Category: 34770-60-0

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.

Intermediate 5A. l -(Isoquinolin-5-yl)-4-methylpiperazin-2-one: To 5- bromoisoquinoline (1.66 g, 7.96 mmol) and 4-methylpiperazin-2-one (1, 8.76 mmol) was added DMSO (7 mL), 1, 10-phenanthroline (0.144 g, 0.796 mmol), potassium carbonate (3.30 g, 23.89 mmol) and the mixture was degassed with Ar for 30 min., copper(I)iodide (1.213 g, 6.37 mmol) was added and the reaction was heated in oil bath at 130 C overnight. The reaction was cooled to room temperature and quenched with NuEta4OmicronEta (10 mL) and water (20 mL) and diluted with EtOAc. The aqueous layer was extracted EtOAc (2 x 50 mL) and then, nBuOH (lx 30 mL). Combined organic layers were washed with – I l l – brine and dried (MgS04). Purification by silica gel chromatography afforded 1.5g (78%) yellow solid. MS (ESI) m/z: 242.0 (M+H)+.

34770-60-0, 34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; PINTO, Donald J.P.; CLARK, Charles G.; SMITH, II, Leon M.; ORWAT, Michael J.; JEON, Yoon; CORTE, James R.; WO2014/160668; (2014); 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

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(iii) (S)- 1 -(4- 1 [2-Amino-4-( 1 -hvdroxyhexan-3-ylamino)-6-methylpyrimidin-5-yl]methyl } -3- methoxyphenyl)-4-methylpiperazin-2-one To a solution of the product from step (ii) (126 mg, 0.240 mmol) in 1 ,4-dioxane (1 mL) was added Cul (46.0 mg, 0.240 mmol), N,N ‘-dimethyldiaminoethane (52.0 mu, 0.480 mmol), 4-methylpiperazin-2-one (55.0 mg, 0.480 mmol), and Cs2C03 (234 mg, 0.720 mmol). The mixture was heated to 100C and stirred for 1 Oh. After cooling, water was added and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried (Na2S04). After removal of the solvent in vacuo, the crude residue was used for the next reaction without further purification. To the crude residue in THF (1.0 mL) was added tetra-rc-butylammonium fluoride (1.0 mL, 1M solution in THF) and the mixture was stirred at r.t.. After 5h, water was added and the resulting mixture was extracted with EtOAc. The combined organic solutions were washed with brine, and then dried(Na2S04). After removal of the solvent in vacuo, the crude residue was purified by silica gel column chromatography to give the title compound as a white amorphous solid (19.6 mg, 0.0430 mmol, 18%); NMR: 6.94 (1H , d), 6.86 (1 H, d), 6.75 (1H, dd), 5.07 (2H, br s), 4.90 (1H, d), 4.51 (1H, br s), 4.13 (1 H, m), 3.88 (3H, s), 3.69-3.65 (2H, m), 3.67 (2H, s,),3.31-3.26 (2H, m), 3.25 (2H, s), 2.78-2.76 (2H, m), 2.40 (3H, s), 2.35 (3H, s), 1.80-1.76 (1H, m), 1.44-1.1 1 (5H, m), 0.81 (3H, t); LC-MS: m/z = 457 [MH+] (T = 1.48).

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; ASTRAZENECA AKTIEBOLAG; TOSAKI, Shinya; HORI, Seiji; WO2012/67268; (2012); 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.

A mixture of 1 -bromo-4-iodobenzene (0.87 g, 3.1 mmol), 4-methylpiperazin-2- one (0.30 g, 2.6 mmol), 3P04 (1.1 g, 5.1 mmol), trans-N, N’-dimethylcyclohexane-l ,2-diamine (0.08 mL, 0.51 mmol) and dioxane (5 mL) was purged with argon gas for 10 min. Copper(I) iodide (0.049 g, 0.26 mmol) was added, the vial sealed and heated at 110 C in an oil bath for 22 h. The reaction was then allowed to cool to rt and was diluted with EtOAc and saturatedNaHC03 was added. The resulting mixture was extracted with EtOAc and the combined organic extracts were dried over MgS04 and concentrated to give the crude product. Purification by silica gel chromatography (MeOH/CH2Cl2, 5:95 to 1 :9) gave an inseparable 2: 1 mixture of the desired product and l-(4-bromophenyl)-4-methylpiperazin-2-one (200 mg). NMR (400 MHz, CDCI3) 6 7.66 (d, J = 8.0 Hz, 2H), 7.02 (d, J = 8.0 Hz, 2H), 3.64 (t, J = 5.0 Hz, 2H), 3.22 (s, 2H), 2.73 (t, J = 5.0 Hz, 2H), 2.35 (s, 3H); MS ESI 317.1 [M + H]+, calcd for [C, ,H|3IN20+ H]+ 317.01.

34770-60-0, As the paragraph descriping shows that 34770-60-0 is playing an increasingly important role.

Reference£º
Patent; UNIVERSITY HEALTH NETWORK; PAULS, Heinz, W.; LI, Sze-Wan; SAMPSON, Peter Brent; FORREST, Bryan T.; WO2012/48411; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics