Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Reference Example 10 benzyl 3-methylpiperazine-1-carboxylate A 4 g portion of 2-methylpiperazine was dissolved in 40 ml of dichloromethane, and 1.71 g of benzyl chloroformate was added dropwise thereto at -78 C. After 1 hour of stirring, the mixture was washed by adding water and dried and then the solvent was evaporated to obtain 2.0 g of the title compound., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Yamanouchi Pharmaceutical Co. Ltd.; US6673799; (2004); B1;,
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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: In a 1 L round-bottom flask with a magnetic stir bar, compound 7 (46 g, 0.2014 mol, 1.0 eq.) was diluted in DIEA (41.64 mL, 0.2416 mol, 1.2 equivalents) and THF (700 mL). Solid N-Boc piperazine (39.38 g, 0.2114 mol, 1.05 eq.) was slowly added in portions. A mild exothermic reaction was observed. The reaction mixture was allowed to stir at room temperature for 2 hours then was quenched with saturated NaCl solution (100 mL), water (400 mL), and EtOAc (500 mL). The layers were separated and the aqueous layer was extracted with EtOAc (2 x 200 mL). The combined organic layers were dried (Na2SO4) and concentrated to give a gray solid. The crude solid was stirred in 2:1 TBME/hexanes (300/150 mL) overnight. The solids were filtered then washed with hexane (250 mL) to recover 52 g of impure product. The TBME/hexanes slurry was repeated to recover 46 g (59%) of compound 8. All remaining impure material was combined and purified via silica gel chromatography (4:1 hexane/EtOAc) to recover another 11.2 g (14%) of 8 for a total combined yield of 57.2 g (74%).

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

Reference£º
Patent; ARAXES PHARMA LLC; DENG, Xiaohu; LI, Liansheng; LONG, Yun Oliver; LIU, Yuan; REN, Pingda; MANI, Neelakandha S.; ALLISON, Brett D.; SALES, Zachary S.; LIANG, Jimmy T.; (71 pag.)WO2017/100546; (2017); 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.53788-49-1,tert-Butyl 4-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

53788-49-1, Indole-2-carboxylic acid (5.2 g) in THF (200 mL) was treated with [CARBONYIDIIMIDAZOLE] (4.8 g) and stirred at ambient temperature for 10 min whereupon [4-METHYL-PIPERAZINE-1-CARBOXYLIC] acid tert-butyl ester (5.0 g) was added. The mixture was stirred at ambient temperature for 72 h and the solvent removed under reduced pressure. The residue was dissolved in ethyl acetate and washed with saturated sodium bicarbonate solution. The organic portion was separated, dried over sodium sulfate and filtered, and solvent was evaporated to afford a solid. Recrystallization from hot ethanol afforded [4- (1 H-] lndole-2-carbonyl)-piperazine-1-carboxylic acid ter-butyl ester (4. 2 g).

As the paragraph descriping shows that 53788-49-1 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2004/22061; (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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

B) 4-(4-Iodo-benzyl)-3-oxo-piperazine-l-carboxylic acid tert-butyl ester: Sodium hydride (1.30 g, 33.5 mmol) was added to a slurry of 3-oxo-piperazine-l- carboxylic acid tert-butyl ester (6.70 g, 33.4 mmol) from step A in 25 mL dry N,N- dimethylformamide and 90 mL dry tetrahydrofuran under argon atmosphere and cooled to O0C. The mixture was stirred at room temperature until a solution was obtained after 30 minutes. 4-Iodobenzyl bromide (9.90 g, 33.4 mmol), dissolved in 20 mL tetrahydrofuran, was added dropwise. The reaction was stirred for 1 hour to give a white slurry. Ethyl acetate and water was added. The organic phase was washed three times with water, once with brine, dried (sodium sulfate) and evaporated. The crude was purified on a silica column using dichloromethane / methanol (97 : 3) as eluent to give 12.2 g of the sub-title product (yield 87 %). 1H NMR (400 MHz, chloroform-d as solvent and internal reference) delta(ppm) 1.46 (s, 9H), 3.24 (m, 2H), 3.58 (t, 2H, J= 5.2 Hz), 4.14 (s, 2H), 4.54 (s, 2H), 7.01 (d, 2H, J= 8.3 Hz), 7.66 (d, 2H, J= 8.4 Hz)., 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; WO2007/8144; (2007); 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.25057-77-6,1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of (S)-l, 2-dimethylpiperazine (45g, 190.6mmol, leq) in EtOH (450mL) was added TEA (106.9mL, 762.7mmol, 4eq) under argon for 20min., then followed by addition of l-bromo-2,4-difluoro-5-nitrobenzene (47.8g, 286.0mmol, 1.5eq) at RT under argon atm and heated to 85C for 16h. TLC analysis indicated formation of less polar spot, then the reaction mixture was cooled to RT and solvent was evaporated under reduced pressure to give crude product, which was purified by column chromatography (silica gel, 100-200 mesh) using 0-30% EtOAc in pet ether as an eluent to afford (S)-4-(4-bromo-5-fluoro-2-nitrophenyl)-l,2- dimethylpiperazine (42g, 92%) as a yellow solid. LCMS: [M+H]+ 332.0.

25057-77-6, As the paragraph descriping shows that 25057-77-6 is playing an increasingly important role.

Reference£º
Patent; ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR); AL-AWAR, Rima; ZEPEDA-VELAZQUEZ, Carlos Armando; PODA, Gennady; ISAAC, Methvin; UEHLING, David; WILSON, Brian; JOSEPH, Babu; LIU, Yong; SUBRAMANIAN, Pandiaraju; MAMAI, Ahmed; PRAKESCH, Michael; STILLE, Julia Kathleen; (1053 pag.)WO2017/147700; (2017); 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

N-(5-tert-Butylisoxazol-3-yl)-N- {3- [ (2-chloropyrimidin-5-yl) ethynyl] phenyl} urea (Intermediate 9) (0.22 g) and tert-butyl 4-(2-aminoethyl)-piperazine-1-carboxylate (0.38 g) were stirred in MeCN (10 mL) and hydrogen chloride (I. OM solution in ether) (0.11 mL) was added dropwise. The reaction mixture was stirred and heated at 70¡ãC for 4 hours. The solvent was evaporated and the residue was dissolved in DCM (20 mL) and TFA (10 mL). The reaction mixture was stirred at ambient temperature for 2 hours, the solvent was evaporated and the product was purified by flash chromatography on silica using 1-20percent (7N NH3 in MeOH) in DCM as eluent. The product was triturated with ether to give the title compound as an off-white solid (274 mg, 99percent); ‘H NMR (DMSO-d6) 1.29 (s, 9H), 2.45-2. 57 (m, 2H), 2.57-2. 65 (m, 4H), 3.03-3. 10 (m, 4H), 3.39-3. 49 (m, 2H), 6.49 (s, 1H), 7.10-7. 16 (m, 1H), 7.29-7. 35 (m, 2H), 7.51 (t, 1H), 7.75 (s, 1H), 8.40-8. 52 (m, 3H), 8.99 (s, 1H), 9.62 (s, 1H) ; MS m/e MH+ 489.

192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/60970; (2005); 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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Example 54 – Preparation of Intermediate 19 The synthesis of Intermediate 19 followed the procedure of General Procedure 15 following: Intermediate 18 Intermediate 19 To a cooled solution (0C) of 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (Intermediate 18, 3.5 g, 14.3 mmol) in dry dichloromethane (70 mL) was added triethylamine (TEA, 5 mL, 35.9 mmol) followed by morpholine-4-carbonyl chloride (3.35 mL, 28.7 mmol). The reaction mixture was stirred at room temperature for 3 hours. To the mixture was added ice-cold water (20 mL), then it was extracted into EtOAc (2 x 50 mL). The combined organic layers were dried over sodium sulfate, filtered and concentrated under reduced pressure. The crude residue was purified by flash chromatography using 30% EtOAc/n-hexane to afford 1-tert-butyl 2-methyl 4- (morpholine-4-carbonyl)piperazine-1,2-dicarboxylate (Intermediate 19, 3.6 g, yield: 72%) as an off white solid; TLC: 50% ethyl acetate in hexane. Rf-0.5.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; VERSEON CORPORATION; SHORT, Kevin Michael; ESTIARTE-MARTINEZ, Maria de los Angeles; KITA, David Ben; SHIAU, Timothy Philip; (340 pag.)WO2016/138532; (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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Step B 4-t-Butoxycarbonyl-2-ketopiperazine A mixture of 500 mg (5 mmol) of piperazinone, 1.2 g (5.5 mmol) of t-butyldicarbonate and 2 g of sodium chloride in 7.5 mL of water and 10 mL of chloroform was heated to reflux 4 hrs. The reaction mixture was cooled to room temperature and extracted with ethyl acetate. The combined ethyl acetate extracts were dried over anhydrous magnesium sulfate. Solvent removal gave a crude product which was purified on silica gel using 5% methanol in ethyl acetate as solvent to give 925 mg of the desired carbamate lactam as white solid. 1 H NMR (CDCl3): 1.46(s,9H); 3.37(m,2H); 3.62(m,2H); 4.08(s,2H), 5625-67-2

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Merck & Co., Inc.; US5629322; (1997); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 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

Add (3-((3-(pyridin-3-yl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-6-yl)thio)propanoic acid to a round bottom flask (50 mg) followed by N,N-dimethylformamide (5 ml), 4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (42 Mg), 2-(7-oxobenzotriazole)-N,N,N’,N’-tetramethylUrea hexafluorophosphate (74 mg) and triethylamine (0.05 ml). The reaction system was stirred at room temperature for 14 hours under argon atmosphere. anti-After completion, the solvent was evaporated to dryness under reduced pressure. Organic phase with water,After washing with saturated brine, it was dried over anhydrous sodium sulfate. The organic phase is filtered and evaporated to dryness under reduced pressure to give a crude material.Alkane (5 mL) was added in trifluoroacetic acid (1 mL). The reaction system was stirred at room temperature for 14 hours under argon atmosphere. After the reaction,The solvent was evaporated to dryness under reduced pressure and the mixture was diluted with water and then neutralized with saturated sodium hydrogen carbonate. Aqueous phase acetic acidThe organic layer was washed with water and saturated brine and dried over anhydrous sodium sulfate. The organic phase is filtered and steamed under reduced pressureAfter drying, get a rough product. The crude product was purified by purified silica gel column chromatography to afford purified compound 173.

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

Reference£º
Patent; Chinese Academy Of Sciences Hefei Matter Sciences Institute; Liu Jing; Liu Qingsong; Liu Xuesong; Wang Beilei; Jiang Zongru; Yu Kailin; Chen Cheng; Zou Fengming; Liu Qingwang; Liu Xiaochuan; Wang Wei; Wang Wenliang; Hu Chen; Wang Wenchao; Wang Junjie; Wang Li; (82 pag.)CN109942544; (2019); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

2.6 g of 3-oxetanone, 1.0 g of sodium cyanoborohydride and 0.16 ml of acetic acid are added to a solution of 2.0 g of benzyl piperazine-1-carboxylate in 20 ml of acetonitrile and then stirred for 16 hours at RT. The reaction mixture is diluted with water and filtered through a Chem Elut.(R). cartridge, eluting with DCM. The combined organic phases are dried over MgSO4 and the solvent is evaporated under vacuum. The residue is purified by preparative HPLC and 1.7 g of a white solid is obtained.

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SANOFI; US2012/277205; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics