Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

Example Al 4; a) Preparation of intermediate 38; A mixture of intermediate 11 (0.918 g; 3 mmol), EDCI (0.843 g; 4.4 mmol), HOBt (0.594 g; 4.4 mmol) and 10 ml of DMF was stirred at room temperature for 15 minutes. Benzenepropanoic acid hydrazide (1.045 g; 6.4 mmol) was added. The mixture was stirred at room temperature for 18 hours. The solvent was evaporated. The residue was stirred in water and extracted with CH2Cl2. The organic layer was dried, filtered and evaporated. The mixture was purified with HPLC method C. The pure fraction were collected and the solvent was evaporated. The residue was dried, yielding 0.941 g of intermediate 38.

162046-66-4, 162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148840; (2008); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

EXAMPLE 511 2-{[(2-{[3-(4-cyclopentyl-1-piperazinyl)propyl]amino}phenyl)sulfonyl]amino}-8-methyl-5,6,7,8-tetrahydro-1-naphthalenecarboxylic acid EXAMPLE 511A 3-(4-cyclopentyl-1-piperazinyl)-1-propanamine [0873] A mixture of N-(3-bromopropyl)phthalimide (0.8 g, 3.0 mmol), 1-cyclopentylpiperazine (0.46 g, 3.0 mmol), and K2CO3 (1.66 g, 12.0 mmol) in CH3CN (30 mL) was heated to reflux for 3 hours, cooled to room temperature, and filtered through diatomaceous earth (Celite). The filtrate was concentrated, treated with 6N HCl (9.0 mL) and acetic acid (18.0 mL), heated to reflux overnight, and concentrated. The residue was treated with potassium carbonate (1.66 g) in CH3CN (30 mL) for 1 hour. After filtration of the solid, the solvent was evaporated to provide the desired product. MS (DCI/NH3) m/e 212 (M+H)+; 1H NMR (300 MHz, DMSO-d6) delta 8.04 (br s, 2H), 3.68 (m, 4H), 3.41 (m, 4H), 3.21 (m, 2H), 2.91 (m, 2H), 2.0 (m, 4H), 1.84-1.73 (m, 4H), 1.55 (m, 2H)., 21043-40-3

As the paragraph descriping shows that 21043-40-3 is playing an increasingly important role.

Reference£º
Patent; Comess, Kenneth M.; Erickson, Scott A.; Henkin, Jack; Kalvin, Douglas M.; Kawai, Megumi; Kim, Ki H.; BaMaung, Nwe Y.; Park, Chang Hoon; Sheppard, George S.; Vasudevan, Anil; Wang, Jieyi; Barnes, David M.; Fidanze, Steve D.; Kolaczkowski, Lawrence; Mantei, Robert A.; Park, David C.; Sanders, William J.; Tedrow, Jason S.; Wang, Gary T.; US2004/167128; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

694499-26-8, General procedure: To a solution of 8a-e (20 mmol) and triethylamine (40 mmol) indichloromethane (20 ml), a solution of 4a-f (1.5 eq) in dichloromethane(10 ml) was added dropwise at room temperature over20 min and stirred overnight. The mixture was washed with saturatedaqueous sodium bicarbonate and brine. After removing thesolvent under reduced pressure, the crude product was purifiedby flash chromatography on silica gel, eluting with dichloromethaneand methanol (10-30%), yielding the title compounds.

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
Article; Yao, Dahong; Wang, Jing; Wang, Guan; Jiang, Yingnan; Shang, Lei; Zhao, Yuqian; Huang, Jian; Yang, Shilin; Wang, Jinhui; Yu, Yamei; Bioorganic Chemistry; vol. 68; (2016); p. 112 – 123;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

182618-86-6, 1-Boc-4-(4-Nitrophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 17b 4-(4-Amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester 4-(4-Amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester was prepared from 4-(4-Nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester, (as prepared in Reference Example 17a) as prepared in Reference Example 13b., 182618-86-6

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Pierson, Edward; Sohn, Daniel; Haeberlein, Markus; Davenport, Timothy; Chapdelaine, Marc; Horchler, Carey; McCauley, John P.; US2003/13708; (2003); A1;,
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59702-31-7, 1-Ethylpiperazine-2,3-dione is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a four-necked flask was added 4-ethyl-2,3-dioxopiperazine (14.2 g, 0.1 mol)Dichloromethane (60 ml) and trimethylchlorosilane (13.0 g, 0.12 mol) were added. The temperature was controlled to -10 to -20 C. and triethylamine (25.5 g, 0.25 mol) was added dropwise to -5 to 0, Stirring for 12min;Ethyl-2,3-dioxopiperazine chloride (22.4 g, 0.11 mol) was dissolved in 20 ml of methylene chloride,The temperature was controlled at 0 C ~ -5 C for 40min, warmed to 25 C and incubated for 8h. After the reaction was completed, the temperature was lowered to -15 C, filtered and the filter cake was rinsed with precooled dichloromethane (8ml). The mother liquor was combined and concentrated (30 ~ 40 , the degree of vacuum is <0.1MPa) to obtain crude product 0.4g (yield 98.6%, purity 95%)., 59702-31-7

As the paragraph descriping shows that 59702-31-7 is playing an increasingly important role.

Reference£º
Patent; Jiangxi Fuxiang Pharmaceutical Co., Ltd.; Zheng Yuyi; Wu Xiaofeng; Zhou Zhongbo; Xie Yongju; Wang Dongdong; (8 pag.)CN104529914; (2017); B;,
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Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step D: (3R,9aS}-3-(3-Cyano-4-fluoro-2-methyl-phenyl)-3-hydroxy-hexahydro-pyrazino[2,1-c][1,4]oxazine-8-carboxylic acid tert-butyl ester: Diisopropylethylarnine (44.0 mL, 252 mmol)was added to a stirred, room temperature mixture of72 wt% 3-(2-Bromo-acetyl)-6-fluoro-2-methyl-benzonitrile (69 g, 194 mmol) and (S)-4-N-Boc-2-hydroxymethyl-piperazine ( 42.0 g, 194 mmol) in THF (1000 mL) and the mixture was stirred at room temperature for 18h. The reactionwas diluted with 1 L EtOAc, washed 2x with 500 mL 10% w/wNaHC03 aqueous solution,dried over MgS04, filtered and concentrated. The residue was purified by column chromatographyon silica gel ( 40-80% EtOAc/Hexanes, linear gradient), to give the title compound.?~+%, 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); A1;,
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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

4-(1 H-Pyrazol-4-yl)butanoic acid (100 mg, 0.65 mmol), HOBt (96 mg, 0.71 mmol), TBTU (228 mg, 0.71 mmol), anhydrous triethylamine (144 ??, 1.04 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (100 mg, 0.71 mmol) and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 10% yield. H NMR (300 MHz, CDCI3) ? 7.49 (d, 4H), 6.91 (d, 2H), 3.77 (t, 2H), 3.58 (t, 2H), 3.24 (t, 4H), 2.57 (t, 2H), 2.37 (t, 2H), 1.91-2.01 (m, 2H). MS (+ESI) calcd for C18 H21 F3 N4 O m/z: [M + H]+ , 366.1677; found 368.177 [Diff(ppm) = 1 .55]., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1.Synthesis of 4-Ethyl-1-(4-nitrophenyl)piperazine To 4-fluoro-1-nitrobenzene(1 eq) in N,N-dimethylformamide was added Ethyl piperazine (2 eq) and N,N-diisopropylethyl amine (2 eq) and heated at 80 C. for 16 h.Concentrated the resultant mixture and partitioned between ethyl acetate and water.The organic layer was then washed with brine and dried with sodium sulfate and concentrated.Passed through a plug of silica to yield 4-Ethyl-1-(4-nitrophenyl)piperazine. MS: MH+=235., 5308-25-8

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Amiri, Payman; Fantl, Wendy; Levine, Barry Haskell; Poon, Daniel J.; Ramurthy, Savithri; Renhowe, Paul A.; Subramanian, Sharadha; Sung, Leonard; US2004/122237; (2004); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step I: tert-butyl (2S)-4-(4-bromophenyl)-2-methyl-piperazine-1-carboxylate (1-35) A mixture of 1-34 (10 g, 50 mmol), 1,4-dibromobenzene (29.4 g, 125 mmol), cesium carbonate (24.3 g, 75 mmol) and BINAP (1.5 g, 2.5 mmol) in 1,4-dioxane (250 mL) was degassed in a stream of argon for 15 minutes. To the mixture was added tris(dibenzylideneacetone)dipalladium(0) (0.900 g, 2.5 mmol), and the reaction mixture was again degassed for additional 15 minutes. After stirring at 90 C. for 18 hours, the volatiles were removed by evaporation, and the obtained residue was diluted with water (250 mL), followed by extraction with ethyl acetate (250 mL*3). The combined organic layers were washed with brine (50 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (60-120 mesh) using 10% EtOAc in hexanes to give the desired product 1-35 as a white solid (5.5 g, 31%); LCMS: m/z 357.1 [M++1], 359.1 [M++2].

169447-70-5, The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; BHOSALE, Sandeep; NAIK, Keshav; SALUNKHE, Videsh; MUNOT, Yogesh; BHUNIYA, Debnath; (132 pag.)US2017/8885; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

325145-35-5, (S)-tert-Butyl 2-ethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

325145-35-5, Example 2J kJlBOCA 250 ml round bottom flask was charged with A2 (4g, 15.9 mmol), 1-Boc-2-S-ethyl piperazine A3 (prepared as per Kiley et al Org. Prep. Proc. Int. 1990, 22, 761; 4.2 g, 18.6 mmol), tris(dibenzylideneacetone)dipalladium , (340 mg, 0.37 mmol), racemic-2,2′-bis(diphenylphosphino)-1 ,1′-binaphthyl (BINAP) (495 mg, 0.74 mmol), cesium carbonate (12g, 37.2 mmol) and toluene (80 ml). After the mixture was heated at 1003C for 16 h, fresh tris(dibenzylidene- acetone)dipalladium (340 mg, 0.37 mmol) and BINAP (495 mg, 0.74 mmol) were added and the heating was continued for 3 days. The solvent was removed in vacuo, and the residue was suspended in a 100 ml portion of ethyl acetate. This mixture was extracted with water and brine, dried over sodium sulfate, and concentrated in vacuo. Purification of the residue via silica gel flash chromatography (5percentmethanol/ 95percent DCM) yielded 5.3 g of a partially purified material which was used directly in the next step. M+H = 350

The synthetic route of 325145-35-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SCHERING CORPORATION; PHARMACOPEIA, INC.; WO2008/8453; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics