Heterocyclic Building Blocks-piperazine

639068-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of potassium carbonate (1.4370 g, 10.40 mmol) in water (3 mL) was added to a mixture of l-N-/-Boc-3,5-dimethyl piperazine (0.6882 g, 3.21 mmol) and mPEG3- Br (0.8872 g, 3.91 mmol) in a vial. The resulting mixture was heated at 120 ¡ãC for 1.5 h by using microwave. The mixture was diluted with water, extracted with dichloromethane (3 x 30 mL). The combined organic solution was washed with brine, dried over brine, concentrated. The residue was dried under high vacuum. The residue was separated with flash column chromatography on silica gel column using 1-5percent methanol/dichloromethane, and NH-column using 0-5percent methanol/ dichloromethane to afford the intermediate.

639068-43-2 tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 22219990, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); 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.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, A mixture of 0.3 g (1.12 mmol) of the product prepared in step 2.6 and 491 mg (2.24 mmol) of the product prepared in step 2.2 in 6 mL of NMP is placed in a 10 mL microwave tube. The sealed tube is placed in a microwave oven (CEM machine, Discover model) and the mixture is heated under pressure at 120 C. for 60 minutes at a power of 75 W, and then cooled to room temperature. 15 mL of water and then 5 mL of saturated aqueous NaHCO3 are added and the precipitate formed is drained by suction and then dried in an oven. The crude solid is purified by chromatography on a column of silica, eluting with a dichloromethane/methanol gradient (100/0 to 90/10). 0.055 g of the expected product is obtained in the form of an orange powder. m.p.=281 C. %. M+H+=451. Yield=11%. 1H NMR (DMSO-d6, 400 MHz): delta 11.8 (broad s, 1H); 10.3 (s, 1H); 10.2 (d, 1H); 9.0 (s, 1H); 8.0 (broad s, 1H); 7.8 (d, 2H); 7.40 (d, 2H); 7.2 (d, 1H); 4.4 (q, 2H); 3.5 (m, 4H); 3.30 (s, 3H); 2.30 (m, 4H); 1.3 (t, 3H).

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SANOFI; US2012/277220; (2012); 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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.,59702-07-7

Preparation of compound 30a: 4-(6-(5-(5-(4-methoxybenzylamino)-l,3,4-thiadiazol- 2-yl)-l-tosyl-lH-indol-3-yl)pyridin-2-yl)-l-methylpiperidin-2-oneA glass microwave reaction vessel was charged with 5-(3-(6-fluoropyridin-2-yl)-l-tosyl- lH-indol-5-yl)-N-(4-methoxybenzyl)-l,3,4-thiadiazol-2-amine (300 mg, 0.512 mmol) and l-methylpiperazin-2-one (117 mg, 1.024 mmol) in NMP (5 mL) followed by Et3N (214\L, 1.537 mmol). The reaction was stirred and heated in an oil bath at 150 ¡ãC for 60 h, and the mixture was diluted with DCM and washed with H20, brine, dried, filtered and concentrated to give the crude product. MS (ESI, pos. ion) m/z: 680 (M+1).

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMGEN INC.; WANG, Hui-Ling; CEE, Victor, C.; HERBERICH, Bradley, J.; JACKSON, Claire, L., M.; LANMAN, Brian, Alan; NIXEY, Thomas; PETTUS, Liping, H.; REED, Anthony, B.; WU, Bin; WURZ, Ryan; TASKER, Andrew; WO2012/129338; (2012); 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.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