Month: May 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115619-01-7,4-(4-Ethylpiperazin-1-yl)phenylamine,as a common compound, the synthetic route is as follows.

115619-01-7, A mixture of 5 (0.49g, 2.39mmol), H2O (0.75ml) and AcOH (3ml) was mixed with the 83 (0.15g, 3.13mmol) and refiuxed for overnight. The reaction was quenched by saturated NaHCO3 (aq.) and the mixture was extracted by ethyl acetate (30ml x 3). The residue was purified by flash column over silica gel (dichloromethane: methanol = 9: 1, Rf = 0.25) to afford 87 (0.60g, 80.20%) as a pale orange solid. 1H-NMR (300MHz, CDCl3): delta 1.16 (t, J= 7.2 Hz, 3H), 2.48 (q, J= 7.2 Hz, 2H), 2.64 (t, J= 5.1 Hz, 4H), 2.81 (d, J= 5.4 Hz, 3H), 3.22 (t, J= 5.1 Hz, 4H), 4.86 (s, 1H), 5.54 (s, 1H), 6.69 (s, 1H), 6.95 (d, J= 9.0 Hz, 2H), 7.18 (d, J= 8.7 Hz, 2H), 8.14 (s, 1H).

115619-01-7 4-(4-Ethylpiperazin-1-yl)phenylamine 936738, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; TAIPEI MEDICAL UNIVERSITY; YEN, Yun; LIOU, Jing-Ping; CHEN, Chun-Han; (70 pag.)WO2017/15400; (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.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

692058-21-2, tert-Butyl 4-(2,2,2-trifluoroethyl)piperazine-l-carboxylate (1.44 g, 5.37 mmol) was dissolved in 15 mL dichloromethane and trifluoroacetic acid (3.67 g, 32.2 mmol) The reaction was carried out for 1 hour at room temperature. After the reaction was completed, the solvent was evaporated under reduced pressure to give the titleCompound.

692058-21-2 1-Boc-4-(2,2,2-trifluoroethyl)piperazine 16748694, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Nanjing Shenghe Pharmaceutical Co., Ltd.; Wang Yong; Zhao Liwen; Ge Chongxun; Huang Yiqiang; Cao Chen; Li Qingqing; Hou Shaohua; (63 pag.)CN108276382; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6,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.

Into a 100-mL round-bottom flask was placed 1-methyl-7-((2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)-1,2,3,4-tetrahydroquinoline-2-carboxylic acid (50 mg, 0.15 mmol), N,N-dimethylformamide (5 mL), 4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)aniline (128 mg, 0.45 mmol), 4-(dimethylamino)pyridine (54 mg, 0.45 mmol), and N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (85 mg, 0.44 mmol). The mixture was stirred at room temperature overnight then concentrated. The residue was applied onto a silica gel column and eluted with ethyl acetate/petroleum ether (1 :5 to 1:0). The resulting product was further purified by prep-HPLC to yield N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-1-methyl-7-((2-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)-1,2,3,4-tetrahydroquinoline-2-carboxamide (7.5 mg, 8%). (ES, m/z): [M+H]+ = 607.30; NMR (400 MHz, methanol-iri, ppm) d 8.02 (d, J = 2.1Hz, 1H), 7.92 (d, J= 5.7 Hz, 1H), 7.82 (d, J = 8.5 Hz, 1H), 7.75 (d, J= 8.6 Hz, 1H), 7.01 (d, = 8. l Hz, 1H), 6.57 (d, J= 2.3 Hz, 1H), 6.50 (d, = 5.6 Hz, 1H), 6.41 (dd,.7= 8.0, 2.3 Hz, 1H), 6.07 (d, J= 1.1Hz, 1H), 4.11 (t,.7= 4.9 Hz, 1H), 3.66 (s, 2H), 2.95 (s, 3H), 2.77 (m, 2H), 2.55 (m, 9H), 2.54 – 2.41 (m, 2H), 2.39-2.16 (m, 2H), 1.33 (m, 2H), 1.13 (t, J= 12 Hz, 3H).

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

Reference：
Patent; LYCERA CORPORATION; AICHER, Thomas Daniel; SKALITZKY, Donald J.; TOOGOOD, Peter L.; VANHUIS, Chad A.; (416 pag.)WO2019/200120; (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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: The mixture of 13a (151 mg, 0.423 mmol) and 4 N HCl in 1,4-dioxane solution (1.38 ml) was stirred at room temperature overnight. After concentration, the residue was crystalized with etherto afford the white precipitation. The resulting solid was collected by filtration to afford 14a (121 mg, 98.0%) as the white solid. MSESI (m/z) = 257 [M+H]+. To a solution of 4a (116 mg, 0.35 mmol)in DMF (2.3 ml) was added 14a (120 mg, 0.42 mmol), COMU (225 mg, 0.525 mmol) and Et3N (177 mg, 1.75 mmol) at room temperature.The reaction mixture was stirred at same temperature for 1.5 h. The reaction mixture was diluted with sat. NaHCO3 solution to afford the pale yellow precipitation. The resulting solid was collected by filtration to 16a, 163765-44-4

As the paragraph descriping shows that 163765-44-4 is playing an increasingly important role.

Reference：
Article; Tsuno, Naoki; Yukimasa, Akira; Yoshida, Osamu; Suzuki, Shinji; Nakai, Hiromi; Ogawa, Tomoyuki; Fujiu, Motohiro; Takaya, Kenji; Nozu, Azusa; Yamaguchi, Hiroki; Matsuda, Hidetoshi; Funaki, Satoko; Yamanada, Natsue; Tanimura, Miki; Nagamatsu, Daiki; Asaki, Toshiyuki; Horita, Narumi; Yamamoto, Miyuki; Hinata, Mikie; Soga, Masahiko; Imai, Masayuki; Morioka, Yasuhide; Kanemasa, Toshiyuki; Sakaguchi, Gaku; Iso, Yasuyoshi; Bioorganic and Medicinal Chemistry; vol. 25; 7; (2017); p. 2177 – 2190;,
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.381242-61-1,1-(4-Nitro-2-(trifluoromethyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

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

As the paragraph descriping shows that 381242-61-1 is playing an increasingly important role.

Reference：
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.34334-28-6,4-(4-Methylpiperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

To a solution of 13 (1eq.) and CoCl2 6H20(2.1 eq.), NaBH4 (10 eq.) was added. The reaction mixture wasstirred for 5h and then filtered on a celite pad. The organic phase wasevaporated under reduced pressure. The yellow oil was purified by flashchromatography on silica gel (CH2Cl2:MeOH 8:2). Thedesired compound was obtained as a white solid (50%). 1H NMR (400MHz, MeOD): delta(ppm) 2.42(s, 3H); 2.74(t, J=8, 4H); 3.17(t, J=8, 4H), 4.43(s,2H); 6.89(d, J=8, 2H); 7.18(d, J=8, 2H). Anal. Calcd. for C12H19N3:C, 70.20; H, 9.33; N, 20.47; found; C, 70.10; H, 9.13; N, 20.27, 34334-28-6

34334-28-6 4-(4-Methylpiperazin-1-yl)benzonitrile 763205, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Radi, Marco; Bernardo, Vincenzo; Vignaroli, Giulia; Brai, Annalaura; Biava, Mariangela; Schenone, Silvia; Botta, Maurizio; Tetrahedron Letters; vol. 54; 38; (2013); p. 5204 – 5206;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

169447-70-5, (S)-tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of l-fluoro-4-nitrobenzene (3.5 g, 24.8 mmol) and K2C03 (10.2 g, 74.4 mmol) in DMF (15 mL) at 0C, (S)-tert-butyl 2-methylpiperazine- l-carboxylate (4.9 g, 24.8 mmol) was added and the mixture was stirred at rt overnight. The mixture was diluted with ice cold water (50 mL), the resulting precipitate was filtered and solid was washed with hexane (30 mL) to obtain (S)-tert-butyl 2-methyl-4-(4- nitrophenyl)piperazine-l-carboxylate (4.0 g, 51% yield). 1H NMR (400 MHz, DMSO- d6): delta 8.03 (d, 2H), 6.94 (d, 2H), 4.15-4.13 (m, 1H), 3.84-3.73 (m, 3H), 3.36-3.05 (m, 3H), 1.40 (s, 9H), 1.08 (d, 3H). LCMS m/z calcd for [M+H]+ 322.37, found 222.3., 169447-70-5

As the paragraph descriping shows that 169447-70-5 is playing an increasingly important role.

Reference：
Patent; ASANA BIOSCIENCES, LLC; VENKATESAN, Aranapakam M.; SMITH, Roger A.; THOMPSON, Scott K.; LAPING, Nicholas; KULKARNI, Bheemashankar; HALLUR, Gurulingappa; VISWANADHAN, Vellarkad N.; PENDYALA, Muralidhar; KETHIRI, Raghava Reddy; TYAGI, Rajiv; SIVANANDHAN, Dhanalakshmi; BAKTHAVATCHALAM, Rajagopal; WO2015/38417; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59878-57-8, General procedure: A mixture of magnolol (266mg, 1mmol), NaOH (40mg, 1mmol) and 37% formaldehyde solution (0.61mL) in ethanol (20mL) was stirred for 24hat room temperature. The mixture was extracted with ethyl acetate and the organic phase was washed with saturated salt water, dried with anhydrous Na2SO4, filtered, concentrated under reduced pressure, and purified by flash column chromatography on silica gel, to afford the pure product 12a. 12a (148mg, 0.5mmol) was dissolved in 10mL of CH2Cl2, the reaction mixture was cooled to 0C and SOCl2 (119mg, 1mmol) was added. The mixture was washed with saturated sodium bicarbonate solution, dried with anhydrous Na2SO4, filtered, concentrated under reduced pressure to give 12b. A 25mL round-bottomed flask was charged with 12b (100mg, 0.32mmol), different nitrogen heterocycles (0.32mmol), CsCO3 (140.4mg, 0.43mmol) and catalytic amount of KI. To this mixture were added MeCN (10mL) and the temperature was maintained at 80C overnight. The reaction mixture was cooled to room temperature and added H2O (10mL), followed by extraction with ethyl acetate. The combined organic extracts were washed with saturated salt water, dried over Na2SO4, filtered, concentrated under reduced pressure, and purified by column chromatography on silica gel, to afford the products A1-A22, respectively.

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Tang, Huan; Zhang, Yongguang; Li, Dan; Fu, Suhong; Tang, Minghai; Wan, Li; Chen, Kai; Liu, Zhuowei; Xue, Linlin; Peng, Aihua; Ye, Haoyu; Chen, Lijuan; European Journal of Medicinal Chemistry; vol. 156; (2018); p. 190 – 205;,
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.1214196-85-6,1-(tert-Butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

A suspension of 1-Boc-piperazine-2-carboxylic acid (9, 2.0 g, 8.69 mmol), EDCI (1.99 g, 10.42 mmol) and DMAP (0.32 g,2.61 mmol) in MeOH/CH2Cl2 (1:1) was stirred at 40 C for 1.5 hr, then the resulting solution was cooled down to room temperature and stirred for another 4 hrs. After removing the solvent, the residue was dissolved in CH2Cl2. The solution was washed with H2O (50 mL x 3). The combined aqueous was re-extracted with CH2Cl2 (40 mL x 3). All of the organics were combined, washed with 1 N NaHCO3 (50 mL x 3) and brine, and finally dried over Na2SO4. The product, a colorless liquid, was purified via flash chromatography, eluted with CH2Cl2 then 10% MeOH/CH2Cl2. Rf= 0.7 (10% MeOH/CH2Cl2, stained by phosphomolybdic acid (PMA)); yield – 84%, 1214196-85-6

As the paragraph descriping shows that 1214196-85-6 is playing an increasingly important role.

Reference：
Article; Zhao, Huanyu; Prosser, Anthony R.; Liotta, Dennis C.; Wilson, Lawrence J.; Bioorganic and Medicinal Chemistry Letters; vol. 25; 21; (2015); p. 4950 – 4955;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5271-27-2, 1-Methyl-3-phenylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1 -Methyl-3-phenylpiperazine (17.6 g; 0.1 mol) was dissolved in 100 dichloromethane. Triethylamine (15 ml; 0.1 mol) was added. A solution of benzoyl chloride (16 g; 0.1 14 mol) in dichloromethane was slowly added under cooling. After the total addition a white suspension was formed. The mixture was quenched with 10percent sodium carbonate. The organic layer was washed again with carbonate, dried and evaporated to an oil (ca 30 g). Purification by silica filtration using CH2CI2/Me0H (95:5). Evaporation of the appropriate fractions yielded 26.2 g oil (94 percent) Chiral GC: no separation using various methods.

5271-27-2, 5271-27-2 1-Methyl-3-phenylpiperazine 2760009, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; N.V. ORGANON; WO2007/144409; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics