Heterocyclic Building Blocks-piperazine

5294-61-1, N-(2,6-Dimethylphenyl)-2-(piperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5294-61-1

To a solution of benzyl OXIRAN-2-YMETHYLCARBAMATE (12mmoles, 2. 5G) in ethanol (LOOML) was added triethylamine (24mmoles, 3. 34ML), followed by the addition of N- (2, 6- DIMETHYLPHENYL)-2-PIPERAZINYLACETAMIDE (24mmoles, 5.94g), a compound of formula (4). The resulting mixture was refluxed for 18 hours, then solvent removed from the reaction mixture under reduced pressure. The residue was purified by column chromatography on silica gel, eluting with 5% MEOH/DICHLOROMETHANE to give N-(2, 6-DIMETHYLPHENYL)-2-(4- {2-HYDROXY-3- [(PHENYLMETHOXY) carbonylamino] propyl} piperazinyl) acetamide, a compound of formula (5), as an off-white solid. Yield: 2.25g.

As the paragraph descriping shows that 5294-61-1 is playing an increasingly important role.

Reference£º
Patent; CV THERAPEUTICS, INC.; WO2004/63180; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 242 3-(2-chloro-6-fluoro-phenyl)-7-methylsulfanyl-2H-pyrimido[5,4-e][1,3]oxazin-4-one (150 mg, 0.462 mmol, 1.0 eq) in 24 toluene (3 mL) was added 25 m-CPBA (199 mg, 1.16 mmol, 2.5 eq) and allowed to stir at rt for 30 min. 66 Tert-butyl 4-(4-aminophenyl) piperazine-1-carboxylate (128 mg, 0.462 mmol, 1.0 eq) and 27 DIPEA (238 mg, 1.85 mmol, and 4.0 eq) were added and allowed to stir at rt for 1 h. Progress of reaction was monitored by LCMS. After completion of reaction, precipitated compound was filtered off and washed with toluene (2 mL) and dried under vacuum to afford 188 tert-butyl 4-[4-[[3-(2-chloro-6-fluoro-phenyl)-4-oxo-2H-pyrimido[5,4-e][1,3]oxazin-7-yl]amino]phenyl]piperazine-1-carboxylate (90 mg, 35.1%). LCMS: 555 [M+1]+, 170911-92-9

As the paragraph descriping shows that 170911-92-9 is playing an increasingly important role.

Reference£º
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

Example 12 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol OR 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11-piperazinyldibenzo[b,f][1,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25-30 C., and was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 mole)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110-112 C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check for absence of compound of Formula IV) and was cooled to 25 C. to 30 C. To which, was added 150 cc DM water, then the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extract and the organic layer were combined, to which was added 250 cc water and was acidified with acetic acid to obtain a pH of 2-3. The reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The extract and the organic layer were combined, to which was washed with DM (dimineralized) water 300 cc twice. The organic layer was distilled off under vacuum below 70 C. to afford 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol. Purity of 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol was 99.0% (area % by HPLC).

5747-48-8, As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; Kansal, Vinod Kumar; Ahmad, Suhail; Lal, Kanhaiya; Patil, Bhatu Tumba; US2008/241949; (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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(a) (2S,5R)-4-(5-Methoxycarbonyl-pyridin-2-yl)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester A mixture of 6-fluoronicotinic acid methyl ester (200 mg, 1.29 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester was heated at 120 C in DMSO (2.0 mL) with potassium carbonate (178 mg, 1.29 mmol) for 2 h. The reaction mixture was partitioned between ethyl acetate (20.0 mL) and water (5.0 mL). The organic layer was washed with water (2 x 5.0 mL), dried over sodium sulfate, filtered and concentrated to give the title intermediate as a yellowish oil.

548762-66-9, 548762-66-9 (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate 11745988, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Theravance Biopharma R&D IP, LLC; MCKINNELL, Robert Murray; LONG, Daniel D.; VAN ORDEN, Lori Jean; JIANG, Lan; LOO, Mandy; SAITO, Daisuke Roland; ZIPFEL, Sheila; STANGELAND, Eric L.; LEPACK, Kassandra; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; EP2635571; (2015); B1;,
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Piperazines – an overview | ScienceDirect Topics

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 5 This Example illustrates the preparation of (R or S) N- (3- [4- methanesulphonylpiperazinyl]-3-phenylpropyl)-4- [2- (4-fluorophenylsulphonyl) ethyl] – piperidine (Compound 14, Table III). A solution of (R or S) N- (3-chloro-3-phenylpropyl)-4- [2- (4-fluorophenylsulphonyl)- ethyl] -piperidine (Method F; 310 mg) in dichloromethane (6 ml) was added to N- methanesulphonyl-piperazine hydrochloride (150 mg) followed by triethylamine (313)-D). The mixture was stirred for 48 hours, diluted with dichloromethane (5 ml) and MP-carbonate resin (1.34g), PS-ISOCYANATE resin (682 mg) and PS-thiophenol resin (577 mg) were added. The mixture was stirred for 5 hours, filtered and the resins were washed with 10% methanol in dichloromethane (2×25 ml). The combined filtrates were evaporated to dryness and the residue was passed through a 20g Isolute column eluted with a solvent gradient of ethyl acetate-10% methanol/ethyl acetate to give the title compound, yield 81 mg; MH+ 552. NMR (CDCL3) : 1.12-1. 32 (m, 4H), 1.52-1. 66 (m, 4H), 1.76-1. 93 (m, 3H), 2.08 (m, 1H), 2.21 (m, 1H), 2.47-2. 51 (m, 4H), 2.71 (s, 3H), 2.77-2. 88 (m, 2H), 3.03-3. 10 (m, 2H), 3.12-3. 21 (m, 4H), 3.37 (m, 1H), 7.14 (d, 2H), 7.15-7. 32 (m, 5H), 7.88 (m, 2H)., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; WO2004/56773; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,103-76-4

In THF (30 ml) were added N-(2-hydroxyethyl)piperazine (500 mg, 3.84 mmol), a solution of formaldehyde (3117 mg, 38.41 mmol) and sodium cyanoborohydride (1207 mg, 19.20 mmol). The mixture was heated up to 50 C. overnight under stirring. After cooling some water was added and the mixture was extracted with DCM (3¡Á). The organic layers were dried over MgSO4 and evaporated. The residue was purified over a silica plug with DCM/MeOH 9:1 as eluant to afford an oil (370 mg, Y=67%). 1H NMR (DMSO-d6) delta 4.45 (t, J=5.3 Hz, 1H), 3.51-3.45 (m, 2H), 3.02-2.84 (m, 4H), 2.71-2.64 (m, 2H), 2.61 (s, 3H), 2.58-2.53 (m, 2H), 2.47-2.43 (m, 2H).

As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference£º
Patent; ARES TRADING S.A.; US2008/51397; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 1-(4-fluorophenyl)-2-piperazinone used in the above procedure was prepared as follows:A mixture of 2-piperazinone (1.5 g, 15.0 mmol), 1-fluoro-4-iodobenzene (3.5 ml, 30.0 mmol), copper(l) iodide (0.57 g, 3.0 mmol), N,N’-dimethyl-1 ,2-cyclohexanediamine (0.95 ml, 6.0 mmol) and potassium phosphate (9.5 g, 44.9 mmol) in 1 ,4-dioxane (20 ml) was heated at reflux (1 10 0C) under argon for 24 hours. The mixture was allowed to cool to room temperature and then diluted with methanol, and filtered through a pad of celite, washing with methanol. The filtrate was evaporated in vacuo and the resulting residue was dissolved in dichloromethane and 0.88 aqueous ammonia solution (~5ml) in water (~30ml). The mixture was then extracted into dichloromethane (x3), and the combined organic extracts were washed with water (x1 ) and dried over magnesium sulphate. The solvent was evaporated in vacuo and the crude product was purified further by column chromatography on flash-silica gel, eluting with 0-10percent methanol in dichloromethane. The relevant fractions were combined and the solvent was evaporated in vacuo. The residue was purified by SCX, eluting first with methanol and then with 2M ammonia in methanol. The basic fractions were combined and the solvent was evaporated in vacuo to give crude product which was purified again by flash-silica gel column chromatography, eluting with 20percent 2M ammonia in methanol in dichloromethane, to give 1-(4-fluorophenyl)-2- piperazinone (560 mg) as a colourless solid. LC/MS [M+H]+ = 195., 5625-67-2

5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2009/53459; (2009); 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

Stepl: To a solution of 1 (0.31 g, 1.43 mmol) in THF (20 mL) was added Ti(OEt)4 (0.595 g, 2.58 mmol) and N-(4-trifluoromethylphenyl)-piperazine 2 (0.3 g, 1.3 mmol). The mixture was stirred at 40’C for 24h, quenched by adding ice- water, extracted with ethyl acetate (3 x 20 mL), dried. Purification by column chromatography (PE/EA:1/1) gave product 3 (0.25 g, 41%)., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; COGNITION THERAPEUTICS, INC.; CATALANO, Susan, M.; RISHTON, Gilbert; IZZO, Nicholas, J.; WO2013/29057; (2013); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0138]1-(2-hydroxyethyl)piperazine (Compound 3) (16.6 g, 127.6 mmol)) and 2-methyl-4,6-dichloropyrimidine (Compound 2) (10.4 g, 63.8 mmol) were mixed with methylene dichloride (80 mL) in reaction flask to be stirred for 2.5 h at 30 C., and then triethylamine (1.8 mL) was added with the reaction overnight in thermal insulation. After vacuum filtration, the cake was rinsed by methylene dichloride. The filtrate was vacuum condensed to dry, and then n-hexane (40 mL) was added to grow the grains for 1 h by stirring. After vacuum filtration, the cake was rinsed by n-hexane (20 mL) and dried at 40 C. to constant weight to give white solid target Compound 4 (14.7 g, yield: 89.8%).[0139]Element analysis: C11H17ClN4O, Calculated: C, 51.46; H, 6.67; N, 21.82. Found: C, 51.45; H, 6.69; N, 21.82.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nan Jing Cavendish Bio-Engineering Technology Co. Ltd.; Yan, Rong; Yang, Hao; Hou, Wen; Xu, Yongxiang; US2013/30177; (2013); 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A mixture of 2- (5-amino-2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yl) -2-phenylpropanoic acid (60 mg, 0.154 mmol) , the product of Step B (35.3 mg, 0.154 mmol) , HATU (70.6 mg, 0.18 mmol) and DIPEA (40 mg, 0.308 mmol) in DMF (3 mL) was stirred overnight. The reaction mixture was poured into H 2O (15 mL) and extracted with EtOAc (10 mL x 3) . The combined organic layers were washed with brine, dried over Na 2SO 4, concentrated and purified by prep-TLC (petroleum ether/EtOAc=1: 2) to give the target compound (34 mg, 36.8%) as a white solid. MS: M/e 601 (M+1) +., 192130-34-0

As the paragraph descriping shows that 192130-34-0 is playing an increasingly important role.

Reference£º
Patent; BEIGENE, LTD.; ZHANG, Guoliang; ZHOU, Changyou; (152 pag.)WO2019/196803; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics