Month: November 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

A suspension of 2-chloro-/V-methyl-/V-(4-nitrophenyl)acetamide (1.0 g, 4.37 mmol) in ethyl acetate (10 mL) was heated to 40 C for 30 min and added l-methylpiperazine (1.2 mL, 10.9 mmol) at the same temperature. The mixture was stirred at 50 C for 2 h. The reaction mixture was cooled to RT and diluted with ethyl acetate. The solution was washed with water and dried over anhydrous sodium sulfate. The solution was filtered, concentrated and diluted with methanol. The solution was subjected to hydrogenation in the presence of palladium on carbon as catalyst under 25 bar of hydrogen pressure at 25 C for 2 h. The catalyst was removed by filtration and the solvent was evaporated at 60 C to yield 400 mg of the desired compound. 1 H NMR (400 MHz, DMSO-de) d 1.88 (s, 3H), 2.14-2.19 (m, 4H), 2.63-2.68 (m, 4H), 2.80 (s, 2H), 3.01 (s, 3H), 5.20 (br s, 2H), 6.53 (d, J= 8.1 Hz, 2H), 6.88 (d, J= 8.7 Hz, 2H)., 109-01-3

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

Reference£º
Patent; ICHNOS SCIENCES S.A.; CHAUDHARI, Sachin, Sundarlal; GHARAT, Laxmikant, Atmaram; IYER, Pravin; DHONE, Sachin, Vasantrao; ADIK, Bharat, Gangadhar; WADEKAR, Prashant, Dilip; GOWDA, Nagaraj; BAJPAI, Malini; (233 pag.)WO2020/70331; (2020); A1;,
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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.

The product was prepared according to General Procedure 1 using 8-tert-butyl- 6-(4,4-difluorocyclohexyl)imidazo [1 ,2-b]pyridazine-2-carboxylic acid (500 mg, 1.482 mmol), DMF (10 mL), HATU (845.3 mg, 2.223 mmol), Huenig?s base (775 tL, 4.449 mmol) and tert-butyl 3,3-dimethylpiperazine-1-carboxylate (476.4 mg, 2.223 mmol Purification by flash chromatography on silica gel was carried out under standard condition to afford title compound tert-butyl 4-[8-tert-butyl-6-(4,4-difluorocyclohexyl)imidazo [1 ,2-b]pyridazine-2- carbonyl]-3,3-dimethyl-piperazine-1-carboxylate (766 mg, 1.435 mmol, 96.85%) as a white solid. ?H NMR (400 MHz, Chloroform-cl) oe 8.23 (s, 1H), 6.72 (s, 1H), 4.31 (t, J= 6.3 Hz, 2H), 3.68-3.34 (m, 4H), 2.81 (t, J= 10.9 Hz, 1H), 2.24 (dt, J= 12.3, 7.2 Hz, 2H), 2.12 -1.72 (m, 6H), 1.59 (s, 6H), 1.52 (t, J= 1.9 Hz, 9H), 1.47 (d, J= 1.7 Hz, 9H). LC-MS: 534.26 (M+Hj., 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; VERTEX PHARMACEUTICALS INCORPORATED; FARMER, Luc J.; FOURNIER, Pierre-Andre; LESSARD, Stephanie; LIU, Bingcan; ST-ONGE, Miguel; STURINO, Claudio; SZYCHOWSKI, Janek; YANNOPOULOS, Constantin; WO2015/48245; (2015); A1;,
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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

General procedure: The mixture of 2a (1.9 g, 8.8 mM), morpholine (1.1 mL, 13.2 mM) and triethylamine (1.8 mL, 13.2 mM) were heated to reflux in THF for 2 h. The mixture was partitioned between ethyl acetate (60¡Á2 mL) and water (40¡Á2 mL), the organic layer was evaporated. The oily residue 3a utilized as materials without further purification., 109-01-3

As the paragraph descriping shows that 109-01-3 is playing an increasingly important role.

Reference£º
Article; Wang, Lu; Zhang, Qing; Zhu, Gaoyuan; Zhang, Zhimin; Zhi, Yanle; Zhang, Li; Mao, Tianxiao; Zhou, Xiang; Chen, Yadong; Lu, Tao; Tang, Weifang; European Journal of Medicinal Chemistry; vol. 130; (2017); p. 86 – 106;,
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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a stirring solution of 2-methylpiperazine 7 (3 g, 30.00 mmol) in CH2C12 (100 mL) under argon atmosphere were added triethylamine (9 mL, 90.00 mmol) and Boc-anhydride (7.2 mL, 33.00 mmol) at 0 ¡ãC; warmed to RT and stirred for 16 h. The reaction was monitored by TLC; after completion of the reaction, the volatiles were removed in vacuo. The crude was washed with -pentane (2 x 20 mL) and dried in vacuo to afford compound 9 (5 g, 83percent) as off- white solid. TLC: 5percent MeOH/ CH2C12 (R/. 0.4); 1H-NMR (OMSO-d6, 400 MHz): delta 3.80- 3.62 (m, 2H), 3.27-3.09 (m, 2H), 2.83-2.71 (m, 2H), 2.37-2.17 (m, 1H), 1.39 (s, 9H), 0.92 (d, J= 6.3 Hz, 3H)., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION; ARNOLD, Lee Daniel; MAAG, Hans; TURNER, JR., William W.; (274 pag.)WO2016/168619; (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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

A solution of methyl 4-((N-phenylvinylsulfonamido)methyl)benzoate (0.300 g, 0.905 mmol), (2S,6R)-2,6-dimethylpiperazine (0.207 g, 1.811 mmol) and N,N-Diisopropylethylamine (0.189 mL, 1.086 mmol) in tetrahydrofuran (5 mL) was stilTed at the room temperature for 5 hr. Then, water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with aqueous saturated ammonium chloride solution, dried with anhydrous MgSO4, filtered, and concentrated in vacuo. The residue was chromatographed (Si02, 4 g cartridge; methanol / dichloromethane =0 percent to 10 percent) to give methyl4-(((2-((3S,5R)-3 ,5-dimethylpiperazin- 1 -yl)-N-phenylethyl) sulfonamido)methyl)benzo ate as white solid (0.403 g, 99.9 percent).

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; CHOI, Daekyu; MIN, Jaeki; BAE, Miseon; YANG, Hyunmo; KIM, Dohoon; (644 pag.)WO2017/18803; (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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

[4990] A solution of N-(4-(chloi methyl)phenyl)thiomotpholine-4-carboxamide 1,1-dioxide (l.OOOg.3.303 mmol), tert-butyl (3S,5R)-3.5-dimethylpipeiazine-l-carboxylate (1.416 g.6.606 mmol) and potassium carbonate (1.369 g, 9.909 mmol) in acetonitrile (50 mL) prepared at the room temperature was stirred at the same temperature for 18 hr and concentrated under the reduced pressure. Then, water was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous MgS0 , filtered, and concentrated in vacuo. The residue was diluted with diethylether (15 mL) and stirred. The resulting precipitates were collected by filtration, washed by diethylether, and dried to give tert-butyl (2S,6R)-4-(4-(l,l-dioxidothiomorpholine-4-carboxamido)benzyl)-2,6-dimethylpiperaz ine-l-carboxylate as pale yellow solid (1.580 g, 99.5 ).

129779-30-2, The synthetic route of 129779-30-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; KIM, Yuntae; LEE, Chang Sik; SONG, Hyeseung; GWAK, Dal-Yong; LEE, Jaeyoung; OH, Jung Taek; LEE, Chang Gon; KIM, II Hyang; (1041 pag.)WO2017/23133; (2017); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

934-98-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

00106] Step 6. To a solution of 4-((lH-indol-3-yl)methyl)-3-ethylaniline (0.8 g, 3.2 mmol) and 4-nitrophenyl carbonochloridate (0.64 g, 3.2 mmol) in THF was added diisopropylethylamine (0.4 g, 3.2 mmol) (16 mL) at 20 ¡ãC and the resulting solution was stirred for 30 min. Then 2-(4-methylpiperazin-l-yl)ethanamine (0.9 g, 6.4 mmol) was added to the solution. After the addition was complete, the mixture was stirred at 20 ¡ãC for 12 h. The mixture was concentrated and purified by preparative HPLC to give l-(4-((lH-indol-3- yl)methyl)-3-ethylphenyl)-3-(2-(4-methylpiperazin-l-yl)ethyl)urea (0.33 g, 26percent) as a yellow solid. 1H NMR (400 MHz, MeOD) delta: 1.13-1.17 (t, 3H), 2.25 (s, 3H), 2.48-2.71 (m, 10H), 3.29- 3.32 (m, 2H), 4.01 (s, 2H), 6.73 (s, 1H), 6.92-6.96 (m, 1H), 7.02-7.08 (m, 3H), 7.18 (s, 1H), 7.29-7.31 (d, J = 8.0 Hz, 1H), 7.39-7.41 (d, J = 7.6 Hz, 1H); MS (M+l+): 220.3.

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; WO2013/148365; (2013); 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.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

Maleic anhydride (501.9 mg, 5.11 mmol) was dissolved in CHC13 (25 mL) and 2-(4- methylpiperazin-l-yl)ethan-l -amine (767 mu^, 5.11 mmol) was then added. The reaction was stirred at room temperature for 2 hours. The solvent was removed in vacuo and the crude solid was resuspended in acetic anhydride (25 mL). To the reaction was then added sodium acetate (250 mg). The reaction was heated to reflux under N2 for 3 hours. After reflux, the reaction was cooled to room temperature and washed with hexanes to obtain 3 (crude) as a dark brown/black oil. MS: m/z (M+l) +: 224.28, 934-98-5

As the paragraph descriping shows that 934-98-5 is playing an increasingly important role.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; BRADNER, James E.; QI, Jun; FEDERATION, Alexander; JACOBSON, Zoe; VARCA, Anthony; (125 pag.)WO2018/58029; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

120737-59-9, tert-Butyl 3-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 135 1-fluoro-4-nitrobenzene (5.0 g, 35.46 mmol, 1.0 eq) and 248 tert-butyl 3-methylpiperazine-1-carboxylate (7.09 g, 35.46 mmol, 1.0 eq) in 95 DMSO (40 mL) was added 64 K2CO3 (9.78 g, 70.92 mmol, 2.0 eq). The reaction mixture was heated at 120¡ã C. for 16 h. Progress of the reaction was monitored by LCMS. Upon the consumption of starting material, mixture was diluted with water (100 mL) and extracted with ethyl acetate (200 mL¡Á2). Combined organic layer was washed with water (50 mL¡Á3), dried over anhydrous Na2SO4 and concentrated under reduced pressure. Crude residue was purified by flash chromatography using 19 ethyl acetate: 20 hexane as eluents to obtain 249 tert-butyl 3-methyl-4-(4-nitrophenyl)piperazine-1-carboxylate (5.5 g, 48.67percent). (0378) LCMS: 322 [M+1]+, 120737-59-9

The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (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.34770-60-0,4-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

To a solution of (5R)-9-[2-(3-bromophenyl)-3,3,3-trifluoro-2-methoxypropanoyl]-5-(4- fluorophenyl)-3,9-diazaspiro[5.5]undecan-2-one (Example 1 14) (100.0 mg, 179 pmol) and 4- methylpiperazin-2-one (CAS-RN: 34770-60-0) (41 .0 mg, 359 pmol) in 1 ,4-dioxane (1 mL) was added caesiumcarbonat (146 mg, 449 pmol), Dipalladium- tris(dibenzylideneacetone)chloroform complex (CAS-RN: 52522-40-4) (9.29 mg, 8.97 pmol) and 4,5-Bis(diphenylphosphino)-9,9-dimethylxanthene (Xantphos, CAS-RN: 161265-03-8). The mixture was stirred at 900 for 8 h. The reac tion mixture was diluted with water and extracted with dichloromethane. The combined organic layer was dried with sodium sulfate, filtered and concentrated in vacuo. The residue was purified via preparative HPLC (method 6) to give the title compound 9.60 mg (90 % purity, 8 % yield).LC-MS (Method): Rt= 1 .04 min; MS (ESIpos): m/z = 591 [M+H]+1H-NMR (400 MHz, DMSO-d6) d [ppm]: 0.243 (0.68), 0.266 (0.45), 0.540 (0.91 ), 0.570 (0.76), 1 .022 (0.74), 1 .056 (1 .20), 1 .145 (0.52), 1 .170 (0.58), 1.279 (1.50), 1 .432 (0.95), 1.463 (0.82), 1 .646 (0.41 ), 1 .898 (0.99), 1 .942 (1 .30), 2.169 (1 .55), 2.219 (2.82), 2.235 (2.31 ), 2.272 (10.52), 2.293 (16.00), 2.331 (0.85), 2.338 (0.64), 2.518 (4.14), 2.523 (2.99), 2.539 (2.14), 2.699 (1 .1 1 ), 2.712 (1 .94), 2.728 (3.32), 2.744 (4.02), 2.757 (2.47), 2.777 (1.05), 2.793 (1 .83), 2.810 (1 .03),2.844 (0.66), 2.876 (1 .09), 2.907 (0.62), 3.027 (0.60), 3.062 (1.38), 3.080 (1 .48), 3.094 (1 .34),3.1 14 (6.29), 3.140 (9.75), 3.240 (2.06), 3.372 (6.95), 3.577 (10.91 ), 3.595 (2.47), 3.606 (2.31 ), 3.623 (1 .30), 3.662 (0.85), 3.676 (1.51 ), 3.690 (1 .67), 3.704 (1.44), 3.714 (1 .15), 3.726 (0.52),3.970 (0.56), 4.004 (0.52), 4.168 (0.85), 4.200 (0.80), 6.944 (1.96), 6.958 (2.39), 6.966 (2.89),6.980 (2.47), 7.035 (1 .05), 7.054 (1.13), 7.1 19 (2.68), 7.134 (2.47), 7.141 (4.97), 7.155 (3.90),7.162 (2.68), 7.177 (1 .96), 7.243 (1.05), 7.266 (2.66), 7.280 (2.17), 7.288 (1 .84), 7.296 (2.25),7.302 (1.88), 7.316 (4.17), 7.336 (1.55), 7.403 (0.99), 7.425 (1.61 ), 7.445 (2.83), 7.466 (1 .92),7.486 (2.41 ), 7.505 (2.66), 7.524 (1.65), 7.565 (0.41 ), 7.573 (0.43), 7.606 (3.05), 7.633 (2.04)., 34770-60-0

The synthetic route of 34770-60-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER AKTIENGESELLSCHAFT; BAYER PHARMA AKTIENGESELLSCHAFT; GRAHAM, Keith; BUCHGRABER, Philipp; AIGUABELLA FONT, Nuria; WITTROCK, Sven; HEINRICH, Tobias; BRAeUER, Nico; KUHNKE, Lara, Patricia; LANGE, Martin; BADER, Benjamin; PRECHTL, Stefan; LIENAU, Philip; KOPITZ, Charlotte, Christine; NOWAK-REPPEL, Katrin; POTZE, Lisette; STEUBER, Holger; (754 pag.)WO2020/48831; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics