Month: April 2021

216144-45-5, 4-(4-Methylpiperazin-1-yl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The solution of compound 5 (150 mg, 0.58 mmol), 4-(4-Methylpiperazino)benzylamine (118 mg, 0.58 mmol) and DIPEA (0.15 ml, 0.86 mmol) DMSO (3.5 mL) was stirred at 105 C. for 2 hours. TLC was checked and the starting material was consumed. The reaction mixture was added to half-saturated ammonium chloride in water (80 mL) and stirred for 30 min, then cooled with ice bath. The solids were collected by filtration, washed by water. The crude product was purified by column chromatography (0-10% MeOH in DCM) to give the product compound 29 as yellow solids. (98 mg, 39% yield). 1H NMR (400 MHz, DMSO-d6) delta 12.10 (br, 1H), 10.67 (s, 1H), 8.34 (s, 1H), 8.28 (s, 1H), 7.20 (d, J=8.8 Hz, 2H), 6.90 (d, J=8.8 Hz, 2H), 5.69 (s, 1H), 4.67 (d, J=5.6 Hz, 2H), 3.10 (m, 4H), 2.43 (m, 4H), 2.21 (s, 3H), 1.98 (m, 1H), 0.98 (m, 2H), 0.79 (m, 2H); ESI-MS: calcd for (C23H27N9) 429, found 452 (MNa+).

216144-45-5, 216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NantBio, Inc.; Tao, Chunlin; Wang, Qinwei; Asad, Sharif; Weingarten, Paul; Ci, Sherry; US2018/346450; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

13754-38-6, General procedure: To a mixture of 1-benzoylpiperazine (1.0 eq) and potassium carbonate (2.0 eq) in dimethylformamide was added dropwise a solution of the corresponding substituted 9-bromo-9H-fluorene (1.0 eq) in dimethylformamide (The synthesis of 9-bromo-9H-fluorene derivatives is reported in supporting information). After stirring for 24 h at room temperature, solvent was removed and the crude residue was dissolved in diethyl ether, washed with brine, dried over magnesium sulfate,filtered and concentrated under vacuum. The residue was purified by flash chromatography as indicated in each case to afford the title compound. Reagents: 1-Benzoylpiperazine (0.08 mmol, 15 mg), potassium carbonate (0.15 mmol, 20 mg) and 9-bromo-3-hexyl-9H-fluorene (0.08 mmol, 25 mg). The crude product was purified by flash chromatography (isocratic, petroleum ether/ethyl acetate 70/30 in 15 min) to afford a yellow oil (18 mg, 56%). TLC Rf: 0.11 (petroleum ether/ethyl acetate 80/20). IR (cm-1): 630, 674, 697, 708, 739, 768, 787, 1001, 1015, 1142, 1155, 1255, 1277, 1301, 1424, 1447, 1633, 2854, 2925. HPLC: method 2, rt = 2.56 min, purity 97%. 1H NMR (300 MHz, CDCl3) delta (ppm): 0.85-1.00 (m, 3H); 1.29-1.48 (m, 6H); 1.62-1.77 (m, 2H); 2.46 (s, 2H); 2.72 (t, J = 7.5 Hz, 2H); 2.86 (s, 2H); 3.38 (s, 2H); 3.82 (s, 2H); 4.87 (s, 1H); 7.15 (dd, J = 1.5 Hz, 7.5 Hz, 1H); 7.32 (td, J = 1.5 Hz, 7.5 Hz, 1H); 7.35-7.48 (m, 6H); 7.53 (s, 1H); 7.55 (d, J = 5.4 Hz, 1H), 7.64 (d, J = 7.5 Hz, 1H); 7.70 (d, J = 7.5 Hz, 1H). 13C NMR (75 MHz, CDCl3) delta (ppm): 14.1 (CH3); 22.6 (CH2); 29.1 (CH2); 31.7 (CH2); 31.8 (CH2); 36.1 (CH2); 43.0 (CH2); 48.4 (CH2); 48.8 (CH2); 49.5 (CH2); 69.7 (CH); 119.7 (CH); 119.8 (CH); 125.6 (CH); 125.9 (CH); 127.0 (CH); 127.1 (2 * CH); 127.5 (CH); 128.2 (CH); 128.4 (2 * CH); 129.6 (CH); 135.9 (C); 140.7 (C); 141.1 (C); 141.2 (C); 143.3 (C); 143.8 (C); 170.3 (C). MS (DCI/CH4) m/z: 438.26 [M+H+], 249.16 [M-188]. HRMS (DCI/CH4): for C30H34N2O [M+H+]: calcd: 438.2671; found: 438.2674.

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference£º
Article; Chollet, Aurelien; Mori, Giorgia; Menendez, Christophe; Rodriguez, Frederic; Fabing, Isabelle; Pasca, Maria Rosalia; Madacki, Jan; Kordulakova, Jana; Constant, Patricia; Quemard, Annaik; Bernardes-Genisson, Vania; Lherbet, Christian; Baltas, Michel; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 218 – 235;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6,75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(R)-2-methylpiperazine (5.025 g, 50.2 mmol) was dissolved in DCM (100 mL). A solution of boc anhydride (5.47 g, 25.1 mmol) in DCM (50 mL) was added dropwise at 0 C. The reaction mixture was stirred at rt for 1 h. The solution was filtered and concentrated under reduced pressure. Water (100 mL) was added to the residue, which was filtered again. The filtrate was saturated with K2CO3 and extracted with Et2O (3¡Á150 mL). The combined organic layers were dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to provide 5.04 g title compound (50%) as a solid. 1H NMR (300 MHz, CDCl3) delta ppm 1.03 (d, J=6.3 Hz, 3H) 1.45 (s, 9H) 1.56 (s, 1H) 2.30-2.46 (m, 1H) 2.65-2.72 (m, 1H) 2.74-2.76 (m, 2H) 2.93-2.95 (m, 1H) 3.93 (br s, 2H).

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

Reference£º
Patent; ASTRAZENECA AB; US2010/216812; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.74879-18-8,(S)-(+)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

In a sealed tube, 7-fluoro-9-methyl-2-(2-methylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one (Intermediate 3; 250 mg, 0.808 mmol), and (S)-2-methylpiperazine (405 mg, 4.04 mmol, 5.0 eq.) were stirred in DMSO (6 mL) and heated at 130 C. overnight. The solvent was removed under high vacuum. The residue was taken up in CH2Cl2 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2SO4 and concentrated in vacuo. The crude was purified by column chromatography (SiO2, CH2Cl2/MeOH=95/5 to 85/15) to afford the title product (135 mg, 43%) as a light yellow solid. MS m/z 390.3 [M+H+].

74879-18-8 (S)-(+)-2-Methylpiperazine 2734219, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Hoffmann-La Roche Inc.; PTC Therapeutics, Inc.; Ratni, Hasane; Green, Luke; Weetall, Maria L.; Naryshkin, Nikolai A.; (33 pag.)US2019/315773; (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.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.,5308-25-8

a) Ethyl 2-(4-ethylpiperazin-l-yl)acetateTo a solution of 1 -ethylpiperazine (1 g, 8.771 mmol, 1.0 eq) in DMF were added K2C03 (3 g, 21.927 mmol, 2.5 eq.) and ethyl 2-bromoacetate (2.19 g, 13.156 mmol, 1.5 eq.). The mixture was stirred at RT for 16 h. The mixture was quenched and extracted as in Intermediate Example 5(a). The solvent was distilled off to afford the product in 76.4 % yield (1.3g).

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference£º
Patent; ORION CORPORATION; LINNANEN, Tero; WOHLFAHRT, Gerd; NANDURI, Srinivas; UJJINAMATADA, Ravi; RAJAGOPALAN, Srinivasan; MUKHERJEE, Subhendu; WO2013/53983; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-Methanesulfonyl-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 10 mmol of Piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester were dissolved in 20 ml methylenchloride. 1.05 eq of DIPEA and mesylchloride were added. The reaction mixture was stirred at room temperature for 30 min. The product was extracted from etylacetate/water. The crude material was redissolved in methanol and treated with 2N NaOH. The reaction mixture was stirred at room temperature for 2 h. The mixture was neutralized with HCl and the product isolated via extraction from ethylacetate/water. MS(ISO): 307.4 (M-H+), 129799-15-1

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference£º
Patent; Ackermann, Jean; Bleicher, Konrad; Ceccarelli Grenz, Simona M.; Chomienne, Odile; Mattei, Patrizio; Schulz-Gasch, Tanja; US2007/129544; (2007); 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, Cyclopropanoyl chloride (112 muL) was added to a mixture of N-tert-butoxycarbonylpiperazine (200 mg) and an excess of potassium carbonate in anhydrous DCM (10 mL) under a nitrogen atmosphere. The mixture was stirred at r.t. for 18 hours, then it was filtered off from inorganics. The organic phase was diluted with Et2O (20 mL) and washed with 1N hydrochloric acid solution (10 mL). The aqueous phase was made basic with 1N sodium hydroxide solution and extracted twice with DCM. The combined organic layers were dried and concentrated in vacuo to give the title compound (210 mg) as an oil. [0238] T.I.c.: AcOEt, Rf=0.45. [0239] NMR (d6-DMSO): 6 (ppm) 3.64-3.28 (m, 8H); 1.94 (m, 1H); 1.4 (s, 9H); 0.7 (m, 4H). [0240] MS (ES/+): m/z=255 [M+H]+.

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

Reference£º
Patent; Alvaro, Giuseppe; Di Fabio, Romano; Maragni, Paolo; Tampieri, Marsia; Tranquillini, Maria Elvira; US2004/14770; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

55121-99-8, (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,55121-99-8

KOtBu (2.81 g, 25.08 mmol) was dissolved in 20 ml DMSO in a round bottom flask. (4-aminophenyl)(4-methylpiperazin-1-yl)methanone (5.0 g, 22.80 mmol) in 30 ml DMSO was added and the resulting mixture was stirred for 15 minutes at r.t. The mixture was cooled in an iced bath for 5 minutes. 5-bromo-2- fluorobenzonitrile (4.6 g, 23.00 mmol) in 20 ml DMSO was added. The ice bath was removed and the mixture stirred for 5 hours while warming to room temperature. Additional KOtBu (2g, 17.82 mmol) was added and the mixture stirred at room temperature overnight. The mixture was diluted with dichloromethane, extracted twice with water, once with brine, then dried over MgSO4, filtered and concentrated. 8.8 g crude brown oil were isolated. The crude product was recrystallized from dichloromethane + ethyl acetate + hexanes. 5.012 g pale yellow crystals were collected by filtration. The mother liquor was concentrated and purified by chromatography on silica, using a gradient from 100% Solvent A to 50% Solvent A+50% Solvent B. Solvent A: 99% dichloromethane + 1% Triethylamine, Solvent B: 99% Ethylacetate + 1% Triethylamine. Evaporation of product containing fractions gave additional 1.8 g product of -70% purity. MS (ESI) m/z 399/401(M+H). 1H NMR (CDCl3) delta ppm 7.63 (s, 1 H), 7.48 (d, 1H, J= 9.2), 7.42 (d, 2 H, J= 7.9), 7.18- 7.14 (m, 3H), 6.41 (s, 1 H), 3.80-3.40 (bm, 4 H), 2.42 (bs, 4H), 2.32 (s, 3H).

The synthetic route of 55121-99-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok, Vinayak; BATT, Douglas, G.; LIU, Qingjie; JOHNSON, Walter, L.; MASTALERZ, Harold; ZHANG, Guifen; ZIMMERMANN, Kurt; WO2010/80474; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Fluoro-2-methoxy-1-nitrobenzene (2.55 g, 14.9 mmol),N-acetylpiperazine (1.91 g, 14.9 mmol),Potassium carbonate (2.47 g, 17.9 mmol)Was added to N, N-dimethylacetamide (25 mL).The reaction was heated to 120 C for 5 hours. Ethyl acetate (50 mL) was added and the mixture was washed with saturated brine (50 mL). The organic layer was dried, dried and column chromatographed (petroleum ether: ethyl acetate = 5: 1) to give the product as a white solid (1.87 g, yield 45.0 %).

13889-98-0, As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference£º
Patent; Shandong Xuanzhu Pharmaceutical Technology Co., Ltd; Wu, Yongqian; (68 pag.)CN105884695; (2016); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Sodium hydride (0.86 g, 21 mmol) was added to fert-butyl (3S)-3-(hydroxymethyl)piperazine-l-carboxylate (1.244 g, 5.75 mmol) in THF (40 ml) at rt. The resulting mixture was stirred at rt for 10 min. 7-Bromo-8-chloro-5,6-difluoroquinazolin-4-ol (1.7 g, 5.75 mmol) was added slowly and the resulting solution was stirred at 40C for 1 h. The reaction mixture was quenched with water (2 ml). The reaction mixture was adjusted to pH = 7 with 2M HCI. The crude product was purified by C18-flash chromatography (0 to 65% MeOH in water (0.1% TFA)) to afford ferf-butyl (3S)-3-{[(7-bromo-8-chloro-6-fluoro-4-hydroxyquinazolin-5-yl)oxy]methyl}piperazine-l-carboxylate (1.65 g, 58%) as a brown solid. XH NMR (400 MHz, DMSO) 1.35 (9H, s), 2.62-3.07 (2H, m), 3.11-3.19 (2H, m), 3.20-3.76 (1H, m), 3.80-3.88 (1H, m), 3.98-4.29 (3H, m), 8.23 (1H, s). m/z: ES+ [M+H]+ = 491., 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; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics