Month: March 2021

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-(2-(cyclopropanecarboxamido)thiazolo[5,4-b]pyridin-5-yl) benzoic acid (150 mg, 0.44 mmol) and triethylamine (90 muL, 0.66 mmol) in toluene (2 niL) was added diphenylphosphoryl azide (0.11 niL, 0.49 mmol). The resulting mixture was stirred at room temperature for 30 minutes and heated at 80 0C for 1 h. To a reaction mixture was added 4-((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl) aniline (121 mg, 0.42 mmol) and triethylamine (90 muL, 0.66 mmol). The reaction mixture was stirred at 80 0C for 2h and most of organic solvent was removed in vacuo. The crude product was diluted with DMSO (3 mL) and purified by preparative HPLC to give the title compound as a TFA salt.1H NMR 600 MHz (CDCl3) delta 8.51 (s, IH), 7.83 (d, J= 1.8 Hz, IH), 7.48 (m, 2H), 7.19 (m, 3H), 7.12 (m, 2H), 6.85 (J, J= 3.0 Hz, IH), 6.49 (m, IH), 6.19 (m, 2H), 3.84 (m, IH), 3.78 (s, 3H), 3.46 (m, 2H), 3.19 (m, IH), 2.90 (m, 2H), 1.99 (m, 2H), 1.69 (m, 2H), 1.19 (J, J= 6.6 Hz, 6H), MS m/z : 624.36 (M + 1).

630125-91-6, 630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; CHOI, Hwan, Geun; SIM, Taebo; GRAY, Nathanael; ZHOU, Wenjun; CHANG, Jae, Won; ZHANG, Jianming; WEISBERG, Ellen; WO2010/144909; (2010); A1;,
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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.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

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.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.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.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.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

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of piperazine-2-carboxylic acid dihydrochloride (25.0 g, 123 mmol), dioxane (180 ml) and 5N aqueous sodium hydroxide solution (90 ml) was added dropwise di-tert-butyl dicarbonate (62.7 g, 288 mmol) under ice-cooling. The mixture was stirred at room temperature for 4 hr, and the solvent was evaporated under reduced pressure. The residue was washed with ether, and acidified to pH=2-3 with concentrated hydrochloric acid under ice-cooling, and the mixture was extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure to give the object product (31.5 g, 77.6%) as a solid. 1H-NMR (CDCl3) delta; 1.44 (18H, s), 2.87 (1H, br s), 3.08-3.23 (2H, m), 3.76-4.10 (2H, m), 4.51-4.75 (2H, m), 5.07 (1H, br s)., 3022-15-9

As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference£º
Patent; Matsumoto, Takahiro; Kamo, Izumi; Nomura, Izumi; US2009/318412; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1 ,1-dimethylethyl 3,3-dimethyl-1-piperazinecarboxylate (100mg, 0.467mol) in tetrahydrofuran (1 OmL) was added triethylamine (0.098ml_, 0.700 mmol) followed by dropwise addition of benzoyl chloride (0.06OmL, 0.513mmol). The reaction mixture was allowed to stir for 30 minutes. The reaction mixture was diluted with DCM (1OmL) and the solution was washed with saturated sodium bicarbonate solution (1OmL, twice), then (0.1 M, aq) HCI (1OmL). The organic layer was dried (MgSO4), filtered and concentrated in vacuo to yield 1 ,1-dimethylethyl 3,3-dimethyl-4- (phenylcarbonyl)-i-piperazinecarboxylate as a colourless oil (162mg, 100%), MS ES+ve m/z 319 (M+H)To 1 , 1 -dimethylethyl 3,3-dimethyl-4-(phenylcarbonyl)-1 -piperazinecarboxylate (162mg, 0.509 mmol) was added 1 M hydrochloric acid in 1 ,4 dioxane (1 OmL), followed by the addition of 3 drops of water. The reaction mixture was allowed to stir for 62hours. The reaction mixture was reduced in vacuo to yield colourless oil. The colourless oil was dissolved in methanol (1 OmL) and passed down a SCX-2 column washing with two column volumes methanol and eluting the product with three column volumes of 2N ammonia solution in methanol The fraction containing eluted product was reduced in vacuo to yield 2,2-dimethyl-1-(phenylcarbonyl)piperazine as a white solid (81 mg, 63%), MS ES+ve m/z 219 (M+H). To a solution of 2,2-dimethyl-1-(phenylcarbonyl)piperazine (81 mg, 0.318 mmol) in DCM (5m L) was added DIPEA (0.172mL, 0.986 mmol), followed by gradual addition of 4-cyanobenzenesulfonyl chloride (70.5mg, 0.350 mmol). The reaction mixture was allowed to stir for 1 hour.The reaction mixture was diluted with DCM (1 OmL) and the solution was washed with saturated sodium bicarbonate solution (1 OmL, twice), then with distilled water (1OmL). The organic layer was dried (MgSO4), filtered and reduced in vacuo to yield a transparent oil (160mg).The oil was then dissolved in 1 :1 MeCN/DMSO (0.9ml) and purified using MDAP (over 3 batches). The fractions containing product were combined and reduced in vacuo to yield the title compound as a white solid (48mg, 32%)1H-NMR (CDCI3) 51.58 (6H, s), 3.00 (2H, s), 3.15 (2H, t, J=5.6Hz), 3.47 (2H, t, J=5.6Hz), 7.31-7.48 (5H, m), 7.84-7.93 (4H, m).MS ES+ve m/z 384 (M+H).

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

Reference£º
Patent; GLAXO GROUP LIMITED; BESWICK, Paul, John; CAMPBELL, Alister; CRIDLAND, Andrew; GLEAVE, Robert, James; PAGE, Lee, William; WO2010/102663; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics