Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.,76003-29-7

Sodium hydride (80 mg, 2.0 mmol, 60% in mineral oil) was added to a solution of 4-tert-butyloxycarbonyl-piperazin-2-one (200 mg, 1.0 mmol) in dimethylformamide (5.0 mL) at 0 C. The reaction was stirred at 0 C. for 0.5 h. To this mixture was added benzyl bromide (300 uL, 2.5 mmol) and the reaction was stirred for 2 h at room temperature. The reaction mixture was quenched with a dilute aqueous solution of sodium bicarbonate and extracted with methylene chloride. The organic extracts were washed with brine and dried over anhydrous sodium sulfate. Purification of the crude residue by chromatography over silica gel using 30% ethyl acetate in hexane gave 4-tert-butyloxycarbonyl-2-benzyl-piperazin-2-one (174 mg, 60% yield). [0350] Hydrochloric acid (0.25 mL, 1.00 mmol, 4 M in 1,4-dioxane) was added to a solution of 4-tert-butyloxycarbonyl-2-benzyl-piperazin-2-one (174 mg, 0.60 mmol) in 1,4-dioxane (1.0 mL). The mixture was stirred overnight. The reaction was concentrated to give 2-benzyl-piperazin-2-one hydrochloride as an off-white solid (130 mg, 97% yield). [0351] 4,5-Bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-1-carbonyl chloride (example 3) was reacted with 2-benzyl-piperazin-2-one hydrochloride using the procedure as described in example 5 to give 4-[4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-carbonyl]-1-benzyl-piperazin-2-one. It was then dissolved in dilute hydrochloric acid (0.5 N, 1 mL) and lyophilized to give 4-[4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-carbonyl]-1-benzyl-piperazin-2-one hydrochloride as an off-white powder (65 mg, 89% yield). LR-MS (APCI): 695.6 [(M+H)+].

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

Reference£º
Patent; Haley, Gregory Jay; Kong, Norman; Liu, Emily Aijun; Simonsen, Klaus B.; Vu, Binh Thanh; Webber, Stephen Evan; US2004/259884; (2004); A1;,
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13889-98-0, 1-Acetylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

13889-98-0, General procedure: Compound 4 0.2 g (0.41 mmol) and 25 muL piperdine (0.82 mmol) was added to the 1.0 mL dried CH2Cl2.Anhydrous Na2CO3 20 mg was then added to the mixture, which was stirred for 12 h. The mixturewas washed with the distilled water, the organic phase was separated and dried over anhydrousNa2SO4, and then concentrated viarotary evaporation. The crude product was purified by silica gelchromatography with petroleum ether-acetone-strong ammonia water (v/v/v, 8/1/0.1) as the eluentto gain 0.18 g yellow solid compound 5a in 90% yield.

The synthetic route of 13889-98-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Feng, Xiu E.; Wang, Qin Jin; Gao, Jie; Ban, Shu Rong; Li, Qing Shan; Molecules; vol. 22; 12; (2017);,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

694499-26-8, 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; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
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129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0256] Alternatively, the title compound can be prepared via the mono-piperidine compound, shown in the above scheme, beginning with Intermediate C, using two stepwise pairs of (a) amino acid coupling from with l-(tert-butyl) 3-methyl piperazine- 1,3- dicarboxylate, and (b) ester hydrolysis. HATU and DIPEA in DMF were employed at room temperature for 12 hours for the coupling reactions. The hydrolyses were accomplished with LiOH at room temperature for one hour. The combination of coupling and hydrolysis occurred in roughly 60% yield when performed on a gram scale. The steps could be accomplished by someone skilled in the art.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference£º
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; LINK, James, T.; LISSANU DERIBE, Yonathan; (91 pag.)WO2019/200217; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1 equiv. of 15 was dissolved in DCM (anhydrous) and 1.5 equiv of TEA was added to reaction mixture and taken down to 0 C. in an ice-bath. To this mixture was added 1.1 equiv of acetyl chloride and was allowed to reach room-temp and stopped after 1 hour. The solvent was removed by reduced pressure and was partitioned between DCM and water. The aqueous was washed 3 times with DCM and all organic washes were combined and dried with sodium sulfte, filtered and concentrated which resulted in a light brown/tan solid (91%). MS (ES) 320.3 [MH+], 170911-92-9

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

Reference£º
Patent; Castelhano, Arlindo; McKibben, Bryan; Steinig, Arno; US2003/229067; (2003); A1;,
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381242-61-1, 1-(4-Nitro-2-(trifluoromethyl)phenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 1-bromo-2-chloroethane (0.43 mL, 5.2 mmol),K2CO3 (0.71 g, 5.2 mmol) in ACN (10 mL) was stirred at 50 C for15 min and then 1-(2-methoxyphenyl)piperazine (4, 0.5 g,2.6 mmol) in ACN (5 mL), was added dropwise within 1 h duration.Reaction mixture was further stirred for 4 h. Then the mixture wasconcentrated under reduced pressure and residue was dissolved inEtOAc (15 mL) and the EtOAc layer was then washed with water(10mL x 3). The combined organic layer was dried (anhyd. Na2SO4)and concentrated under reduced pressure. The resultant waswashed with distilled hexane and again dried under high vaccum.The pure offwhite crystals were obtained by recrystallization usingEtOAc/Hexane (yield: 69%).

381242-61-1, 381242-61-1 1-(4-Nitro-2-(trifluoromethyl)phenyl)piperazine 2771413, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Gupta, Sonal; Pandey, Deepti; Mandalapu, Dhanaraju; Sharma, Vikas; Shukla, Mahendra; Singh, Seema; Singh, Nidhi; Yadav, Santosh Kumar; Tanpula, Dilip Kumar; Singh, Surabhi; Maikhuri, Jagdamba P.; Shukla, Shubha; Lal, Jawahar; Siddiqi, Mohammad I.; Gupta, Gopal; Sharma, Vishnu L.; European Journal of Medicinal Chemistry; vol. 132; (2017); p. 204 – 218;,
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.59702-31-7,1-Ethylpiperazine-2,3-dione,as a common compound, the synthetic route is as follows.

The compound (0.15 g) obtained in Reference Example 20, 1-ethylpiperazine-2,3-dione (75 mg), sodium hydride (14 mg) and N,N-dimethylformamide (1 ml) were stirred at room temperature for 1 hr. The reaction mixture was diluted with ethyl acetate (100 ml), washed with 5% aqueous potassium hydrogen sulfate solution, saturated aqueous sodium hydrogen carbonate solution and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. 4N Hydrogen chloride-ethyl acetate solution (10 ml) was added to the residue, and the mixture was stirred at room temperature for 1 hr. The solvent was evaporated under reduced pressure, and the residue was washed with ethyl acetate to give the title compound (72 mg) as a colorless powder. melting point 264-271C. Elemental analysis (C15H22ClN3O2¡¤0.1H2O) Calcd.: C, 57.45; H, 7.13; N, 13.40. Found: C, 57.19; H, 7.03; N, 13.40., 59702-31-7

The synthetic route of 59702-31-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP1876179; (2008); A1;,
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Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 188 (15 mg, 0.039 mmol) in DMF (3 mL) was added (5)-l-N- Boc-2-methylpiperazine (9.4 mg, 0.047 mmol) and Et3N (10 mu, 0.072 mmol) and heated at 90 C for 2 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH, 10:1) to afford Boc-protected intermediate in quantitative yield. To this was added 1 mL of a solution of CH2Ci2:TFA (7:3) and stirred at rt for 4 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH-NH3 (7 N), 20: 1) to afford 17 mg (98%) of 191. 1H NMR (500 MHz, CDC13): delta 8.17 (s, 1H), 7.35 (d, J= 8.4 Hz, 2H), 7.10 (t, J= 7.8 Hz, 1H), 7.04 (d, J= 8.4 Hz, 2H), 6.72 (dd, J= 8.1, 1.7, 1H), 6.67 (d, J= 7.5 Hz, 1H), 6.60 (s, 1H), 5.29 (d, J= 12.7 Hz, 1H), 5.24 (d, J = 12.7 Hz, 1H), 4.76 (m, 1H), 4.42-4.47 (m, 1H), 3.65 (s, 3H), 3.00-3.12 (m, 2H), 2.84-2.94 (m, 2H), 2.67-2.73 (m, 1H), 1.22 (d, J= 6.8 Hz, 3H); MS (ESI) m/z [M+H]+ 448.3., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
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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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

4-chloro-3-(3-fluorophenyl)-1-[2-(4-methylpiperazin-1-yl)ethyl]-5-phenyl-pyrazolo[3,4-c]pyridazine (Compound 8) A mixture of 4-chloro-3-(3-fluorophenyl)-5-phenyl-1H-pyrazolo[3,4-c]pyridazine (0.33 mmol), 2-(4-methylpiperazin-1-yl)ethanol (0.65 mmol), diethyl azodicarboxylate (114 mg, 0.65 mmol) and triphenyl phosphine (171 mg, 0.65 mmol) in 1,4-dioxane (2 mL) was heated using microwave irradiation to a temperature between 85 and 120¡ã C. for a 30 to 90 min period. The reaction mixture was concentrated in vacuo and the residue was purified by preparative HPLC to provide Compound 8. 1H NMR delta (ppm)(CHCl3-d): 7.81-7.77 (2H, m), 7.57-7.44 (6H, m), 7.20-7.18 (1H, m), 4.95 (2H, t), 3.07 (2H, t), 2.65 (4H, bs), 2.35 (4H, bs), 2.25 (3H, s). LCMS (10 cm_Formic_ACE 3 C18 AR_HPLC_CH3CN) Rt 9.93 min; m/z 451 [M+H] 99.18percent purity., 5464-12-0

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Usher III Initiative; Buerli, Roland Werner; Krishna Esmieu, William Rameshchandra; Lock, Christopher James; Malagu, Karine Fabienne; Owens, Andrew Pate; Harte, William E.; US2014/121205; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: Cool in ice a solution of the product of Preparation 13, Step 3 (1.53 g, 5.2 mmol) and DIPEA (1.10 ml, 6.2 mmol) in THF (40 ml). Add dropwise 4-bromobutyryl chloride (1.01 g, 5.4 mmol). Stir 2 h and partition with ether and satd. NaHCO3. Dry (MgSO4) and concentrate to obtain the carbamate as a yellow solid

154590-35-9, As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference£º
Patent; Schering Corporation; US2004/220194; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics