Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

Example 8: 6-[[2-(Cyclopropylcarbonyl)amino-pyridin-4-yl]oxy]-naphthalene-1-carboxylic acid [4-[(4-methyl-1-piperazinyl)methyl]-3-trifluoromethyl-phenyl]amide; Under an argon atmosphere, a stirred solution of 4-[(4-methyl-1-piperazinyl)methyl]-3- (trifluoromethyl)benzenamine (0.131 g, 0.48 mmol) in dry toluene (5 ml_) is treated with a solution Of AIMe3 (0.6 mL of 2 M in toluene; 1.1 mmol) at 18C. After 30 min, a solution of 3- [[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-1-naphthalenecarboxylic acid, methyl ester (0.174 g, 0.48 mmol) in toluene (5 ml_) is added and the mixture is heated for 2 h at 85- 95C. The cooled mixture is then added to a saturated aqueous solution of NH4CI, stirred for 30 min and extracted with ethyl acetate. The combined extracts are washed (brine), dried (Na2SO4) and solvent is evaporated off under reduced pressure to give a residue, which is purified by column chromatography (SiO2; dichloromethane/methanol/aqueous ammoniaNH3(d 0.88) 95:4.5:0.5) to afford the title compound as a colourless solid, m.p.: 218- 2200C., 694499-26-8

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; WO2008/125691; (2008); A2;,
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.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

A mixture of 4-(4-ethylpiperazin-l-yl)-aniline (1 g, 4.88 mmol), (6-chloro- pyrimidin-4-yl)-methyl-amine (1.81 g, 12.68 mmol, 1.3 eq.), and 4N HC1 in dioxane (15 ml) is heated in a sealed tube to 150C for 5h. The reaction mixture is concentrated, diluted with DCM and a saturated aqueous solution of sodium bicarbonate. The aqueous layer is separated and extracted with DCM. The organic phase is washed with brine, dried (sodium sulfate), filtered and concentrated. Purification of the residue by silica gel column chromatography (DCM/MeOH, 93:7) followed by trituration in diethyl ether affords the title compound as a white solid: ESI-MS: 313.2 [MH]+; tR= 1.10 min (gradient J); TLC: Rf = 0.21 (DCM/MeOH, 93:7)., 115619-01-7

The synthetic route of 115619-01-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; BERGHAUSEN, Joerg; KAPA, Prasad, Koteswara; MCKENNA, Joseph; SLADE, Joel; WU, Raeann; DU, Zhengming; WO2011/71821; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

34770-60-0, Compounds t-butyl-(5-(bromomethyl)-6-(dimethoxymethylpyrid-2-yl)(methyl) aminocarboxylate 15a (70 mg, 0.19 mmol), 174 4-methylpiperazin-2-one (43 mg, 0.38 mmol), 52 sodium hydride (19 mg, 0.47 mmol, 60% 53 mineral oil mixture) and 99 N,N-dimethyl formamide (3 mL) were mixed, and stirred for 1 h at room temperature. This mixture was quenched with 9 water, extracted with dichloromethane (20 mL¡Á3), and the organic phase was washed with saturated brine (20 mL¡Á2). The organic phase was dried over anhydrous sodium sulfate, and filtered to remove the drying agent. The residuals were purified through a preparative silica gel plate (petroleum ether/ethyl acetate 1.5:1), to obtain the target 175 product t-butyl-(6-(dimethoxymethyl)-5-((4-methyl-2-carbonylpiperazin-1-yl)methyl) pyrid-2-yl)(methyl) aminocarboxylate 15b (60 mg, colorless solid), at a yield of 83%. (0274) MS m/z (ESI): 409 [M+1].

34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Nanjing InnoCare Pharma Tech Co., Ltd.; KONG, Norman Xianglong; ZHOU, Chao; ZHENG, Zhixiang; US2019/144427; (2019); 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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A: To a solution of tert-butyl 2-methylpiperazine-1-carboxylate (340 mg, 1.70 mmol) in THF (5 mL) was added sodium hydride (60%, 82 mg, 2.04 mmol). The reaction mixture was stirred at room temperature for 5 min, then methyl 2-chlorobenzoxazole-4-carboxylate (300 mg, 1.41 mmol) in THF (5 mL) was added to the reaction mixture. The reaction mixture was stirred at room temperature for 19 h. The mixture was concentrated under reduced pressure and the resulting residue was purified by column chromatography (silica gel, 20% EtOAc in hexane) to afford methyl 2-(4-(tert-butoxycarbonyl)-3-methylpiperazin-1-yl)benzoxazole-4-carboxylate (336 mg, 63%) as yellow solid. MS consistent.

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMR TECHNOLOGY, INC.; US2008/255114; (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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

The compound (R) -4-Boc-2- methylpiperazine (200mg, 1.00mmol), cyproterone acetate (120mg, 1.20mmol),1- ethyl-3- (3- Dimethylaminopropyl) carbodiimide hydrochloride (287mg, 1.50mmol) and N- hydroxy-7-azabenzotriazole(340mg, 2.50mmol) was dissolved In dichloromethane (20 mL), and under conditions of 0 C tothis solution was added dropwise N, N- diisopropylethylamine (0.70mL, 4.00mmol), room temperature Stirringfor 16h, water was added (10mL ¡Á 2) washing the organic phase was dried over anhydrous Na 2 SO 4, thesolvent was removed concentrate was separated by column chromatography (leaching Lotion: Petroleumether /EtOAc (v / v) = 2/1), to give 260mg of colorless liquid: 1-cyclopropyl-acetyl-4-tert-butoxycarbonyl -2- (R) -Methylpiperazine, yield: 92%., 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); 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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

3022-15-9, piperazine-2-carboxylic acid dihydrochloride (10.0 g, 49.23 mmol) is dissolved in 1:1 dioxane/water (320 ml). 50% Aqueous sodium hydroxide is added to bring the pH to 11. BOC-ON (2-(tert-butoxycarbonyloxyimino)-2-phenylacetonitrile), (15.59 g, 63.32 mmol) is dissolved in dioxane (80 ml) and added dropwise while maintaining the pH at 11 with 50% aqueous sodium hydroxide. The reaction is stirred overnight at ambient temperature. The reaction mixture is then extracted with diethyl ether (5¡Á250 ml) and acidified to pH 2 with concentrated hydrochloric acid. The di-Boc compound is then extracted out with ethyl acetate (4¡Á200 ml) and the acidic aqueous solution containing the desired mono-Boc product is then taken on in the synthesis.

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Aventis Pharmaceuticals Inc.; US7138526; (2006); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78551-60-7, Step 1: 1-Benzyl-4-(tert-butyloxycarbonyl)piperazin-2-thione A mixture of 1-benzyl-4-(tert-butyloxycarbonyl)piperazin-2-one (1.0 mg, 3.4 mmol) and 2,4-bis(4-methoxyphenyl)-1,3-dithia-2,4-diphosphetane-2,4-disulphide (Lawesson’s Reagent) (837 mg, 2.1 mmol) were heated at 90 C. in toluene (10 mL), under nitrogen for 45 min. The mixture was cooled then partitioned between EtOAc (3*50 mL) and water (50 mL). The combined organic layers were dried (Na2 SO4) and evaporated. The residue was chromatographed on silica gel, eluding with CH2 Cl2:EtOAc (100:0?95:5?90:10) to afford the title compound (853 mg, 82%) as a colourless solid. mp. 126-129 C. 1 H NMR (250 MHz, CDCl3) delta 1.47 (9H, s), 3.40-3.44 (2H, m), 3.60-3.65 (2H, m), 4.67 (2H, s), 5.31 (2H, s), 7.31-7.39 (5H, m). MS (ES+) (307, M+1).

As the paragraph descriping shows that 78551-60-7 is playing an increasingly important role.

Reference£º
Patent; Merck Sharp & Dohme Ltd.; US5998415; (1999); 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.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

5271-27-2, EXAMPLE-5 Preparation of 1,2,3,4,10,14b-hexahydro-2-methyl-pyrazino[2,1-a] pyrido{2,3-c} [2]Benzazepine of Formula 17: 1-Methyl-3-phenylpiperazine (50.0 g, 0.284 mol) was heated with 2-chloro-3-cyanopyridine (39.35 g, 0.284 mol) in the presence of potassium fluoride (49.51 g, 0.852 mol) and N,N-dimethylformamide (750.0 ml) as a solvent for 30.0 hrs at 148-154¡ã C., followed by quenching with water and extraction with ethyl acetate gave 1-(3-cyanopyridyl-2-)-4-methyl-2-phenylpiperazine (70.0 g). 1-(3-Cyanopyridyl-2)-4-methyl-2-phenylpiperazine on hydrolysis with saturated alcoholic potassium hydroxide solution (850.0 ml) at 80-85¡ã C. followed by extraction with chloroform gave 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine (20.0 g).

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sebastian, Sonny; Patel, Hetal Virendra; Thennati, Rajamannar; US2002/95038; (2002); 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.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1 : A mixture of lb (4.85g, 16.5mmol) and 9a (16.5g, 0.33mol) in ethanol (50mL) was heated under reflux overnight, then evaporated under high vacuum. The residue was re-dissolved in ethanol and the resulting precipitate was filtered off. The filtrate was concentrated and dried to give crude 9b (4.02g, ca. 100percent).

655225-01-7, As the paragraph descriping shows that 655225-01-7 is playing an increasingly important role.

Reference£º
Patent; TYROGENEX, INC.; LIANG, Congxin; WO2011/41399; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of bromobenzene (300 mg), (S)-2-methylpiperazine (230 mg), (S)-(-)-2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (BINAP) (48 mg), sodium tert-butoxide (266 mg), tris-(dibenzylideneacetone)dipalladium(0) (26 mg) and toluene (15 ml) was stirred at 100 C. for 4 hours under a nitrogen atmosphere. The mixture was cooled to room temperature and saturated aqueous sodium hydrogencarbonate solution was added thereto. The organic layer was separated, washed with brine and dried over magnesium sulfate. The solvent was removed under reduced pressure. The obtained crude product was purified by silica gel column chromatography (chloroform-methanol 20:1) to give the title compound in a pure form. [00204] 1H-NMR (300 MHz, CDCl3) delta 1.11 (d, J=6 Hz, 3H), 2.37 (dd, J=12 Hz,1 Hz, 1H), 2.72 (td, J=12 Hz,3 Hz, 1H), 2.95-3.18 (m, 3H), 3.52 (d, J=12 Hz, 2H), 6.82-6.98 (m, 3H), 7.22-7.29 (m,2H).

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Fujisawa Pharmaceutical Co., Ltd.; US6825200; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics