Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

Thus, in a first step and in accordance with what is described in WO 01/27081, 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone is prepared as follows. 10.5 g (30.0 mmol) 1-acetyl-3-(1-ethoxy-1-phenylmethylene)-6-methoxycarbonyl-2-indolinone (prepared as described in WO 01/27081) and 8.60 g (33.0 mmol) N-[(4-methyl-piperazin-1-yl)-methylcarbonyl]-N-methyl-p-phenylendiamine (prepared as described in WO 01/27081) are dissolved in 80 ml dimethylformamide and mixed for 1 hour at 80C. After cooling, 6.50 ml piperidine is added and the whole is further mixed for 2 hours at room temperature. Water is added, the liquid over the resulting precipitate is sucked up, and the precipitate is washed again with a low quantity of water. The residue is suspended in 200 ml methanol, the liquid is sucked up, and the remaining residue washed with cold water and diethylether. The resulting product is vacuum dried at 110 C. [] Recovered product:12.4 g (77% of theoretical value)IR-spectroscopy:1610, 1655, 1711 cm-1 Tsmp. =253CMolecular formula: C31H33N5O4 Electrospray-mass spectrometry: m/z = 540 [M+H]+ [] Element analysis: calculatedC 68.99H 6.16N 12.98foundC 68.32H 6.29, 262368-30-9

262368-30-9 N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide 21927707, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Boehringer Ingelheim Pharma GmbH & Co.KG; EP1473043; (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.55112-42-0,4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride,as a common compound, the synthetic route is as follows.

55112-42-0, Example 3: Preparation of Zopiclone in Acetone[0066] l-Chlorocarbonyl-4-methyl piperazine hydrochloride (4.92g) in acetone (50 ml) was stirred mechanically at room temperature for 5 min. Then Et3N (4.42g) was added to the slurry over 10 min. During the tri-ethyl amine (Et3N) addition, the temperature rose slightly. After Et3N addition ended, DMAP (0.46g) was added to the slurry, and after 1-2 min of stirring, 7-OH-Py (5g) was added. The reaction mixture was heated to reflux and stirred at reflux for 4 h. After 4h at reflux, heating was stopped and the slurry was cooled to room temperature and ice (~50g) was added. Temperature dropped to -6C and the slurry was stirred till the temperature reached about 200C. The solid was filtered, washed with water (10 ml), and dried in vacuum oven at 400C overnight to obtain zopiclone crude product (6.95g yield 89%; purity 99.62% by HPLC).

55112-42-0 4-Methyl-1-piperazinecarbonyl Chloride Hydrochloride 3016934, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/2629; (2008); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

Intermediate 9: 3-(4-Methylpiperazin-1-yl)-propan-1-ol. 1-Methylpiperazine (6.99 mL, 63 mol) was dissolved in toluene (30 mL). 3-Bromopropanol (2.62 mL, 30 mmol) was added slowly and the mixture was stirred overnight at r.t.. After heating to 80C for 2 h and cooling to r.t., the mixture was filtered and the filter cake was thoroughly washed with toluene. After removal of the solvent, the residue was subjected to Kugelrohr distillation (b.p., 180C / 2 mbar) to obtain a colourless oil (4.08 g, 25.8 mmol, 86 %). 1H NMR (CDCl3): delta = 1.70 (Psi-quint, J ? 5.8 Hz, 2 H), 2.26 (s, 3 H), 2.35-2.6 (m, 8 H), 2.60 (Psi-t, J = 5.8 Hz, 2 H), 3.77 (Psi-t, J ? 5.3 Hz, 2 H), 4.09 (s, br., 1 H).

109-01-3, 109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; 4SC AG; EP1674466; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 20-mL screw-cap vial, 100 mg (0.3 mmol) 2-(2-chlorophenyl)-1-(4-chlorophenyl)- 1H imidazole-4-carboxylic acid, 87 mg (0.33 mmol) TFFH, and 5.0 equiv. PS-DIEA (loading level: 3.50 mmol/g, 429 mg, 1.5 mmol) were heated in 8 mL 1,2-dichloroethane at 35C overnight. The formation of acyl fluoride was monitored by LC-MS. To the mixture, 1.1 equiv. (76 mg, 0.33 mmol) 1-(4-trifluormethylphenyl)-piperazine was added and the reaction continued overnight. The mixture was filtered through a filter tube (polypropylene frit), and the filtrate was evaporated under reduced pressure. The crude product was redissolved in 1 mL MeOH and purified by preparative HPLC to give 45.9 mg of 1-{ [2-(2-chlorophenyl)-1-(4-chlorophenyl)-1H-imidazol-4- yl]carbonyl}-4-[4-(trifluoromethyl)phenyl]piperazine as the trifluoroacetate salt (yellow oil, 23% yield). ?H NMR (400 MHz, CD3COCD3) No. 7.95 (s, 1 H), 7.60 (m, 1 H), 7.30-7.50 (m, 7 H), 7.25 (d, 2 H), 7.05 (d, 2 H), 4.5 (bs, 2 H), 3.80 (bs, 2 H), 3.35 (m, 4 H) ; LC-MS m/z 545.3 (MH+), retention time 4.21 min (method 2), 30459-17-7

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER PHARMACEUTICALS CORPORATION; WO2005/99705; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57184-25-5, 1-(Cyclopropylmethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57184-25-5, 4-Cyclopropylmethyl-piperazine-1-Carboxylic acid 4-(4,4-dimethyl-2,6-dioxo-piperidin-1-yl)-phenyl Ester The title compound was prepared from 4-(4,4-dimethyl-2,6-dioxo-piperidin-1-yl)-phenyl chloroformate and 1-cyclopropylmethyl-piperazine, preparative HPLC (Method C) (45%, off-white crystals). HPLC-MS m/z=400.3 (M+1), Rt: 1.83 min.

As the paragraph descriping shows that 57184-25-5 is playing an increasingly important role.

Reference£º
Patent; Ebdrup, Soren; de Jong, Johannes Cornelis; Jacobsen, Poul; Hansen, Holger Claus; Vedso, Per; US2003/166644; (2003); 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.414910-15-9,tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1-Tertbutoxycarbonyl-4-(cyclopropanecarbonyl) piperazine (190 mg, 0.75 mmol) was dissolved in dichloromethane, and then trifluoroacetic acid (1 mL) was added. The reaction mixture was stirred at room temperature until complete reaction, and then washed with saturated sodium bicarbonate solution for three times. The organic phases were concentrated to give 112 mg (yield 97%) pale yellow solid of N-(cyclopropanecarbonyl) piperazine for use., 414910-15-9

414910-15-9 tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate 968936, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Chengdu Di’ao Pharmaceutical Group Co. Ltd.; JI, Jianxin; GUO, Na; XUE, Ting; KANG, Bingqiang; YE, Xinfa; CHEN, Xin; ZHANG, Tao; EP2799435; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of K2CO3 (8.8 g, 63.8 mmol), l-fluoro-3 -nitrobenzene (3 g, 21.3 mmol), and (S)-tert-butyl-2-methylpiperazine-l-carboxylate (4.26 g, 21.3 mmol) in DMSO (80 mL) was stirred at 130C for 16 hrs. The mixture was then filtered and the filtrate was washed with water, extracted with EtOAc, and purified by chromatography (silica, EtOAc/PE = 1/10) to afford (,S)- tert-butyl-2-methyl-4-(3-nitrophenyl)piperazine-l-carboxylate (1.98 g, 6.18 mmol, 29%). ESI-MS (EI+, m/z): 222.2 [M-99]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NAVITOR PHARMACEUTICALS, INC.; O’NEILL, David John; SAIAH, Eddine; KANG, Seong Woo Anthony; BREARLEY, Andrew; BENTLEY, Jonathan; (184 pag.)WO2018/89493; (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.1235865-77-6,2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl)methyl)piperazin-1-yl)benzoic acid (100 mg, 0.175 mmol)Ethyl 8-(2-nitro-4-aminosulfonylphenylamino)octanoate 68mg (0.175mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI) 167mg (0.875mmol), 4- dimethylaminopyridine 25.6mg (0.21mmol) ,With anhydrous DCM as solvent, at room temperature for 24h. After the reaction was completed, with 1 M hydrochloric acid,Saturated sodium bicarbonate, saturated brine, the aqueous phase was extracted with EA, the organic phase was combined,Concentration gave 160 mg of a solid which was purified by column chromatography with a yield of 85%., 1235865-77-6

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Second Military Medical University; Zheng Canhui; Zhu Ju; Zhou Youjun; Wang Zhongqing; Wang Mingping; Yang Chao; Tian Wei; (18 pag.)CN106957315; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,70261-82-4

To a solution of 4-(3-(4-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)benzoic acid (70 mg, 0.206 mmol) in DMF (1.0 mL) were added HATU (117 mg, 0.309 mmol), N-methyl morpholine (90 muL, 0.824 mmol) and 4-((4-methylpiperazin-1-yl)methyl)aniline (51 mg, 0.309 mmol). The reaction mixture was stirred at room temperature under inert atmosphere for 18 h, then it was diluted with water (15 mL) and extracted with EtOAc (3*30 mL). The combined organic layer was dried over Na2SO4 and was concentrated under reduced pressure. The residue was purified by preparative HPLC (C18, eluent ACN, water, formic acid 0.1%) to afford 4-(3-(4-cyanophenyl)imidazo[1,2-a]pyridin-6-yl)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)benzamide (40 mg, 37%, AUC HPLC 99%) as a white solid. 1H NMR (400 MHz, CD3OD) delta 8.78 (s, 1H), 8.05 (d, J=8.4 Hz, 2H), 7.96-7.90 (m, 4H), 7.84 (s, 1H), 7.83 (d, 0.1=8.4 Hz, 2H), 7.80-7.76 (m, 2H), 7.68 (d, J=8.8 Hz, 2H), 7.34 (d, J=8.4 Hz, 2H), 3.56 (s, 2H), 2.70-2.40 (m, 8H), 2.36 (s, 3H); 13C NMR (100 MHz, CD3OD): delta 168.12, 147.47, 141.62, 139.17, 135.76, 134.82, 134.74, 134.53, 134.40, 131.08, 129.56, 129.44, 128.49, 128.30, 127.79, 126.61, 122.95, 122.18, 119.51, 118.48, 112.72, 63.14, 55.55, 53.15, 45.65; MS (ESI) m/z 527 [C33H30N6O+H]+.

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Agency for Science, Technology and Research; Nacro, Kassoum; Duraiswamy, Athisayamani Jeyaraj; Rao, Lohitha; US2014/371199; (2014); 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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

A mixture of 1 -bromo-4-iodobenzene (0.87 g, 3.1 mmol), 4-methylpiperazin-2- one (0.30 g, 2.6 mmol), 3P04 (1.1 g, 5.1 mmol), trans-N, N’-dimethylcyclohexane-l ,2-diamine (0.08 mL, 0.51 mmol) and dioxane (5 mL) was purged with argon gas for 10 min. Copper(I) iodide (0.049 g, 0.26 mmol) was added, the vial sealed and heated at 110 C in an oil bath for 22 h. The reaction was then allowed to cool to rt and was diluted with EtOAc and saturatedNaHC03 was added. The resulting mixture was extracted with EtOAc and the combined organic extracts were dried over MgS04 and concentrated to give the crude product. Purification by silica gel chromatography (MeOH/CH2Cl2, 5:95 to 1 :9) gave an inseparable 2: 1 mixture of the desired product and l-(4-bromophenyl)-4-methylpiperazin-2-one (200 mg). NMR (400 MHz, CDCI3) 6 7.66 (d, J = 8.0 Hz, 2H), 7.02 (d, J = 8.0 Hz, 2H), 3.64 (t, J = 5.0 Hz, 2H), 3.22 (s, 2H), 2.73 (t, J = 5.0 Hz, 2H), 2.35 (s, 3H); MS ESI 317.1 [M + H]+, calcd for [C, ,H|3IN20+ H]+ 317.01.

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

Reference£º
Patent; UNIVERSITY HEALTH NETWORK; PAULS, Heinz, W.; LI, Sze-Wan; SAMPSON, Peter Brent; FORREST, Bryan T.; WO2012/48411; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics