Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: Methane sulfonyl chloride (58 muL, 0.7 mmol) and triethylamine (238 muL) was added to a solution of compound 2 (180 mg, 0.6 mmol) in dichloromethane (5 mL) and stirred at room temperature for 1 h. After completion of the reaction by TLC, ice water was added to quench the reaction. The mixture was extracted with dichloromethane (20 mL×3). The organic layer was washed with brine and dried over Na2SO4. The solid was filtered off, and the filtrate was concentrated under reduced pressure to give the methylsulfonylated product (210 mg, yield 93%). To a solution of the methylsulfonylated product (210mg, 0.6 mmol) in DMF (5 mL) was added K2CO3 (111 mg, 0.8 mmol), morpholine (93 muL, 1.0 mmol). The mixture was stirred at 90 C for 2 h. After completion of the reaction by TLC, The mixture was extracted with dichloromethane (20 mL×3). The organic layer was washed with brine and dried over Na2SO4. The solid was filtered off, and the filtrate was concentrated under reduced pressure. The residues were separated by silica gel column chromatography (V petroleum ether: V ethyl acetate = 8:1) to give CH-H-1 (108 mg, yield 53%). Under the same conditions, compounds CH-H-2 to CH-H-16 were obtained., 20327-23-5

The synthetic route of 20327-23-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Duan, Zhe; Liu, Jingqiu; Niu, Liping; Wang, Jun; Feng, Mingqian; Chen, Hua; Luo; Bioorganic and Medicinal Chemistry; vol. 27; 15; (2019); p. 3229 – 3236;,
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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

Alternative preparation of 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate 600 mg (2.02 mmol) of bis(trichloromethyl) carbonate and 2.10 ml (15.1 mmol) of triethylamine is added successively to a solution, kept at 0 C., of 1.55 g (4.95 mmol) of 2-(3-aminobenzyl)-6-(3,5-difluorophenyl)-2H-pyridazin-3-one in 20 ml of dichloromethane. 850 mg (5.37 mmol) of 3-(N-methylpiperazine)propan-1-ol is then added, and the reaction mixture is stirred at room temperature for 18 hours. The reaction mixture is partitioned between 1 N NaOH and dichloromethane. The organic phase is dried over sodium sulfate and evaporated. The residue is chromatographed on a silica-gel column with dichloromethane/methanol: 3-(4-methylpiperazin-1-yl)propyl{3-[3-(3,5-difluorophenyl)-6-oxo-6H-pyridazin-1-ylmethyl]phenyl}carbamate as colourless crystals., 5317-33-9

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK PATENT GESELLSCHAFT MIT BESCHRAeNKTER HAFTUNG; US2011/136819; (2011); 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.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

5317-33-9, General procedure: The syntheses of compounds 3-20 were carried out accordingto our previously reported method [17]. Briefly, at room temperature,the acid 2 (150 mg, 0.5 mmol) was acyl chlorinated withthionyl chloride (2.5 mL) and then esterized with various alcoholderivatives in chloroform. The reaction mixture was heated underreflux for 5 h to overnight, and cooled to room temperature. Thesolvent was evaporated under reduced pressure. The crude productwas purified by using silica gel column chromatography to give thetarget product.

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Yang, Hui; Wang, Hao-Wen; Zhu, Teng-Wei; Yu, Le-Mao; Chen, Jian-Wen; Wang, Lu-Xia; Shi, Lei; Li, Ding; Gu, Lian-Quan; Huang, Zhi-Shu; An, Lin-Kun; European Journal of Medicinal Chemistry; vol. 127; (2017); p. 166 – 173;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 55Synthesis of TRV 1094 and TRV 1095toluene / 100C X = CI, BCW 109416h X = F, BCW 1095 TRV 1095[00288] To a degassed solution of 5-bromo-2-fluoro-N-phenylaniline (500 mg, 1.89 mmol), phenyl(piperazin-l -yl)methanonein, (538mg, 2,83 mmol) Cs2C03 ( 1.22g, 3.78 mmol), BINAP ( 55.9 mg, 0.09 mmol) in toluene was charged Pd2(dba)3 ( 86.4 mg, 0.09 mmol). The reaction was sealed under an atmosphere of argon and heated to 100 C for 7h. The mixture was cooled, filtered through celite, washed with ethyl acetate and then concentrated in vacuum. The residue was subjected to silica gel column chromatography (60 % hexane/ ethyl acetate) to furnish the title compound (4-(4- fluoro-3-(phenylamino)phenyl)piperazin-l -yl)(phenyl)methanone, TRV 1095 as an off white solid (387mg, 1.03 mmol) 55%. NMR (500 MHz, CDC13) delta (ppm) 2.90-4.00 (m, 8H), 5.77 (bs, 1H), 6.39 (m, 1H), 6.88 (m, 1 H), 6.97-7.01 (m, 2H), 7.12 (m, 2H), 7.30 (m, 2H), 7.40-7.50 (m, 5H).

13754-38-6, The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; TREVENTIS CORPORATION; REED, Mark, A.; YADAV, Arun; BANFIELD, Scott, C.; BARDEN, Christopher, J.; WO2012/119035; (2012); 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;,
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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.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;,
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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;,
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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

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

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Fluoro-2-methoxy-1-nitrobenzene (2.55 g, 14.9 mmol),N-acetylpiperazine (1.91 g, 14.9 mmol),Potassium carbonate (2.47 g, 17.9 mmol)Was added to N, N-dimethylacetamide (25 mL).The reaction was heated to 120 C for 5 hours. Ethyl acetate (50 mL) was added and the mixture was washed with saturated brine (50 mL). The organic layer was dried, dried and column chromatographed (petroleum ether: ethyl acetate = 5: 1) to give the product as a white solid (1.87 g, yield 45.0 %).

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference：
Patent; Shandong Xuanzhu Pharmaceutical Technology Co., Ltd; Wu, Yongqian; (68 pag.)CN105884695; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The reaction conditions for 1-4.3.28 differ: Under argon atmosphere 1-2.2 (250 mg, 0.54 mmol), potassium carbonate (150 mg, 1.07 mmol), copper (I) iodide (10 mg, 0.05 mmol), Nu,Nu’- dimethylethylendiamine (25 L, 0.23 mmol) and 4-methyl-piperazin-2-one (75 mg, 0.66 mmol) in dioxane (10 mL) are heated to 80 C for 8 d. The reaction mixture is filtered and the solution is concentrated. The residue is purified by reversed phase HPLC. Yield 30%, m/z 500 [M+H]+, rt 0.98 min, LC-MS Method V011 S01.

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; ANDERSKEWITZ, Ralf; GRAUERT, Matthias; GRUNDL, Marc; HAEBEL, Peter, Wilhelm; OOST, Thorsten; PAUTSCH, Alexander; PETERS, Stefan; BINDER, Florian; VINTONYAK, Viktor; WO2014/140075; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics