Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

630125-91-6, A suspension of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (247 mg, 0.858 mmol) in DCM (35 mL) was added to a solution of 2-(4-bromo-2-fluorophenyl)acetic acid (200 mg, 0.858 mmol) in DCM (35 mL). HOBt (197 mg, 1.287 mmol), EDC (247 mg, 1.287 mmol) and Et3N (0.359 mL, 2.57 mmol) was added and the mixture was stirred at 26 C. for 3 h. Then the solution was concentrated and distributed between EA and saturated NaHCO3 solution. The combined organic extract was washed with brine, dried over MgSO4, filtered and concentrated. The crude material was purified by silica column chromatography (PE/EA=10/1). All fractions found to contain product by TLC (PE/EA=5/1, Rf=0.6) were combined and concentrated to yield a light yellow solid of 2-(4-bromo-2-fluorophenyl)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)acetamide (413 mg, 0.822 mmol, 96.0% yield): 1H NMR (400 MHz, CD3OD) delta 7.98-7.91 (m, 1H), 7.79-7.67 (m, 2H), 7.40-7.27 (m, 3H), 3.74 (s, 2H), 3.61 (s, 2H), 2.58-2.39 (m, 11H), 1.09 (s, 4H); ES-LCMS m/z 502.0 (M+H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GlaxoSmithKline Intellectual Property Development Limited; EIDAM, Hilary Schenck; Raha, Kaushik; Gong, Zhen; Guan, Huiping; Wu, Chengde; Yang, Haiying; Yu, Haiyu; Zhang, Zhiliu; CHEUNG, Mui; US2014/275111; (2014); 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

(1) 1-Benzyloxycarbonylpiperazine (19.0 g) was dissolved in pyridine (150 mL) and acetic anhydride (9.0 mL) was added at room temperature. The mixture was stirred for 18 hr. The reaction solution was concentrated under reduced pressure, and a 10percent aqueous citric acid solution was added to the residue. The mixture was extracted with ethyl acetate. The extract solution was washed with saturated brine, dried and concentrated under reduced pressure to give 4-acetyl-1-benzyloxycarbonylpiperazine (22.6 g) as an oil.(2) The above-mentioned compound (7.12 g) was dissolved in tetrahydrofuran (150 mL), and a 1 mol/L lithium bis(trimethylsilyl)amide-tetrahydrofuran solution (41 mL) was added dropwise at -78¡ãC over 40 min. After stirring at said temperature for 1 hr, a solution of ethyl trifluoroacetate (4.85 mL) in tetrahydrofuran (20 mL) was added to the reaction solution. The mixture was gradually warmed to room temperature and stirred for 18 hr. A saturated aqueous ammonium chloride solution was added to the reaction solution, and the mixture was extracted with ethyl acetate. The extract solution was washed with saturated brine, dried and concentrated under reduced pressure. The residue was purified by silica gel chromatography to give 1-benzyloxycarbonyl-4-trifluoroacetoacetylpiperazine (7.35 g) as a pale-yellow solid.(3) In the same manner as in Example 36(1) and using the above-mentioned compound (1.96 g) and phenylhydrazine (0.540 mL), 1-benzyloxycarbonyl-4-(3-trifluoromethyl-1-phenyl-5-pyrazolyl)piperazine (0.416 g) was obtained as an oil.(4) In the same manner as in Example 33(3) and using the above-mentioned compound (416 mg), 1-(3-trifluoromethyl-1-phenyl-5-pyrazolyl)piperazine (286 mg) was obtained as a white solid.(5) In the same manner as in Example 29(1) and using the above-mentioned compound (286 mg) and the title compound (280 mg) of Reference Example 3, 3-{(2S,4S)-1-tert-butoxycarbonyl-4-[4-(3-trifluoromethyl-1-phenyl-5-pyrazolyl)-1-piperazinyl]-2-pyrrolizinylcarbonyl}-1,3-thiazolidine (322 mg) was obtained as a pale-brown powder.(6) In the same manner as in Example 33(5) and using the above-mentioned compound (322 mg), the title compound (294 mg) was obtained as a white solid.1H-NMR(DMSO-d6)delta 2.00-2.28(1H,m), 2.80-4.00(16H,m), 4.44-4.74(3H,m), 6.64(1H,s), 7.44-7.49(1H,m), 7.54-7.59(2H,m), 7.77-7.79(2H,m), 9.03(1H,brs), 10.55(1H,brs).

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mitsubishi Pharma Corporation; EP1426366; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-(2-(cyclopropanecarboxamido)thiazolo[5,4-b]pyridin-5-yl) benzoic acid (150 mg, 0.44 mmol) and triethylamine (90 muL, 0.66 mmol) in toluene (2 niL) was added diphenylphosphoryl azide (0.11 niL, 0.49 mmol). The resulting mixture was stirred at room temperature for 30 minutes and heated at 80 0C for 1 h. To a reaction mixture was added 4-((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl) aniline (121 mg, 0.42 mmol) and triethylamine (90 muL, 0.66 mmol). The reaction mixture was stirred at 80 0C for 2h and most of organic solvent was removed in vacuo. The crude product was diluted with DMSO (3 mL) and purified by preparative HPLC to give the title compound as a TFA salt.1H NMR 600 MHz (CDCl3) delta 8.51 (s, IH), 7.83 (d, J= 1.8 Hz, IH), 7.48 (m, 2H), 7.19 (m, 3H), 7.12 (m, 2H), 6.85 (J, J= 3.0 Hz, IH), 6.49 (m, IH), 6.19 (m, 2H), 3.84 (m, IH), 3.78 (s, 3H), 3.46 (m, 2H), 3.19 (m, IH), 2.90 (m, 2H), 1.99 (m, 2H), 1.69 (m, 2H), 1.19 (J, J= 6.6 Hz, 6H), MS m/z : 624.36 (M + 1).

630125-91-6, 630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; CHOI, Hwan, Geun; SIM, Taebo; GRAY, Nathanael; ZHOU, Wenjun; CHANG, Jae, Won; ZHANG, Jianming; WEISBERG, Ellen; WO2010/144909; (2010); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

31166-44-6, A mixture of benzyl piperazine-1-carboxylate (Aldrich, 3.19 g, 14.5 mmol), 1-(5-fluoro-2-nitrobenzylsulfonyl)naphthalene (5.00 g, 14.5 mmol), and K2CO3 (4.00 g, 29.0 mmol) in DMF (32 mL) was stirred at 100¡ã C. for 3 hours, cooled to room temperature, diluted with water, and extracted with EtOAc. The organic layer was washed with water (3*), dried over Na2SO4, and concentrated in vacuo to provide the title compound (7.82 g, 94percent), characterized by NMR and mass spectral analyses. MS (ES+) m/e 546 (MH+).

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; Wyeth; US2009/318470; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

77279-24-4, tert-Butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,77279-24-4

Take piperazine ethanol 3.0g in 100ml round bottom flask, another 5.5g di-tert-butyl dicarbonate dissolved in 15ml of tetrahydroFuran, the solution was slowly added dropwise to the round-bottomed flask, stirred at room temperature for 4 hours until TLC detected nicotineethanol consumed. Most of the solvent is removed by rotary evaporation and the residue is diluted with water and extracted three times with dichloromethane (50 ml each). The organic phases were combined and dried over anhydrous sodium sulfate to give an oily liquid.This oily liquid was dissolved in 300 ml of methylene chloride and 3.34 ml of thionyl chloride was added slowly at room temperature and the mixture was stirred overnight at room temperature.The reaction mixture was diluted with water and adjusted to pH neutral with a solid of sodium bicarbonate. The organic phase was separated, dried over anhydrous sodium sulfate and dried to give 3.16 g of intermediate A22. Two-step yield of 55%.

As the paragraph descriping shows that 77279-24-4 is playing an increasingly important role.

Reference£º
Patent; Tsinghua University; Rao Yu; Wu Wei; Lan Tianlong; Hu Jiantao; Fan Zhongyun; Huang Binlu; (31 pag.)CN107286098; (2017); A;,
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.

Intermediate 28 : (2,2-Dimethyl-piperazin- lyl)-[ 1 -(3-fluoro-phenyl)- 1Eta-[ 1 ,2,4]triazol-3yl]- methanone A mixture of 460 mg (2.22 mmol) l-(3-fluoro-phenyl)-lH-[l,2,4]triazole-3-carboxylic acid and 330 (2.49 mmol) l-chloro-N,N,2-trimethylpropylamine in 10 mL THF was stirred at RT for 30 min, 500 mg (2.22 mmol) 3,3-dimethyl-piperazine-l-carboxylic acid tert-butyl ester and 620 (4.45 mmol) TEA were added and the mixture was stirred at RT for 1 h. The solvent was removed by distillation and the residue was purified by HPLC. yield: 205 mg (30 %) ESI-MS: m/z = 304 (M+H)+ Rt(HPLC) : 1.24 min (method 3), 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; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HEIMANN, Annekatrin; DAHMANN, Georg; GRUNDL, Marc; MUELLER, Stephan Georg; WELLENZOHN, Bernd; WO2013/87805; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122323-88-0, Methyl piperazine-2-carboxylate dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1 -chloroisoquinoline, intermediate compound I0 (905 mg) was dissolved in CH3CN (72 ml). Potassium carbonate (796 mg) was added followed by piperazine-2-carboxylic acid methyl ester di-hydrochloride (1 .8 g). The mixture was stirred at 100C for 7 days. DCM was added and the mixture washed with water. The organic phase was separated, dried and evaporated by vacuum. The crude material was purified by Si-column eluting with cHex/Ethyl acetate 3:7 to ethyl acetate/MeOH 9:1 to obtain 570 mg of the methyl 4-(isoquinolin-1 -yl)piperazine-2-carboxylate, intermediate compound 11 (Y=38%). LC-MS (M-H+) = 272.2., 122323-88-0

As the paragraph descriping shows that 122323-88-0 is playing an increasingly important role.

Reference£º
Patent; AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.; OMBRATO, Rosella; GAROFALO, Barbara; MANGANO, Giorgina; CAPEZZONE DE JOANNON, Alessandra; CORSO, Gaia; CAVARISCHIA, Claudia; FURLOTTI, Guido; IACOANGELI, Tommaso; (161 pag.)WO2016/96686; (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.1030377-21-9,(S)-1-Boc-2-(Hydroxymethyl)piperazine,as a common compound, the synthetic route is as follows.

To a solution of (S)-l-Boc-2-hydroxymethylpiperazine (1.0 g, 4.62 mmol) in DCE (92.47 ml, 4.624 mmol) was added formaldehyde (3.474 ml, 46.24 mmol) (37% in water) followed by sodium triacetoxyborohydride (4.9 g, 23.12 mmol). The mixture was stirred vigorously at room temperature for 2.5hours. The mixture was treated with saturated sodium bicarbonate (30 mL), stirred for 10 min then extracted with DCM (3 x 10 mL). The combined organic phases were dried over sodium sulfate, filtered and concentrated. ES+APC1 MS m/z 231.1 [M+H]+., 1030377-21-9

As the paragraph descriping shows that 1030377-21-9 is playing an increasingly important role.

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; MARX, Matthew, Arnold; BLAKE, James, F.; FELL, Jay, Bradford; FISCHER, John, P.; MEJIA, Macedonio, J.; (164 pag.)WO2020/47192; (2020); 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

A mixture of 4,5-dichloro-1-ethyl-1H-indole-2-carboxylic acid (440 mg, 1.71 mmol), CH2Cl2 (10 mL), and a catalytic amount of DMF was stirred under Ar, and oxalyl chloride (2M in methylene chloride, 2.0 mL, 4.0 mmol) was added into the mixture over 5 min. The mixture was stirred at room temperature for 1.0 hr and the reaction was concentrated to dryness. Benzene was added and the solution was evaporated to dryness again. The white-yellow solid was re-dissolved in 5 mL of methylene chloride and dripped, under Ar, into a solution of 4-(4-amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (475 mg, 1.71 mmol), and triethylamine (204 mg, 2.0 mmol) in 5 mL of methylene chloride. The mixture was first stirred at room temperature for 0.5 hr then concentrated and the residue was taken up in 50 mL of ethyl acetate and washed with 50 mL of saturated ammonium chloride, brine and dried with anhydrous sodium sulfate. The solvent was removed and the crude product was purified by flash chromatography (hexanes/EtOAc), to afford the desired 4-{4-[(4,5-dichloro-1-ethyl-1H-indole-2-carbonyl)-amino]-phenyl}-piperazine-1-carboxylic acid tert-butyl ester, as an off white solid (750 mg, 85% yield). LCMS for C26H30Cl2N4O3 calcd. (m/e) 516, observed 517 (M+H).

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

Reference£º
Patent; Bolin, David Robert; Hayden, Stuart; Qian, Yimin; Yun, Weiya; US2010/145047; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

76003-29-7, 1-Boc-3-Oxopiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of /er/-butyl 3-oxopiperazine-l-carboxylate (cas: 76003-29-7, 2 g, 10 mmol) in DMF (20 mL) that had been pre-cooled in an ice-water bath was added NaH (800 mg, 2.0 equiv.) in portions under N2. The mixture was stirred for 0.5 hours. (2- bromoethoxy)(ter/-butyl)dimethylsilane (cas: 86864-60-0, 5.3 mL, 2.5 equiv.) was added to the solution at 0 C. The reaction mixture was stirred at 25 C for 12 hours. The reaction mixture was then diluted with water (50 mL) and extracted with EtOAc (3 x 80 mL). The combined organic extracts was then washed with water (50 mL), brine (50 mL), and dried over Na2S04, then concentrated under reduced pressure to a residue. The residue was purified by silica gel chromatography to afford ketopiperazine 1-321 as a pale oil (1.8 g, 50% yield, pale oil). MS (ESI, pos. ion) m/z: 381 (M+23, 76003-29-7

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference£º
Patent; CARMOT THERAPEUTICS, INC.; ENQUIST, Johan; KRISHNAN, Shyam; ATWAL, Suman; ERLANSON, Daniel; FUCINI, Raymond V.; HANSEN, Stig; SAWAYAMA, Andrew; SETHOFER, Steven; (719 pag.)WO2019/183577; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics