Tag: M.W:100-200

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

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

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

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;,
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 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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7,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.

An oven-dried microwave vial (0.5-2.0 ml_ volume) was charged with (S)-2- cyclopropyl-10-((2,5-dichloropyrimidin-4-yl)amino)-3,3-difluoro-7-methyl-1 ,2,3,4-tetrahydro- [1 ,4]oxazepino[2,3-c]quinolin-6(7/-/)-one (Intermediate A10a; 7 mg, 0.015 mmol), 1- methylpiperazin-2-one (4 mg, 0.037 mmol) and DIPEA (13 uL, 0.075 mmol). The reaction vial was flushed with Ar and sealed with a cap. NMP (0.65 ml_) was added and the reaction mixture was heated at 140C under microwave irradiation for 1 h. The reaction mixture was dissolved in DMSO (0.8 ml_) and directly purified by reverse-phase chromatography (Biotage reverse-phase 12 g Ultra C-18 column; 10-60-80-100% MeOH in H2O (containing 0.1 % formic acid)). The product-containing fractions were combined, passed through an SCX-2 (1 g), additional MeOH (10 ml_) was passed through and the product was eluted with 2 N methanolic ammonia (25 ml_). The solvent was removed in vacuo affording the title compound (5 mg, 57%) as an off-white solid. 1 H NMR (600 MHz, methanol-d?) d 8.04 (d, J = 2.2 Hz, 1 H), 8.01 (s, 1 H), 7.92 (dd, J = 9.1 , 2.2 Hz, 1 H), 7.57 (d, J = 9.1 Hz, 1 H), 4.53- 4.38 (m, 2 H), 4.24 (d, J = 18.2 Hz, 1 H), 4.18 (d, J = 18.2 Hz, 1 H), 3.98-3.92 (m, 1 H), 3.92-3.87 (m, 1 H), 3.73 (s, 3 H), 3.47-3.39 (m, 2 H), 3.35-3.28 (m, 1 H), 2.98 (s, 3 H), 1.42-1.37 (m, 1 H), 0.82-0.75 (m, 1 H) 0.68-0.57 (m, 2 H), 0.37-0.31 (m, 1 H); LCMS (Method X4) RT 2.85 min; m/z calcd for C25H27CIF2N703+ [M+H]+: 546.1832, Found: 546.18342.

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

Reference：
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL; BELLENIE, Benjamin Richard; CHEUNG, Kwai Ming Jack; DAVIS, Owen Alexander; HOELDER, Swen; HUCKVALE, Rosemary; COLLIE, Gavin; MENICONI, Mirco; BRENNAN, Alfie; LLOYD, Matthew Garth; (222 pag.)WO2019/197842; (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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, b) 4-(5-Trifluoromethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl esterTo a solution of 17.5 mmol 2-benzenesulfonyl-3-trifluoromethyl-oxirane in 20 ml N,N-dimethylformamide was added 15.9 mmol 4-thiocarbamoyl-piperazine-l-carboxylic acid tert-butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, 1,1′- thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054). The mixture was heated at 90 0C for 10 h. The reaction mixture was then concentrated in vacuo and the residue purified by chromatography (SiO2, ethyl acetate/heptane) to afford the title compound as an orange crystalline solid (yield 26%). MS (m/e): 338.1 (M+H+, 100%).; a) 4-(5-Hydroxymethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl esterTo a solution of 179 mmol 30% aqueous hydrogen peroxide in 60 ml water was added 1 N aqueous sodium hydroxide solution until the pH was 9. The reaction mixture was then cooled to 100C and 163 mmol acrolein was added dropwise. Further amounts of 1 N aqueous sodium hydroxide solution were added during the addition in order to maintain the pH of the reaction mixture between pH 8 and 9. The mixture was stirred for 30 min at 0 0C and then 40.8 mmol thiocarbamoyl-piperazine-1-carboxylic acid tert- butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, 1,1′- thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) was added. To the resulting suspension was added 25 ml ethanol and the mixture was heated at 80 0C for 30 min. The resulting solution was diluted with ethyl acetate/tetrahydrofuran (1:1) and the mixture was washed twice with brine. The organic phase was dried over sodium sulphate and concentrated in vacuo to afford the title compound as a yellow oil (yield 99%). MS (m/e): 300.3 (M+H+, 100%).;f) 4-(4-Methyl-5-trifluoromethyl-thiazol-2-yl)-piperazine-l-carboxylic acid tert-butyl esterA mixture of 4.92 mmol rac-2-benzenesulfonyl-2-methyl-3-trifluoromethyl- oxirane and 5.41 mmol 4-thiocarbamoyl-piperazine-l-carboxylic acid tert-butyl ester (prepared from tert-butyl 1-piperazinecarboxylate, l.l’-thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) in 15 ml N,N-dimethylformamide was heated at 100 0C for 4.5 h. The reaction mixture was then concentrated in vacuo and the residue purified by chromatography (SiO2, ethyl acetate/heptane) to afford the title compound as a yellow crystalline solid (yield 30%). MS (m/e): 352.3 (M+H+, 100%).; a) 4-(Dimethylaminomethylene-thiocarbamoyl)-piperazine-l-carboxylic acid tert-butyl esterA mixture of 122 mmol N,N-dirnethylformamide dimethyl acetal and 6.11 mmol 4- thiocarbamoyl-piperazine-1-carboxylic acid tert-butyl ester (prepared from tert-butyl 1- piperazinecarboxylate, lj’-thiocarbonyldiimidazole and ammonia according to the procedure of J. Med. Chem. 1998, 41, 5037-5054) was heated at 110 0C for 3 h. The reaction mixture was then concentrated in vacuo and the residue was resuspended in ethyl acetate/ tetrahydrofuran ( 1:1) and washed with brine. The organic phase was dried over sodium sulphate and concentrated in vacuo to afford the title compound as a light yellow crystalline solid (yield 95%). MS (m/e): 301.4 (M+H+, 100%).

57260-71-6 tert-Butyl piperazine-1-carboxylate 143452, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2006/72436; (2006); 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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.,75336-86-6

i) tert-Butyl (3/?)-3-methylpiperazine-l-carboxylate;To a solution of (2No.)-2-methylpiperazine (Ig) in THF (10ml) was added di-tert-butyldicarbonate (1.45g). The reaction mixture was allowed to stir at room temperaturefor 18h.The reaction mixture was then partitioned between DCM (100 ml) and HaO (100 ml). Theorganics were separated and the aqueous layer was re-extracted with DCM (2 x 150ml).Organics were combined, dried (MgSO4) and reduced in vacuo to give the subtitle compoundas a clear oil. Yield: 1. Ig’H NMR: (DMSO) 8 0.92 (d, 3H), 1.38 (s, 9H), 2.57-2.70 (m, 1H), 2.76-2.81 (m, 1H), 2.87-2.99 (m, 1H), 3.66-3.74 (m, 4H)

The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/24823; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

25057-77-6, 1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 7 To a solution of N-benzyl-4-piperidone (8.0 g) and 3,4-dimethylpiperazine (9.5 g) in ethanol (100 ml) are added 5% platinum-carbon (2 g) and acetic acid (14.4 ml), and the mixture is subjected to catalytic hydrogenation at room temperature under atmospheric pressure. The catalyst is removed by filtration, and the filtrate is concentrated under reduced pressure. Water is added to the resultant, and the mixture is basified with a 5% aqueous sodium hydroxide solution, and the mixture is extracted with diethyl ether. The extract is washed with water, dried and concentrated under reduced pressure to remove the solvent. The residue is dissolved in ethanol, and thereto is added to conc. hydrochloric acid to give a hydrochloride. The resulting white powder is collected by filtration, dissolved in water, and basified with a 5% aqueous sodium hydroxide solution. The mixture is extracted with diethyl ether, washed with water, dried, and concentrated under reduced pressure to give 4-(3,4-dimethyl-1-piperazinyl)-1-benzylpiperidine (4.2 g). 1 H-NMR (CDCl3) deltappm: 1.04 (3H, d, J=6 Hz), 1.45-2.5 (12H, m), 2.27 (3H, s), 2.7-3.05 (4H, m), 3.48 (2H, s), 7.31 (5H, m).

25057-77-6, The synthetic route of 25057-77-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Otsuka Pharmaceutical Company, Limited; US6140330; (2000); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

109-01-3, 1-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

350 ml of ethanol was added to 155 g (1.547 mol) of N-methylpiperazine. At room temperature (25+/-3 C.), 60 g (0.351 mol) of 4-chloromethylbenzoic acid was added thereto and stirred for 6-7 hours. The reaction was analyzed by HPLC, and then the reaction solution was distilled under reduced pressure to remove ethanol, and 60 ml of 1-butanol was added thereto. The mixture was azeotropically distilled at 70+/-2 C. and concentrated to produce a solid. 600 ml of 2-propanol was added thereto and the mixture was stirred at room temperature (25+/-3 C.) for 30 minutes, stirred under reflux for 15 minutes, and then stirred at room temperature (25+/-3 C.) for 12 hours with slow cooling. The produced precipitate was cooled to 19+/-3 C., stirred for 1 hour and then filtered. The filtrate was washed with 50 ml of cooled 2-propanol and dried in an oven at 60 C., thereby obtaining a white compound of formula (2) (60 g, yield: 72%, purity: 95% or higher).HPLC purity: 99.123% (desmethyl impurity: 0.042%, starting material 0.42%).Thin layer chromatography: Methanol-Dichloromethane (7:5), Rf: 0.2., 109-01-3

109-01-3 1-Methylpiperazine 53167, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; BCWORLD PHARM. CO., LTD.; US2012/330014; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics