Heterocyclic Building Blocks-piperazine

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-Oxo-4-(2-thienyl) butyric acid (63 mg, 0.34 mmol), HOBt (58 mg, 0.43 mmol), TBTU (140 mg, 0.43 mmol), anhydrous triethylamine (0.1 ml, 0.69 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, 0.43 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 81 % yield. H NMR (300 MHz, CDCI3) ? 7.81 (d, 1 H), 7.63 (d, 1 H), 7.49 (d, 2H), 7.13-7.16 (m, 1 H), 6.92 (d, 2H), 3.72-3.81 (m, 4H), 3.28 (t, 4H), 3.25 (t, 2H), 2.81 (t, 2H). MS (+ESI) calcd for C19 H19 F3 N2 02 S m/z: [M + H]+ , 396.1 1 15; found 396.1 1 19 [Diff(ppm) = -1.1 1].

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

Reference：
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
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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 337 (31.8 mg, 0.0684 mmol) was added l-methylpiperazin-2-one (51.5 mg, 0.342 mmol) and Et3N (50 mu) in DMF (1 mL) and heated at 90 °C for 1 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH, 20: 1) to afford 31.8 mg (86percent) of 344. MS (ESI) m/z [M+H]+ 543.1.

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; CHIOSIS, Gabriela; KANG, Yanlong; PATEL, Hardik J.; PATEL, Maulik; OCHIANA, Stefan; RODINA, Anna; TALDONE, Tony; SHRESTHA, Liza; (288 pag.)WO2015/175707; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

100mL round-bottom flask was added 1.84g (10mmol) compound II, 1.26g (10mmol) and Compound III-2 dry 20mL of THF, the resulting mixture was stirred at ice-water bath, was added 2.48 g (12mmol) DCC, the stirring was continued at room temperature overnight. TLC showed the reaction was complete. document.write(“”); The reaction mixture was poured into ice water, stirred, and extracted with dichloromethane 50mL × 3, the combined organic extracts were washed with saturated brine, dried over anhydrous sodium sulfate, the solvent was distilled off on a rotary evaporator and the residue obtained was column chromatography to afford the product I-2, as a white solid.

20327-23-5, As the paragraph descriping shows that 20327-23-5 is playing an increasingly important role.

Reference：
Patent; Zhejiang Pharmaceutical College; Guo, Zhanghua; (6 pag.)CN104387341; (2016); B;,
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Piperazines – an overview | ScienceDirect Topics

57260-70-5, tert-Butyl 4-benzylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-70-5, The procedure described for the preparation of 2a was used with compound 10b (300 mg, 0.96 mmol), 13a (253 mg,1.44 mmol), K2CO3 (265 mg, 1.92 mmol) and CH3CN (15 mL) to obtain 2b (261 mg, 60%) as light brown liquid. Rf = 0.59 (n-hexane:EtOAc: MeOH = 2.5:1.5:1). 1H NMR (500 MHz, CDCl3): d 7.43-7.25(m, 15H), 5.90 (s, 1H), 4.65 (t, J = 7 Hz, 2H), 3.54 (s, 2H), 2.48-2.39(m, 10H), 2.20-2.15 (m, 2H); 13C NMR (125 MHz, CDCl3): d 167.7,140.8, 138.3, 129.2, 128.8, 128.7, 128.3, 127.11, 127.1, 63.1, 54.9,53.1, 51.4, 48.7, 26.7.

The synthetic route of 57260-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Paudel, Suresh; Acharya, Srijan; Yoon, Goo; Kim, Kyeong-Man; Cheon, Seung Hoon; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2266 – 2276;,
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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: Pd2(dba)3 (330 mg, 0.3 mmol), Xantphos (350 mg, 0.7 mmol) and KOtBu (1.6 g, 15 mmol) were addedinto a solution of compound 180-1 (2.0 g, 5.4 mmol) and (2S,6R)-2,6-dimethylpiperazine (0.8 g, 7 mmol) in toluene (30mL). Under nitrogen gas atmosphere, the reaction mixture was stirred at 120°C for 5h, then poured into H2O. The mixturewas extracted with ether (3330 mL), the organic phase was dried over sodium sulfate. The residue was purified bycolumn chromatography to deliver compoud 180-2 (1.7 g, yield 70percent) as yellow solid. MS ESI calcd for C29H28N4O [M+H]+ 449, found 449.

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; WU, Hao; LIN, Jun; LI, Yunhui; WEI, Changqing; CHEN, Shuhui; LONG, Chaofeng; CHEN, Xiaoxin; LIU, Zhuowei; CHEN, Lijuan; (212 pag.)EP3124482; (2017); A1;,
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Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step-1: To a stirred solution of methyl 2-oxo-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-6-carboxylate (0.18 g, 0.9366 mmol) in acetic anhydride (4 ml) was added triethyl orthobenzoate (0.630 g, 2.8098 mmol) at RT and the mixture was refluxed for 3 h at 110 C. The reaction mixture was evaporated and the resulting residue was used as such into next step without purification. [0212] Step-2: To a stirred solution of product from step-1 (0.18 g) in DMF (4 ml) was added N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (0.180 g, 0.6861 mmol) at RT and the reaction mixture was heated at 110 C. for 1 h. The reaction mixture was cooled to RT and stirred with triethyl amine (1 ml) for half an hour. The reaction mixture was evaporated and the crude product was purified by column chromatography using 0 to 10% methanol in dichloromethane as eluent to afford (Z)-methyl 1-acetyl-3-((4-(N-methyl-2-(4-methylpiperazin-1-yl) acetamido)phenylamino)(phenyl)methylene)-2-oxo-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-6-carboxylate as yellow solid. MS (ES+): m/z 583.4 (MH+)., 262368-30-9

The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ANGION BIOMEDICA CORP.; NARAYAN, Prakash; HUANG, Brian; PAKA, Prani; PAKA, Latha; GOLDBERG, Itzhak D.; US2015/105380; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

70261-82-4, To a mixture of 7- (3-BROMOPHENYL)-5-METHYL-M (3,4, 5- trimethoxyphenyl) imidazo [5, 1-f] [1,2, 4] TRIAZIN-2-AMINE (EXAMPLE 9) (40 mg, 0.085 MMOL), 4- [ (4-METHYLPIPERAZIN-1-YL) METHYL] ANILINE (20.9 mg, 0.102 MMOL), (S)- (-)-2, 2′-Bis (DIPHENYLPHOSPHINO), 1, 1 -BINAPHTHYL ((S)-BINAP) (15.9 mg, 0.026 MMOL), Tris (DIBENZYLIDINEACETONE) DIPALLADIUM (0) (7.8 mg, 0. 008 MMOL) and sodium t-butoxide (11.4 mg, 0.12 MMOL) was added1, 4-dioxane (1.5 ML). In a sealed reaction vessel, the mixture was heated with microwave radiation at 140 C for 60 minutes. After cooling to room temperature, diluted mixture with methanol (5 mL) and ethyl acetate (5 mL) followed by filtration over celite. Removed solvent under reduced pressure and diluted brown residue in DMSO (1.0 mL). Injected (2 x 0.5mL) on an Agilent reverse phase prep LC subjected to a gradient elution using ACETONITRILE (0. 1% Formic acid): water (0. 1% Formic acid) (10: 90 to 90: 10). The appropriate fractions were combined and concentrated under reduced pressure to give 5-methyl-7- [3-({4-[(4-methylpiperazin-1-yl)methyl]phenyl}amino)phenyl]-N- (3,4, 5- trimethoxyphenyl) imidazo [5, 1-4 [1,2, 4] TRIAZIN-2-AMINE (0.021 g) as a yellow SOLID. 1H NMR (CDCI3) : No. 8.78 (s, 1 H), 8.47 (s, 1 H), 8.09 (dd, J= 1.9, 1. 8 Hz, 1H), 8.0-7. 98 (m, 1H), 7.33 (dd, J= 7.9, 7.8 Hz, 1H), 7.19 (ddd, J= 7.9, 2.2, 0.8 Hz, 1H), 7.16-7. 14 (m, 2H), 7.11 (s, 1H), 7.07-7. 05 (m, 2H), 6.94 (m, 2H), 3.82 (s, 9H), 3.53 (s, 2H), 2.90-2. 54 (m, 14H). MS m/z 595 (M+1).

70261-82-4 4-(4-Methylpiperazin-1-ylmethyl)phenylamine 3153996, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2004/87652; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

39539-66-7, 4-Methylpiperazine-1-carbonyl chloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of this product (50 mg, 0.1 mmol), 4-methylpiperazine-1-carbonylchloride (89 mg, 0.6 mmol), diisopropylethylamine (142 mg, 1.1 mmol), in dioxane (0.5 mL) was submitted to microwave irradiation (300 W) for 60 minutes at 160 C. The reaction solution was cooled to room temperature and slowly poured into a stirring saline solution (10 mL). The resulting precipitate was collected by filtration, washed with water and purified by RP-HPLC (C18, 0 to 100% CH3CN in 0.1% aqueous HCO2H) to yield 1-280 as a pale yellow solid (6 mg, 10%) MS m/z=574 (M+H).

39539-66-7, The synthetic route of 39539-66-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Millennium Pharmaceuticals, Inc.; US2005/256102; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N4-(5-Isopropyl-1H-pyrazol-3-yl)-N6-[2-(4-methylpiperazin-1-yl)ethyl]-N2-(3-phenylisoxazol-5-ylmethyl)-pyrimidine-2,4,6-triamine. A mixture of 6-chloro-N4-(5-isopropyl-1H-pyrazol-3-yl)-N2-(3-phenylisoxazol-5-ylmethyl)-pyrimidine-2,4-diamine (250 mg, 0.611 mmol) and 2-(4-methylpiperazin-1-yl)-ethylamine (500 mg, 3.50 mmol) in 1-butanol (2 mL) was heated to 180° C. in a 50 mL sealed tube. The mixture was heated for 1 h, then cooled to room temperature and diluted with methanol (10 mL). The mixture thus obtained was purified via preparative reverse phase HPLC to give the desired product (93 mg, 29percent) as a white solid. 1H-NMR (400 MHz, d6-CDCl3): delta 7.8 (m, 2H), 7.4 (m, 3H), 6.5 (s, 1H), 5.9 (s, 1H), 5.2 (s, 1H), 4.8 (m, 2H), 3.5 (br s, 2H), 2.8 (m, 1H), 2.5 (m, 10H), 2.4 (s, 3H), 1.2 (m, 6H); MS (EI) for C27H36N10O: 517.3 (MH+)., 934-98-5

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; EXELIXIS, INC.; US2009/232828; (2009); A1;,
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

General procedure: N-Cbz piperazine (0.55 g, 2.48 mmol, 1 eq) and carboxylic acid 8c?g (2.48 mmol, 1 eq) were dissolved in dry DMF (10 mL), the reaction mixture flushed with argon and cooled to 0 °C. N-methyl morpholine (NMM; 7.44 mmol,3 eq), hydroxybenzotriazole hydrate (HOBt; 2.98 mmol,1.2 eq) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimidehydrochloride HCl salt (EDC; 3.22 mmol, 1.3 eq) were slowly added. The reaction mixture was stirred under argon atmosphere for 5 h at 0 °C and an additional 15 h at room temperature. DMF was evaporated under reduced pressure and the residue redissolved in dichloromethane (10 mL).The dichloromethane phase was washed with H2O (1 x 10 mL), a 1 M HCl solution (3 x 10 mL), saturated aqueous NaHCO3 solution (3 9 10 mL), brine (1 x 20 mL), dried over Na2SO4, filtered, and the solvent evaporated under reduced pressure. The crude product was purified by flash column chromatography using ethyl acetate/hexane solvents as eluents to afford compounds 9c?g., 31166-44-6

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

Reference：
Article; Juki?, Marko; Frlan, Rok; Chan, Fiona; Kirby, Robert W.; Madge, David J.; Tytgat, Jan; Peigneur, Steve; Anderluh, Marko; Kikelj, Danijel; Medicinal Chemistry Research; vol. 24; 6; (2015); p. 2366 – 2380;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics