Category: 485841-52-9

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of (R)-3-cyclohexyl-2, 3-dihydropyrrolo [1,2, 3-de] -1, 4-benzoxazine-6- carboxylic acid (120 mg, 0.421 mmol) and (S)-1, 2-dimethylpiperazine (62 mg, 0.547 mmol) in N,N-dimethylformamide (3.0 mi) was added 1- (3-dimethylaminopropyl)-3- ethylcarbodiimide (97 mg, 0.505 mmol) and 1-hydroxy benzotriazole (68 mg, 0.505 mmol). The mixture was stirred at room temperature for 18 h, then partitioned between dichloromethane and water. The aqueous layer was extracted with dichloromethane, and combined organic layers were washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash chromatography eluting with 0-20% (v/v) methanol in ethyl acetate to afford the title compound as the free base. Hydrochloride salt formation was achieved by the addition of hydrogen chloride (2 M solution in diethyl ether; 0.5 mi) to a solution of the free base in diethyl ether (2 ml) and ethanol (1 ml). The solvent was removed in vacuo and the precipitate was dried to afford title compound (1: 1 hydrochloride salt) as a solid (84 mg, 0.20 mmol). ‘H NMR (400MHz, CD30D) 81. 00-1. 35 (5H, m), 1.39 (3H, d, J 4. 8), 1.58 (1H, d, J 12.0), 1.60-1. 70 (1H, m), 1.70-1. 82 (3H, m), 1.82-1. 90 (1H, m), 2.96 (3H, s), 3.20- 3.70 (5H, m), 4.20-4. 30 (2H, m), 4.40-4. 70 (2H, m), 4.71 (1H, d, J 10.0), 6.67 (1H, d, J 8.2), 7.08 (1H, t, J8. 2), 7.21 (1H, d, J 8.2), 7.74 (1H, s); EsIMS : m/z = 382.1 [M+H] +, 268.1

485841-52-9, The synthetic route of 485841-52-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AKZO NOBEL N.V.; WO2005/58327; (2005); 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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of (R)-3-cyclohexyl-2, 3-dihydropyrrolo [1,2, 3-de] -1, 4-benzoxazine-6- carboxylic acid (120 mg, 0.421 mmol) and (S)-1, 2-dimethylpiperazine (62 mg, 0.547 mmol) in N,N-dimethylformamide (3.0 mi) was added 1- (3-dimethylaminopropyl)-3- ethylcarbodiimide (97 mg, 0.505 mmol) and 1-hydroxy benzotriazole (68 mg, 0.505 mmol). The mixture was stirred at room temperature for 18 h, then partitioned between dichloromethane and water. The aqueous layer was extracted with dichloromethane, and combined organic layers were washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash chromatography eluting with 0-20% (v/v) methanol in ethyl acetate to afford the title compound as the free base. Hydrochloride salt formation was achieved by the addition of hydrogen chloride (2 M solution in diethyl ether; 0.5 mi) to a solution of the free base in diethyl ether (2 ml) and ethanol (1 ml). The solvent was removed in vacuo and the precipitate was dried to afford title compound (1: 1 hydrochloride salt) as a solid (84 mg, 0.20 mmol). ‘H NMR (400MHz, CD30D) 81. 00-1. 35 (5H, m), 1.39 (3H, d, J 4. 8), 1.58 (1H, d, J 12.0), 1.60-1. 70 (1H, m), 1.70-1. 82 (3H, m), 1.82-1. 90 (1H, m), 2.96 (3H, s), 3.20- 3.70 (5H, m), 4.20-4. 30 (2H, m), 4.40-4. 70 (2H, m), 4.71 (1H, d, J 10.0), 6.67 (1H, d, J 8.2), 7.08 (1H, t, J8. 2), 7.21 (1H, d, J 8.2), 7.74 (1H, s); EsIMS : m/z = 382.1 [M+H] +, 268.1

485841-52-9, The synthetic route of 485841-52-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AKZO NOBEL N.V.; WO2005/58327; (2005); 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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of (R)-3-cyclohexyl-2, 3-dihydropyrrolo [1,2, 3-de] -1, 4-benzoxazine-6- carboxylic acid (120 mg, 0.421 mmol) and (S)-1, 2-dimethylpiperazine (62 mg, 0.547 mmol) in N,N-dimethylformamide (3.0 mi) was added 1- (3-dimethylaminopropyl)-3- ethylcarbodiimide (97 mg, 0.505 mmol) and 1-hydroxy benzotriazole (68 mg, 0.505 mmol). The mixture was stirred at room temperature for 18 h, then partitioned between dichloromethane and water. The aqueous layer was extracted with dichloromethane, and combined organic layers were washed with brine, dried over Na2SO4 and concentrated. The residue was purified by flash chromatography eluting with 0-20% (v/v) methanol in ethyl acetate to afford the title compound as the free base. Hydrochloride salt formation was achieved by the addition of hydrogen chloride (2 M solution in diethyl ether; 0.5 mi) to a solution of the free base in diethyl ether (2 ml) and ethanol (1 ml). The solvent was removed in vacuo and the precipitate was dried to afford title compound (1: 1 hydrochloride salt) as a solid (84 mg, 0.20 mmol). ‘H NMR (400MHz, CD30D) 81. 00-1. 35 (5H, m), 1.39 (3H, d, J 4. 8), 1.58 (1H, d, J 12.0), 1.60-1. 70 (1H, m), 1.70-1. 82 (3H, m), 1.82-1. 90 (1H, m), 2.96 (3H, s), 3.20- 3.70 (5H, m), 4.20-4. 30 (2H, m), 4.40-4. 70 (2H, m), 4.71 (1H, d, J 10.0), 6.67 (1H, d, J 8.2), 7.08 (1H, t, J8. 2), 7.21 (1H, d, J 8.2), 7.74 (1H, s); EsIMS : m/z = 382.1 [M+H] +, 268.1

485841-52-9, The synthetic route of 485841-52-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AKZO NOBEL N.V.; WO2005/58327; (2005); 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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.,485841-52-9

75 mg (0.16 mmol) of 3-[(chloroacetyl)amino]-N-[6-(2-fluorophenyl)pyridin-3-yl]-4- (trifluoromethoxy)benzamide (intermediate 14) were dissolved in 0.69 mL of anh DMF. 4.1 mg (0.025 mmol) of potassium iodide, 0.042 mL (0.24 mmol) of N-ethyl-N-isopropylpropan-2-amine and 27.5 mg (0.24 mmol) of (2S)-l,2-dimethylpiperazine were added. It was stirred at rt overnight. The reaction mixture was concentrated to dryness under vacuum. The residue was purified by HPLC (method 2) yielding 34.5 mg (39%) of the title compound. XH-NMR (400 MHz, DMSO-d6): delta [ppm]= 1.01 – 1.12 (m, 3H), 2.09 – 2.45 (m, 5H, partly overlapping with the DMSO signal), 2.77 – 3.02 (m, 3H), 3.25 (br. s, 2H), 7.30 – 7.39 (m, 2H), 7.44 – 7.52 (m, 1H), 7.64 – 7.70 (m, 1H), 7.82 – 7.91 (m, 2H), 7.94 – 8.00 (m, 1H), 8.31 (dd, 1H), 8.75 – 8.81 (m, 1H), 9.07 (d, 1H), 9.91 (s, 1H), 10.75 (s, 1H). LC-MS (method 4): Rt = 0.99 min; MS (ESIpos): m/z = 546 [M+H]+.

As the paragraph descriping shows that 485841-52-9 is playing an increasingly important role.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; THEDE, Kai; BENDER, Eckhard; SCOTT, William J.; RICHTER, Anja; ZORN, Ludwig; LIU, Ningshu; MOeNNING, Ursula; SIEGEL, Franziska; GOLZ, Stefan; HAeGEBARTH, Andrea; LIENAU, Philip; PUEHLER, Florian; BASTING, Daniel; SCHNEIDER, Dirk; MOeWES, Manfred; WO2014/147021; (2014); A2;,
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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.,485841-52-9

A solution of tert-butyl (l-(5-(3-cyano-6-ethoxypyrazolo[l,5-a]pyridin-4- yl)pyridin-2-yl)-4-formylpiperidin-4-yl)carbamate (Intermediate P71, 278 mg, 0.567 mmol) and (S)-l,2-dimethylpiperazine (Intermediate P93; 270 mg, 2.36 mmol) in DCE (5 mL) was stirred for 30 min at ambient temperature before adding NaBH(AcO)3 (480.4 mg, 2.267 mmol). The resulting mixture was stirred overnight at ambient temperature, then concentrated in vacuo. The residue was suspended in 4: 1 DCM:iPrOH, and extracted sequentially with saturated NaHCCb(aq) (2x) and brine. The organic extracts were dried over anhydrous Na2S04(S), filtered and concentrated in vacuo. The residue was purified by silica chromatography (using 0-15% [MeOH with 1% H4OH] in DCM as the gradient eluent) to cleanly afford the title compound (133 mg, 40% yield). MS (apci) m/z = 589.3 (M+H).

485841-52-9 (S)-1,2-Dimethylpiperazine 28305740, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ANDREWS, Steven W.; ARONOW, Sean; BLAKE, James F.; BRANDHUBER, Barbara J.; COLLIER, James; COOK, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; MCFADDIN, Elizabeth A.; MCKENNEY, Megan L.; MCNULTY, Oren T.; METCALF, Andrew T.; MORENO, David A.; RAMANN, Ginelle A.; TANG, Tony P.; REN, Li; WALLS, Shane M.; (946 pag.)WO2018/71454; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

485841-52-9, (S)-1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Diisopropylethylamine (215mul, 1.25mmol) was added to a solution of compound17a(300mg, 0.54mmol) in DMF (6ml), followed by Dimethylamine dihydrochloride (61mg, 0.75mmol), HOBt (7mg, 0.05mmol) and EDC/HCl (116mg, 0.60mmol). The solution was stirred for 16h at room temperature. The reaction mixture was diluted with saturated aqueous sodium bicarbonate, and extracted with EtOAc. The organic layer was washed with brine (3 times), and dried over magnesium sulfate. The mixture was filtered, and the solvent was removed in vacuo to afford the crude product. The residue was purified by flash silica gel chromatography with CHCl3/MeOH (30:1, v/v) to give the pale orange solid (116mg, 40% yield), which was precipitated from Et2O/n-hexane;

485841-52-9, 485841-52-9 (S)-1,2-Dimethylpiperazine 28305740, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Miyazaki, Masaki; Naito, Hiroyuki; Sugimoto, Yuuichi; Yoshida, Keisuke; Kawato, Haruko; Okayama, Tooru; Shimizu, Hironari; Miyazaki, Masaya; Kitagawa, Mayumi; Seki, Takahiko; Fukutake, Setsuko; Shiose, Yoshinobu; Aonuma, Masashi; Soga, Tsunehiko; Bioorganic and Medicinal Chemistry; vol. 21; 14; (2013); p. 4319 – 4331;,
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.485841-52-9,(S)-1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.,485841-52-9

General procedure: To a solution of 53 (0.1 mmol, 1.0 eq.) in EtOH (2 mL) was addedEt3N (10.0 eq.) and corresponding amine (5.0 eq.). The reactionwasstirred at 85 C overnight, and then quenched with saturatedNaHCO3 aqueous solution. The aqueous layer was extracted withdichloromethane. The organic layer was dried over Na2SO4 andconcentrated. The residue was purified by silica gel column chromatography(dichloromethane/methanol 100/1) to give thedesired product.

The synthetic route of 485841-52-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Du, Qian; Fu, Chunyan; Ge, Wenxiang; He, Sudan; Li, Zhanhui; Luo, Lusong; Ma, Haikuo; Sun, Xiaotian; Tian, Sheng; Wang, Xu; Wang, Yujie; Zhang, Xiaohu; Zhang, Yi; Zheng, Jiyue; Zhu, Fang; European Journal of Medicinal Chemistry; (2019);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

485841-52-9,485841-52-9, (S)-1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: (S)-1,3-Dimethylpiperazine dihydrochloride (0.16 g, 0.85 mmol) was added in oneportion to (2S)-2-bromo-N-(3-{2-[(3-methoxy-1-methyl-1 H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1 Hindol-7-yl)propanamide (0.2 g, 0.43 mmol, Intermediate 32) and potassium carbonate (0.24 g, 1.7 mmol) in DMF (2 mL) at 0C. The resulting solution was stirred at 25C for 16 hours. The crude product was purified by preparative HPLC (X Bridge C18, 5 tim, 19×150 mm; Mobile Phase A: water0.05% TFA, Mobile Phase B: acetonitrile; Flow rate: 20 mLmin; Gradient: 20%B70%B in 10 mm; 254 nm) to afford (2R)-2-[(2S)-2,4-dimethylpiperazin-1-yl]-N-(3-{2-[(3-methoxy-i -methyl-i H-pyrazol-4-yl)amino]pyrimidin-4-yl}-i H-indol-7-yl)propanamide (49 mg, 23%, Example 1) as a white solid;

The synthetic route of 485841-52-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAND, Annika, Birgitta, Margareta; GRIMSTER, Neil, Patrick; KAWATKAR, Sameer; KETTLE, Jason, Grant; NILSSON, Magnus, K.; RUSTON, Linette, Lys; SU, Qibin; VASBINDER, Melissa, Marie; WINTER-HOLT, Jon, James; WU, Dedong; YANG, Wenzhan; GRECU, Tudor; MCCABE, James; WOESSNER, Richard, Donald; CHUAQUI, Claudio, Edmundo; (175 pag.)WO2017/50938; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics