Month: August 2021

548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Half of the solid from the previous step was treated with N,N-diisopropylethylamine (0.5 mL, 3 mmol), DMSO (0.5 mL, 7 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (273 mg, 1.27 mmol) and the reaction mixture was heated at 120 C overnight, concentrated by rotary evaporation, dissolved in a small amount of DCM and purified by silica gel chromatography (0-50% ethyl acetate:hexanes) to produce the title intermediate (288 mg, 29 % yield) as a yellow solid. (m/z): [M+H]+ calcd for C24H27F4N4O4 591.09, 593.09 found 593.2.

548762-66-9, As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

Reference：
Patent; Theravance Biopharma R&D IP, LLC; MCKINNELL, Robert Murray; LONG, Daniel D.; VAN ORDEN, Lori Jean; JIANG, Lan; LOO, Mandy; SAITO, Daisuke Roland; ZIPFEL, Sheila; STANGELAND, Eric L.; LEPACK, Kassandra; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; EP2635571; (2015); B1;,
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

Weighing 2-methoxy-4 – (4-methyl piperazin-1-yl) aniline (12C) (2.21g, 10mmol), the 100 ml round-bottom flask. N sequentially adding to the reaction bottle, N-dimethylformamide (20 ml), 2, 4, 5-trichloro-pyrimidine (1.83g, 10mmol) and potassium carbonate (1.79g, 13mmol). The reaction temperature is increased to 80 C stirring 4 hours. After cooling to room temperature to be reacted, the reaction solution is poured into ice water (50 ml), the residue is extracted with methylene chloride (100 ml × 2), the combined organic phase with saturated salt water (50 ml × 2), dried anhydrous sodium sulfate, after concentrating under reduced pressure, the residue is separated by silica gel column chromatography (dichloromethane/methanol (v/v) =15:1) to obtain the title of yellow solid product 2,5-dichloro-N-(2-methoxy-4 – (4-methyl piperazin-1-yl) phenyl) pyrimidin-4-amine (12D) (3.4g, yield: 92.5%), 122833-04-9

As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Patent; Four Chuanhaisike Pharmaceutical Co., Ltd.; Li, Yao; Weiy, Onggang; Zang, Guobiao; Li, Guanpeng; Hu, Shihong; (73 pag.)CN105384694; (2016); A;,
Piperazine – Wikipedia
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

Synthesis of 6-(4-cyclopentylpiperazin-l-yl)-9H-purin-2-amine (28): Compound 1 (0.5 g, 2.95 mmol) was dissolved in acetonitrile (8 mL) and potassium carbonate (1.63 g, 11.8 mmol) and 1 – cyclopentylpiperazine (0.91 g, 5.9 mmol) were added. The reaction was stirred under the N2 atmospheric condition at 100C for 12 hours. Organic layer was extracted with CHCI3 system and column chromatography was done by using CH3OH and CHCI3 system to give compound 28 (yield 60%) as a off-white solid. 1H NMR (300MHz, DMSO-d6) delta ppm 7.66 (s, 1H), 5.72 (s, -NH2), 4.09 (m, 4H), 2.46 (t, J = 4.2 Hz, 4H), 2.42-2.39 (m, 1H), 1.61 -1.50 (m, 4H), 1.43-1.29 (m, 4H). ESI-MS m/z 288.14 (M+H).

21043-40-3, 21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH; TALUKDAR, Arindam; GANGULY, Dipyaman; MUKHERJEE, Ayan; PAUL, Barnali; RAHAMAN, Oindrila; KUNDU, Biswajit; ROY, Swarnali; DEBLINA, Raychaudhuri; (60 pag.)WO2019/92739; (2019); A1;,
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Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,115761-79-0

To a solution of l-(2,4-difluorophenyl)piperazine [C.A.S. 115761-79-0] (0.088 g, 0.446 mmol) in DCE (2.14 ml) stirred at r.t. was added D88 (0.1 g, 0.371 mmol) and the resulting mixture was stirred at r.t. overnight. Then, acetic acid (0.037 ml) was added and stirred at r.t. for 4 h more. Then, sodium triacetoxy-borohydride (0.87 g, 0.409 mmol) was added and stirred at r.t. overnight. The reaction mixture was neutralized with Na2CO3 (aqueous sat. solution) and extracted with DCM. The organic layer was dried (Na2SO4) and concentrated in vacuo. The crude product thus obtained was purified by column chromatography (silica gel; DCM/EtOAc from 100/0 to 50/50 as eluent). The desired fractions were collected and concentrated in vacuo. The residue obtained was triturated with DIPE to yield final compound E224 (0.107 g, 64%).

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; ADDEX PHARMA S.A.; CID-NUNEZ, Jose, Maria; OEHLRlCH, Daniel; TRABANCO-SUAREZ, Andres, Avelino; TRESADERN, Gary, John; VEGA RAMIRO, Juan, Antonio; MACDONALD, Gregor, James; WO2010/130424; (2010); 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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

(iii) 3-((4-((4-(3-(5-(tert-Butyl)-2-methoxy-3-(methylsulfinyl)phenyl)ureido)naphthalen-1- yl)oxy)pyridin-2-yl)amino)-5-methoxy-N-(2-(4-methylpiperazin-1-yl)ethyl)benzamideHATU (150 mg, 0.394 mmol) was added to a solution of the product from step (ii) above (200 mg, 0.284 mmol), 2-(4-methylpiperazin-1-yl)ethanamine (60 mg, 0.419 mmol) and diisopropylethylamine (150 L, 0.859 mmol) in DMF (2 mL). The reaction mixture was stirred at rt for 72h. Water (10 mL) added and the resulting solid filtered off, washed with water (2 mL) and dried to afford the title compound (0.19 g). 1H NMR (400 MHz, DMSO-ds) delta 9.41 (s, 1 H), 9.07 (s, 1 H), 8.96 (s, 1 H), 8.51 (d, 1 H), 8.28 (d, 1 H), 8.21 (t, 1 H), 8.12 (d, 1 H), 8.10 (d, 1 H), 7.88 (d, 1 H), 7.77-7.67 (m, 1 H), 7.66-7.58 (m, 1 H), 7.56 (t, 1 H), 7.50 (t, 1 H), 7.40 (d, 1 H), 7.36 (d, 1 H), 6.86 (dd, 1 H), 6.58 (dd, 1 H), 6.14 (d, 1 H), 3.87 (s, 3H), 3.74 (s, 3H), 2.79 (s, 3H), 2.43 (t, 2H), 2.32 (s, br, 10H), 2.15 (s, 3H), 1.32 (s, 9H). LCMS m/z 794 (M+H)+(ES+)

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

Reference：
Patent; RESPIVERT LIMITED; TOPIVERT PHARMA LIMITED; FYFE, Matthew Colin Thor; THOM, Stephen Malcolm; BAKER, Thomas Matthew; HARBOTTLE, Gareth William; HASIMBEGOVIC, Vedran; RIGBY, Aaron; WO2015/92423; (2015); 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

To n-butanol (2 mL) was added compound 4A-3 (30 mg, 0.135 mmol) and compound 5A-1 (47 mg, 0.135 mmol), and then p-toluenesulfonic acid (23.3 mg, 0.135mmol) was added under stirring. The mixture was heated to 100C and stirred for 5 hours. After TLC indicated the reaction was completed, the reaction mixture was concentrated under reduced pressure to give a crude product, which was further purified and isolated by column chromatography to obtain an off-white solid product, compound I-13 (56 mg, yield 77.8%). 1H NMR (400 MHz, cd3od) delta 8.49 (d, J=8.4 Hz, 1H), 8.07 (s, 1H), 7.86 (dd, J=8.0, 1.3 Hz, 1H), 7.67 (d, J=8.7 Hz, 1H), 7.60 (dd, J=11.5, 4.3 Hz, 1H), 7.30 (t, J=7.6 Hz, 1H), 6.67 (s, 1H), 6.49 (dd, J=8.7, 2.1 Hz, 1H), 3.84 (s, 3H), 3.29-3.20 (m, 4H), 2.97-

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; Humanwell Healthcare (Group) Co., Ltd.; WANG, Xuehai; XU, Yong; SHENG, Xijun; ZHANG, Xiaolin; XIA, Hangui; YANG, Zhongwen; YUE, Yang; HUANG, Lu; XIAO, Qiang; (80 pag.)EP3372594; (2018); 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.128102-16-9,(R)-4-Benzyl 1-Boc-2-methylpiperazine-4-carboxylate,as a common compound, the synthetic route is as follows.

A solution of 4-benzyl 1-tert-butyl 2-methylpiperazine-1,4-dicarboxylate (4.8 g, 14.4 mmol) in methanol (25 mL) was added 480 mg of 10% Pd/C and stirred at room temperature under hydrogen overnight. Filtered and concentrated to give the title product (2.8 g, yield 97%) as colorless oil. 1H-NMR (400 MHz, CDCl3) delta (ppm): 1.21 (d, J=6.8 Hz, 3H), 1.46 (s, 9H), 2.64-2.70 (m, 1H), 2.74-2.78 (m, 1H), 2.88-3.01 (m, 3H), 3.78 (d, J=12.4 Hz, 1H), 4.16 (m, 1H); LC-MS (ESI) m/z: 201 (M+1)+, 128102-16-9

The synthetic route of 128102-16-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); 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

To a stirred solution of tert-butyl 4-(3-hydroxypropyl)piperazine-l-carboxylate (7.0 g, 28.64 mmol) in THF (50 mL), was added triethylamine (8 mL, 57.29 mmol) at room temeperature. After 5 min, benzoyl chloride (3.66 mL, 31.51 mmol) was added dropwise at 0 C under inert atmoshphere. After addition, the resultant reaction mixture was stirred at room temperature for 1 h. After completion of reaction (monitored by TLC), the reaction was quenched with water (100 mL) and extracted with ethyl acetate (3 X 250 mL). The combined organic layer was dried over anhydrous sodium sulphate and concentrated – – under reduced pressure to afford 43 (7.8 g) as a off-white solid. *H NMR (400 MHz, CDC13): delta 8.06 – 8.00 (m, 2H), 7.59 – 7.52 (m, 1H), 7.48 – 7.40 (m, 2H), 4.38 (tj = 6.6 Hz, 2H), 3.50 – 3.39 (m, 4H), 2.53 (t, / = 7.3 Hz, 2H), 2.43 (br t, / = 4.9 Hz, 4H), 1.98 (quin, / = 6.8 Hz, 2H), 1.46 (s, 9H); LCMS (M+H) = m/z 349.7 [M+H+]; purity~83%., 132710-90-8

132710-90-8 1-Boc-4-(3-hydroxypropyl)piperazine 16217800, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; TOPADUR PHARMA AG; NAEF, Reto; TENOR, Hermann; (135 pag.)WO2017/85056; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

50606-32-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

8.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl esterTo a solution of intermediate 8.2 (7.37 g) in CH2Cl2 (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDCI-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with CH2Cl2, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with CH2Cl2. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1 :0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00.

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

Reference：
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; LEHMANN, David; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/122504; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

502649-29-8, 1-Boc-3-Benzylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

502649-29-8, A solution of l-benzyl-2-methyl-lH-pyrrole-3-carboxylic acid (150 mg) , tert-butyl 3-benzylpiperazine-l-carboxylate(193 mg) , WSC-HCl (174 mg) , HOBt (139 mg) and DMF (10 ml) was stirred at room temperature for 12 hr. Then, the mixture was poured into a saturated aqueous sodium bicarbonate solution and extracted with ethyl acetate. The extract was washed successively with water and brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated in vacuo. The residue was subjected to silica gel column chromatography, and the fraction eluted with ethyl acetate-hexane (1:9 to 1:3) was concentrated in vacuo to give an amorphous solid (140 mg) . 110 mg of the resulting amorphous was dissolved in dichloromethane (2 ml), and TFA (2 ml) was added thereto. After stirring at room temperature for 2 hr,. the mixture was poured into a saturated aqueous sodium bicarbonate solution (50 ml) and extracted with ethyl acetate. The extract was washed with brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated in vacuo. The residue was subjected to silica gel column chromatography, and eluted with ethyl acetate-methanol (1:1). The target fraction was concentrated, and then the residue was dissolved in ethyl acetate. The mixture was acidified with a 4 N hydrogen chloride-ethyl acetate solution, and then concentrated in vacuo to give the desired product (45 mg) as an amorphous solid. MS (ESI+, m/e) 374 (M+l)

The synthetic route of 502649-29-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2007/94513; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics