, 3H), 2.45 (s, 1.5H), 2.43 (s, 1.5H), 1.46 (s, 9H), 1.27 (d,J6.8 Hz, 1.5H), 1.12 (d, J6.8 Hz, 1.5H). 13C NMR (CDCl3) d: 168.1,167.8, 166.8, 166.8, 163.4, 162.8, 162.4, 154.41, 154.37, 137.9, 137.8,137.4, 137.3, 131.4, 131.43, 131.41, 130.38, 130.36, 129.64, 129.60,126.0, 125.8, 125.4, 80.6, 50.3, 46.9, 46.3, 46.2, 45.5, 41.5, 38.8, 38.0,28.5, 22.55, 22.50, 22.20, 22.15, 21.10, 21.08, 15.6, 15.5. To a solution of tert-butyl 4-(4,6-dimethyl-2-(o-tolyl)pyrimidine-5-carbonyl)-2-methylpiperazine-1-carboxylate (28) (45 mg,0.11 mmol) in DCM (3 mL) was added 10 drops of TFA and allowed to stir at room temperature for 18 h. The volatiles were evaporated to afford the product, a colourless oil (35 mg, quant.) as a mixture of conformers., 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Lim, Zelong; Duggan, Peter J.; Wan, Soo San; Lessene, Guillaume; Meyer, Adam G.; Tuck, Kellie L.; Tetrahedron; vol. 72; 9; (2016); p. 1151 – 1160;,
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259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

80.1: 4-(6-Methoxy-pyridine-2-carbonyl)-3,3-dimethyl-piperazine-1-carboxylic acid tert-butyl ester A mixture of 410 mg (2.28 mmol) 6-methoxy-2-pyridinecarboxylic acid and 400 muL (3.02 mmol) 1-chloro-N,N,2-trimethylpropenylamine in 10 mL THF was stirred at RT. After 1.5 h, 600 mg (2.66 mmol) 3,3-dimethyl-piperazine-1-carboxylic acid tert-butyl ester and 1.00 mL (5.81 mmol) DIPEA was added and the reaction mixture was stirred at RT for 30 min The reaction mixture was diluted with saturated NaHCO3 solution and extracted with EtOAc. The combined organic phases were dried over sodium sulfate, filtered and concentrated in vacuo. The crude material was purified by flash chromatography (PE/EtOAc=1/1).Yield: 780 mg (84%)ESI-MS: m/z=350 (M+H)+ Rt(HPLC): 1.23 min (method 3), 259808-67-8

259808-67-8 1-Boc-3,3-Dimethylpiperazine 22710387, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; US2013/158042; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

4-Nitropyrazole (2.81 g, 13.88 mmol) and 1-hydroxyethyl-4-methylpiperazine (1.0 g, 6.94 mmol) were dissolved in anhydrous tetrahydrofuran (50 mL), and a solution of triphenylphosphine (3.64 g, 13.88 mmol) and diisopropyl azodicarboxylate (2.81 g, 13.88 mmol) in anhydrous tetrahydrofuran (6 mL) was added dropwise under nitrogen gas atmosphere. The reaction solution was stirred at room temperature for 1 hour, and then 1N hydrochloric acid (30 mL) and water (50 mL) was added. The aqueous phase was extracted with ethyl acetate (50 mL*2). The combined organic phase was dried over anhydrous sodium sulfate, filtered and the filtrate was concentrated. The residue was purified by silica gel column chromatography (dichloromethane: methanol=10:1) to give compound 22-c (1.0 g, yield 60.2percent). LC-MS (ESI): m/z=240.2[M+H]+., 5464-12-0

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.; XU, Zusheng; ZHANG, Nong; WANG, Tinghan; SUN, Qingrui; WANG, Yuguang; (90 pag.)US2018/208604; (2018); A1;,
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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

A solution of 740 mg (2.71 mMol) of 4- (4-METHYL-PIPERAZIN-1-YLMETHYL)-3- trifluoromethyl] benzenamine in 12.5 ml CH2CI2 and 2.5 ML pyridine is cooled in an ice-bath under N2-atmosphere. Then a solution of 375 PL (2.85 MMOL) of 2-nitrobenzoyl chloride (Fluka, Buchs, Switzerland) in 12.5 ml CH2CI2 is added dropwise. After 30 min, the resulting mixture is diluted with EtOAc and 0.5 N HCI, the aqueous layer separated off and extracted with EtOAc. The organic phases are washed 3 times with 0.5 N HCI and then discarded. The combined aqueous phases are turned basic by the addition of saturated NA2CO3 solution and extracted with 3 portions of EtOAc. The organic phases are washed with brine, dried (NA2SO4) and CONCENTRATED IN VACUUO. COLUMN chromatography (SiO2 ; ETOAC X EtOAc/EtOH (+ 1 % ET3N) 97: 3) gives the title compound ; MS: [M+1] + = 423.

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/52884; (2004); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

173 2-flH-Ihdazol-4-yl)-4-morpholin-4-yl-6-((2S.6R)-2A6-trimethyl-piperazin-l- ylmethylVthieno[3 ,2-dlpyrimidineTo (66) (1.5g) in ethanol (3OmL) was added sodium borohydride (Ig). After 4 h the reaction mixture was quenched with brine and the resulting solid was collected by filtration, and air dried to furnish 168 (2-chloro-4-morpholin-4-yl- thieno[3,2-d]pyrimidin-6-yl)-rnethanol (1.42g).To a solution of 168 (1.42g) in toluene (14ml), warmed to 400C, was added phosphorous tribromide (0.16ml). The resulting mixture was then heated to 1000C for 6 h, was cooled, diluted with chloroform, washed with brine, and dried (MgSO4). The solvent was removed in vacuo to yield 6-bromomethyl-2-chloro-4-morpholin-4- yl-thieno[3,2-d]pyrimidine, 169 (1.4Og). EPO A mixture of (3R,5S)-3,5-dimethyl-piperazine-l-carboxylic acid tert-buty ester (0.92g), 6-bromomethyl-2-chloro-4-mophiholin-4-yl-thieno[3,2-d]pyrimidine (Ig) and potassium carbonate (1.59g) in MeCN (10ml) was heated to reflux for 5 days. The reaction mixture was subsequently cooled, diluted with chloroform, washed with brine and dried (MgSO4), and the solvent was removed in vacuo. The residue was purified by flash column chromatography to yield (3S,5R)-4-(2-chloro- 4-mophiholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl)-3,5-dimethyl-piperazine-l- carboxylic acid tert-butyl ester, 170 (1.2g). Treatment of this compound with HCl in DCM/MeOH produced 2-chloro-6-(2S,6R)-2,6-dimethyl-piperazin- 1 -ylmethyl)-4- mophiholin-4-yl-thieno[3,2-d]pyrimidine, 171, which was then methylated using 37% formaldehyde solution and sodium borohydride in MeOH, furnishing 172. 1H NMR (400MHz, CDCl3) 1.17 (6H, d), 1.92 (2H, t), 2.3 (3H, s), 2.73 (2H, d), 2.83 (2H, m), 3.95 (4H, m), 4.03 (4H, m), 4.18 (2H, s), 7.36 (IH, s), 7.48 (IH, t), 7.56 (IH, d), 8.26 (IH, d), 9.00 (IH, s), 10.40 (IH, br m); MS (ESI+) 478 (MH+).

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PIRAMED LIMITED; WO2006/46031; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirring solution of tert-butyl 3,3-dimethylpiperazine-1-carboxylate (300 mg, 1.4 mmol) in DCM (3 mL) was added MsCl (321 mg, 2.8 mmol) and K2CO3(425 mg, 4.2 mmol). After being stirred at 20 C for 4 hrs, the resulting mixture was diluted with DCM (80 mL), then washed with water (30 mL) and brine (30 mL), dried over anhydrous Na2S04and concentrated in vacuo. The residue was purified by column chromatography (eluting with PE/EA=5/1, v:v) to give tert-butyl 3,3-dimethyl-4-methylsulfonyl-piperazine-l-carboxylate (270 mg) as a colorless oil.

259808-67-8, The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; HAN, Xingchun; JIANG, Min; WANG, Jianhua; WANG, Yongguang; YANG, Song; (211 pag.)WO2018/1952; (2018); A1;,
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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 a solution of Intermediate 4 (4.63 mmol) and (i?)-3-(hydroxymethyl)- piperazine- l-carboxylic acid tert-butyl ester (1 g, 4.62 mmol) in DMF (20 mL) was added DIPEA (6.94 mmol). The reaction mixture was heated at 100C for 7 h, then cooled and stirred at room temperature for 2 days. The reaction mixture was concentrated in vacuo and partitioned between EtOAc and water. The organic layers were dried over sodium sulfate and concentrated again. The resulting orange oil was purified by column chromatography on silica gel, with a gradient of 1% increasing to 20% MeOH in DCM, to yield the title compound (0.42 g, 24.8%) as a yellow gummy solid. LCMS (ES+) 367.8 (M+H)+, RT 0.8 minutes (method 3).

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

Reference£º
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; BROOKINGS, Daniel Christopher; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; KULISA, Claire Louise; NEUSS, Judi Charlotte; REUBERSON, James Thomas; WO2013/68458; (2013); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: These amines were required for the syntheses of 4 and 20 respectively. To a solution of 4-nitrobenzylchloride (1 mmol) in anhydrous THF (3 mL) was added 1-methylpiperazine or piperidine (1 mmol) and triethylamine (1.5 mmol, 0.21 mL). The solution was heated at 70 C overnight. The reaction mixture was then extracted with dichloromethane and water. The organic fractions were combined, dried over anhydrous Na2SO4, and concentrated under reduced pressure. The residue was purified by column chromatography (hexane/EA 1:4) and characterized by 1H NMR (Supplementary Information). It was dissolved in 10 mL ethanol, PtO2 (0.01 g) was added under nitrogen. Hydrogenation was carried out on a Parr hydrogenator at 50 psi for 16 h. The catalyst was then removed by filtration and the filtrate was concentrated in vacuo to give the amine in quantitative yield., 70261-81-3

70261-81-3 1-Methyl-4-(4-nitrobenzyl)piperazine 677795, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Nguyen, Thuy; Sakasegawa, Yuji; Doh-Ura, Katsumi; Go, Mei-Lin; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 2917 – 2929;,
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.169448-87-7,(R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Lithium aluminium hydride (1M in THF, 17.6 ml) was added to a solution OF TERT- butyl (2R)-2-(HYDROXYMETHYL) PIPERAZINE-1-CARBOXYLATE (1.27 g) in THF (40 ml) at 0C, then the reaction was warmed to room temperature. The solution was stirred for 3 hours, then heated at reflux for 1 hour, cooled to 0C and quenched by sequential addition of water (0.2 ml), sodium hydroxide (2N, 0.2 ml) and then water (0.4 ml). The resulting slurry was filtered and concentrated in vacuo to give [(2R)-1-methylpiperazin-2-yl]methanol (0.44 g) ; Mass spectrum MH+ 131., 169448-87-7

169448-87-7 (R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate 24820219, apiperazines compound, is more and more widely used in various fields.

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

848482-93-9, (S)-4-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred mixture of (5)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (1.0 g, 4.34 mmol) and a2C03 (0.90 g, 10.80 mmol) in water (10 mL) was added solution of FMOC-C1 (1.23 g, 4.77 mmol) in 1,4-dioxane (10 mL) dropwise at 0 C. The reaction mixture was stirred at room temperature for 16 h then diluted with water (50 mL) and washed with MTBE (25 mL). The aqueous layer was acidified with IN aqueous HQ (10 mL) to pH 2 and extracted with EtOAc (3 x 50 mL). The combined organic extracts were washed with brine solution (50 mL), dried over anhydrous a2S04, filtered and concentrated to afford the title compound (0.87 g) as an off- white solid. The crude product was used in the next step without purification., 848482-93-9

The synthetic route of 848482-93-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; BLIZZARD, Timothy Allen; BIFTU, Tesfaye; WO2013/148478; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics