Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of starting material (25 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-1-yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in t-BuOH (1.5 mL) was heated at 100 C. in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The solvent was removed in vacuo and the residue was purified by ISCO to afford the title compound (24.7 mg)., 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£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (2016); 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.

Step 1: Preparation of 3-iodo-4-methyl-N-[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylphenyl]benzamide 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline (2.27 g, 8.3 mmol), 3-iodo-4-methyl-benzoyl chloride (10 mmol), 15 ml tetrahydrofuran, and 10 ml triethylamine were added into a reactor and stirred at room temperature for 4 hours. After completion of the reaction, the resultant was washed with a saturated NaHCO3 solution, extracted with ethyl acetate and water, washed with a saturated NaCl solution, dried over anhydrous Na2SO4. The solvent was removed by distillation under reduced pressure. The residue was purified by silica gel column chromatography, to give a yellow oily matter. 1H NMR (500 MHz, CDCl3) delta: 8.39(s,1 H,N-H), 8.29(s,1 H,Ar-H), 7.88(d, 1 H, Ar-H), 7.86(s, 1 H, Ar-H), 7.75(d, 1 H, Ar-H), 7.73(d, 1 H, Ar-H), 7.28(d, 1 H, Ar-H), 3.62(s, 2H, PhCH2), 2.60(b, 8H, 4x-CH2), 2.47(s, 3H,-CH3), 2.31 (s, 3H,-CH3)., 694499-26-8

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; WANG, Yong; ZHAO, Liwen; ZHANG, Wenping; CHEN, Hongyan; BI, Sheng; GAO, Yiping; CHEN, Hongbin; LIU, Yang; XU, Xin; ZHANG, Cang; EP2896620; (2015); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

2,2-dimethylpiperazine (1 1 .5 kg, 101 mol) was dissolved in ethanol (48.5 L) and the solution was cooled to approximately 9C. Di-tert-butyl dicarbonate (21 .9 kg, 100 mol) was dissolved in ethanol (41 .7 L). The solution of di-tertbutyl dicarbonate was added to the solution of dimethylpiperazine over a period of 2 h 30 min, keeping the temperature of the reaction below 15C. Ethanol (12.4 L) was added and the solution was stirred overnight at a temperature between 12-25C. The reaction was warmed to reflux and 75 L were distilled off. Ethanol (76 L) was added to the reaction and the solution was heated to 52C and transferred to a suspension of D,L-tartaric acid (7.5 kg, 50.0 mol) in ethanol (25.2 L), and warmed to 51 C. Ethanol (25.3 L ) was added and the reaction was kept at 20C overnight. The precipitate was filtered off and washed with ethanol (28.1 L). The solid was dried in a vacuum oven at 50C overnight to yield compound (XVIII) (27.1 kg, 93%) with 99% purity according to GC analysis.

259808-67-8, As the paragraph descriping shows that 259808-67-8 is playing an increasingly important role.

Reference£º
Patent; H. LUNDBECK A/S; JACOBSEN, Mikkel Fog; BRANDES, Sebastian; WO2014/96151; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,31166-44-6

Step 1 : benzyl 4-((l-(tert-butoxycarbonyl)piperidin-4-yl)methyl)piperazine-l-carboxylate Sodium triacetoxyborohydride (1732 mg, 8.17 mmol) was added to a mixture of benzyl piperazine-l-carboxylate (600 mg, 2.72 mmol), tert-butyl 4-formylpiperidine-l-carboxylate (697 mg, 3.27 mmol) and acetic acid (156 uL, 2.72 mmol) in DCM (14 mL) at room temperature. After stirring at room temperature overnight, the mixture was quenched with sat. NaHCC , the aq. layer was CH2CI2 extraction (2X20 mL). The combined org. fractions were dried over Na2SC>4 and concentrated to dryness. The residue was purified by ISCO column chromatography (silica gel ISCO 24 g prepacked, eluting with 0-100percent EtOAc/Hexane) to give the title compound (693 mg). LCMS m/z (M+H): Calc’d 418.2, found 418.4.

31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; RUDD, Michael, T.; BENNETT, David Jonathan; WAI, Jenny; MENG, Zhaoyang; (257 pag.)WO2017/95758; (2017); 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.259808-67-8,1-Boc-3,3-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Reference Example 46 2-(2,2-Dimethyl-piperazin-l-yl)-acetamideTo a solution of 3,3-dimethyl-piperazine-l-carboxylic acid tert-butyl ester (0.55 g, 2.57 mmol) in acetonitrile (10 mL) were added 2-bromoacetamide (0.42 g, 3.08 mmol), potassium carbonate (1.06 g, 7.70 mmol) and tetrabutylammonium iodide (95 mg, 0.257 mmol). The reaction mixture was heated at 60 C for 18 h, then concentrated in vacuo. The resulting residue was partitioned between DCM and water. The organic layer was separated, dried (Na2SO4), and concentrated in vacuo to give 4-carbamoylmethyl-3,3-dimethyl- piperazine-1-carboxylic acid tert-butyl ester as a cream solid. 4-Carbamoylmethyl-3,3- dimethyl-piperazine-1-carboxylic acid tert-butyl ester was subsequently BOC-deprotected by using the general method to give the title compound as a white solid (0.43 g, 97 %). [M + H]+ 172.1, 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; F.HOFFMANN-LA ROCHE AG; WO2009/53716; (2009); 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.150407-69-5,(S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

DIEA (0.3 mL) and HATU (0.63 g) were added to (S)-1-((benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (0.6 g) in DCM (20 mL), and the mixture was stirred for 30 min. Intermediate 1 (1.5 g) was then added, and the mixture was stirred o.n. Volatiles were removed under vacuum evaporated, and the residue taken into EtOAc (60 mL), washed with 0.2% HCl (3×20 mL), sat. NaHC03 (2×15 mL), brine (15 mL), and dried (Na sulfate). Solvent was evaporated under vacuum and the crude product purified by silica gel chromatography (gradient 0-12% MeOH in DCM)., 150407-69-5

150407-69-5 (S)-1-((Benzyloxy)carbonyl)-4-(tert-butoxycarbonyl)piperazine-2-carboxylic acid 1512536, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; MICURX PHARMACEUTICALS, INC.; GORDEEV, Mikhail Fedorovich; LIU, Jinqian; WANG, Xinghai; YUAN, Zhengyu; (134 pag.)WO2016/100578; (2016); 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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, To the mixture of 450 mg 1-methylpiperazin-2-one (3.00 mmol) and 1.00 g K2C03 (7.24 mmol) in 5 mL TI-IF I mL 2-bromoethanol (14. Immol) was added and the mixture was stirred at 65¡ãC for 16h. The mixture was cooled to room temperature, filtered andconcentrated under reduced pressure. The residue was purified via flash chromatography using DCM and MeOH to give 4-(2-hydroxyethyl)-1-methyl-piperazin-2-one.MS: (M+H) 159.4.

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; KOTSCHY, Andras; SZLAVIK, Zoltan; CSEKEI, Marton; PACZAL, Attila; SZABO, Zoltan; SIPOS, Szabolcs; RADICS, Gabor; PROSZENYAK, Agnes; BALINT, Balazs; BRUNO, Alain; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; CHEN, I-Jen; PERRON-SIERRA, Francoise; WO2015/97123; (2015); 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.304897-49-2,tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

solution of tert-butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (0.900 g, 3.089mmol), pyridine (0.299 mL, 3.706 mmol) and ethanesulfonyl chloride (0.477 g, 3.706 mmol) in dichloromethane (30 mL) was stirred at the room temperature for 12 hr. Then, water was added to the reaction mixture, followed by extraction with dichloromethane. The organic layer was washed with aqueous saturated ammonium chloride solution, dried with anhydrous MgSO4, filtered, and concentrated in vacuo. The residue was chromatographed (Si02, 12 g cartridge; ethyl acetate / hexane = 0 % to 40 %) to give tert-butyl 4-(4-(ethylsulfonamido)benzyl)piperazine-1-carboxylate as yellow solid (0.800 g, 67.5 %).

304897-49-2, 304897-49-2 tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate 12045001, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; CHOI, Daekyu; MIN, Jaeki; BAE, Miseon; YANG, Hyunmo; KIM, Dohoon; (644 pag.)WO2017/18803; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of tert-butyl 4-(4-bromobenzyl)-3-oxopiperazine-] -carboxylate (89)Sodium hydride (60% dispersion in mineral oil, 0.72g, l8mmol) was added to a suspension of 4-Boc-piperazinone (88) (3g, lSmmol) in DMF (30m1) under argon. The reaction mixture was stirred at room temperature for 30 minutes, and 4-bromobenzylbromide (87)(4.5g, l8mmol) was added. The reaction mixture was heated at 60 C for one hour, cooled down, diluted with ethyl acetate (lOOml) and washed with water (1 OOml) and brine (lOOml). The ethylacetate solution was dried over sodium sulfate, and concentrated. The crude material was purified with automated column chromatography using petroleum ether and ethyl acetate as eluents to give 1 -((3,5 ?-bis(trifluoromethyl)- [1,1 ?-biphenyll -4-yl)methyl)piperazin-2-one (89)(5.33g) as off white solid. Yield: 96%. Synthesis confimed by LCMS and MS (positive ion mode).

76003-29-7, The synthetic route of 76003-29-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ZALICUS PHARMACEUTICALS LTD.; PAJOUHESH, Hassan, A.; HOLLAND, Richard; ZHANG, Lingyun; PAJOUHESH, Hossein, O.; LAMONTAGNE, Jason; WHELAN, Brendan; SHORT, Glenn, F., III.; ROMERO, Donna, L.; WO2013/131018; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

200 mg of intermediate VIII was dissolved5 ml of N, N-dimethylacetamide,To the system was added 454 mul of N, N-diisopropylethylamine,360 mg of benzotriazole-N, N, N ‘, N’-tetramethyluronium hexafluorophosphate,Stir added 107.27 mg of 1-cyclopropylmethyl-formyl piperazine,After 24 hours of reaction at room temperature,The reaction was stopped, water was added to the system and extracted with methylene chloride. The organic layer was subjected to column chromatography to give 85.8 mg (I-1) as a white solid in 30% yield., 59878-57-8

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; East China University of Science and Technology; Shanghai Institute of Materia Medica Chinese Academy of Sciences; Li, Jian; Miao, Zehong; Ding, Jian; Jiang, Hualiang; Liu, Yunxia; Huan, Xiajuan; Song, Shanshan; Chen, Yi; Ren, Guobin; (46 pag.)CN104003940; (2017); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics