Some tips on 59702-07-7

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, [0808] To a solution of (8-((5-cyano-4-((2-methoxyethyl)amino )pyridin-2-yl)carbamoyl)-2-( dimethoxymethyl)-5,6, 7,8-tetrahydro-1 ,8-naphthyridin-3-yl)methyl methanesulfonate(intermediate 170, 368 mg, 0.657 mmol) in DCM(2.7 ml) at room temperature was added NEt3 (0.319 ml,2.301 mmol) followed by 1-methylpiperazin-2-one (120 mg,1.052 mmol). The reaction mixture was stirred at room temperaturefor 2 hand partitioned between DCM and water. Thewater layer was extracted multiple times with DCM, thecombined organic layers were dried using Na2S04 , filteredand evaporated. The crude product was purified by silica gelcolunm chromatography using a gradient ofMeOH (0-3percent) inDCM to yield the title compound as a white solid. (UPLC-MS3) tR 0.87 min; ESI-MS 553.3 [M+Ht. 1H NMR (600 MHz,CDCI3 ) ll13.75 (s, lH), 8.20 (s, lH), 7.64 (br s, lH), 7.58 (s,lH), 5.56 (s, lH), 5.23 (d, lH), 4.06-4.01 (m, 2H), 3.70 (br s,2H), 3.63 (t, 2H), 3.50-3.42 (m, 8H), 3.40 (s, 3H), 3.31 (br s,2H), 3.14 (br s, 2H), 2.96 (br s, 3H), 2.87-2.80 (m, 2H), 2.71(br s, 2H), 2.03-1.96 (m, 2H).

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Novartis AG; Buschmann, Nicole; Fairhurst, Robin Alec; Furet, Pascal; Knoepfel, Thomas; Leblanc, Catherine; Liao, Lv; Mah, Robert; Nimsgern, Pierre; Ripoche, Sebastien; Xiong, Jing; Han, Bo; Wang, Can; Zhao, Xianglin; US2015/119385; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

Brief introduction of 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

59702-07-7, A solution of 2,6-dichloro-4-cyclopropylpyridine-3,5-dicarbonitrile (synthesis described in example 4 step 2, 238 mg, 1 mmol) 1-methylpiperazin-2-one (114 mg, 1 mmol), and triethylamine (121 mg, 1.2 mmol) in N,N-dimethylformamide (8 mL) was stirred at room temperature for 30 minutes, then diluted with water (50 mL) and extracted with ethyl acetate (50 mL x 2). The combined organic layers were dried and concentrated under vacuum to give 2-chloro-4-cyclopropyl-6-(4-methyl-3-oxopiperazin-1-yl)pyridine-3,5-dicarbonitrile (260 mg, 83percent) as a brown solid. LCMS m/z = 315.8 [M+H]+.

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ADAMS, Nicholas David; BENOWITZ, Andrew B.; RUEDA BENEDE, Maria Lourdes; EVANS, Karen Anderson; FOSBENNER, David T.; KING, Bryan Wayne; LI, Mei; MILLER, William Henry; REIF, Alexander Joseph; ROMERIL, Stuart Paul; SCHMIDT, Stanley J.; WIGGALL, Kenneth; (1283 pag.)WO2017/216726; (2017); A1;,
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Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 59702-07-7

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of (8-((5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)carbamoyl)-2-(dimethoxymethyl)-5,6 ,7 ,8-tetrahydro-1 ,8-naphthyridin-3-yl)methyl methanesu Ifonate (intermediate170, 368 mg, 0.657 mmol) in DCM (2.7 ml) at room temperature was added NEt3 (0.319 ml, 2.301mmol) followed by 1-methylpiperazin-2-one (120 mg, 1.052 mmol). The reaction mixture was stirred at room temperature for 2 h and partitioned between DCM and water. The water layer was extracted multiple times with DCM, the combined organic layers were dried using Na2504, filtered and evaporated. The crude product was purified by silica gel column chromatography usinggradient of MeOH (0-3percent) in DCM to yield the title compound as a white solid. (UPLC-MS 3) tR 0.87mm; ESl-MS 553.3 [M+H].1H NMR (600 MHz, CDCI3)5 13.75 (s, IH), 8.20 (s, IH), 7.64 (brs, IH),7.58 (s, I H), 5.56 (s, I H), 5.23 (d, I H), 4.06 ? 4.01 (m, 2H), 3.70 (br s, 2H), 3.63 (t, 2H), 3.503.42 (m, 8H), 3.40 (s, 3H), 3.31 (br s, 2H), 3.14 (br s, 2H), 2.96 (br s, 3H), 2.87 ?2.80 (m, 2H), 2.71(br s, 2H), 2.03 ? 1.96 (m, 2H)., 59702-07-7

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; BUSCHMANN, Nicole; FAIRHURST, Robin Alec; FURET, Pascal; KNOePFEL, Thomas; LEBLANC, Catherine; MAH, Robert; NIMSGERN, Pierre; RIPOCHE, Sebastien; LIAO, Lv; XIONG, Jing; ZHAO, Xianglin; HAN, Bo; WANG, Can; WO2015/59668; (2015); A1;,
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Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 1-Methylpiperazin-2-one

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, A mixture of 3-bromomethylbenzoic acid (4.30 g, 20 mmol), 1-methylpiperazin-2-one (2.3 g, 20 mmol),38 and powdered potassiumcarbonate (2.76 g, 20 mmol) in ethanol (50 mL) was stirredfor 17 h at room temperature. The solvent was evaporated off underreduced pressure to give a residue which was treated with HCl(10 mL of 2 M) and extracted with EtOAc. The combined extractswere washed with water, dried and the solvent was evaporatedoff under reduced pressure to give 8, which was recrystallised fromEtOAc/hexane to give a cream crystalline solid, mp 161?166 C; 1HNMR (DMSO-d6) d 2.63 (t, J = 5.5 Hz, 2H), 2.80 (s, 3H), 2.96 (s, 2H),3.26 (t, J = 5.5, 2H), 3.61 (s, 2H), 7.46 (d, J = 8.0 Hz, 2H), 7.90 (d,J = 8.0 Hz, 2H), 12.9 (br s, 1H).

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Manley, Paul W.; Blasco, Francesca; Mestan, Ju?rgen; Aichholz, Reiner; Bioorganic and Medicinal Chemistry; vol. 21; 11; (2013); p. 3231 – 3239;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 59702-07-7

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

Preparation of l-methyl-4-r2-(4-{l-r3-(trifluoromethyl)ri,2,41triazolor4,3- blpyridazin-6-yllpiperidin-4-yl}phenoxy)ethyllpiperazin-2-oneDIPEA (15.27 niL, 87.69 mmol) was added to 2-(4-{l-[3-(trifluoromethyl)[l,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl}phenoxy)ethyl methanesulfonate (14.19 g, 29.23 mmol) and 1 -methylpiperazin-2-one (CAS 59702-07-7, 3.67 g, 32.15 mmol) in DMA (70 mL). The resulting solution was stirred at 1100C for 1 hour. The reaction mixture was cooled to room temperature, absorbed onto silica, evaporated to dryness and then purified by flash silica chromatography, elution gradient 0 to 3percent MeOH in DCM. Pure fractions were evaporated and the resulting gum was scratched with ether until solid. The solid was stirred in ether (100 mL) for 4 hours then collected by filtration and dried to give l-methyl-4-[2-(4-{l-[3- (trifTuoromethyl)[ 1 ,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4- yl}phenoxy)ethyl]piperazin-2-one (10.08 g, 68.5percent) as a solid.IH NMR (399.9 MHz, CDC13) delta 1.76 (2H, m), 2.00 (2H, m), 2.75 – 2.87 (5H, m), 2.95 (3H, s), 3.11 (2H, m), 3.28 (2H, s), 3.34 (2H, t), 4.09 (2H, t), 4.37 (2H, m), 6.86 (2H, d), 7.11 – 7.14 (3H, m), 7.92 (IH, d); m/z = 504 [M+H]+., 59702-07-7

The synthetic route of 59702-07-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; RABOW, Alfred, Arthur; WO2010/131022; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 59702-07-7

59702-07-7, 59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

Example 1786-(3-fluorophenyl)-N-{(1S,3R)-3-[(4-methyl-3-oxopiperazin-1 -yl)carbonyl] cyclopenty^nicotinamide To a solution of (1 R, 3S)-3-({[6-(3-fluorophenyl)pyridine-3-yl]carbonyl}amino) cyclyopentanecarboxylic acid (Example 1 1 b, 49.3 mg, 0.15 mmol) and triethylamine (68.2 mg, 0.675 mmol) in dimethylformamide (1.3 mL) was added HBTU (65.2 mg, 0.172 mmol) and the solution was stirred at room temperature for 1 hour. 1-Methylpiperazin-2-one (29.4 mg, 0.195 mmol) was added and the solution was stirred at room temperature overnight. The dimethylformamide was removed by evapouration in vacuo and the residue was partitioned between water (7 mL) and ethyl acetate (7 ml_). The organic layer was separated and evaporated to give a red-brown gum which was purified by HPLC Method (B) to give 23.2 mg of the title compound (LCMS Method (A), RT 2.83 min, 100percent area ES m/z [M+] 424.19).

59702-07-7, 59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER LIMITED; WO2009/153720; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 1-Methylpiperazin-2-one

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

Example 0723 Triethylamine was added to a solution of hydrochloride (23 mg) of 1-methylpiperazin-2-one in dichloromethane (1 mL), followed by adjusting to pH 8. 3-(4-(6-((5-Isopropylpyridazin-3-yl)amino)-1,5-naphthyridin-3-yl)-1H-pyrazol-1-yl)propanal (19 mg), acetic acid (0.01 mL), and sodium triacetoxyborohydride (42 mg) were added thereto, followed by stirring at room temperature for 1 hour. The solvent was distilled off under reduced pressure, and the obtained residue was purified by silica gel column chromatography (ethyl acetate-methanol, NH silica), thereby obtaining 4-(3-(4-(6-((5-isopropylpyridazin-3-yl)amino)-1,5-naphthyridin-3-yl)-1H-pyrazol-1-yl)propyl)-1-methylpiperazin-2-one (4.4 mg) as a white solid. 1H-NMR (DMSO-d6) delta: 10.70 (1H, s), 9.05 (1H, d, J=1.8 Hz), 8.86 (1H, d, J=2.1 Hz), 8.72 (1H, s), 8.52 (1H, s), 8.24- 8.18 (3H, m), 7.70 (1H, d, J=9.3 Hz), 4.24-4.17 (2H, m), 3.30-3.25 (2H, m), 3.09-2.98 (1H, m), 2.87-2.83 (2H, m), 2.80 (3H, s), 2.66-2.60 (2H, m), 2.40-2.32 (2H, m), 2.07-1.98 (2H, m), 1.34 (6H, d, J=7.2 Hz). MS m/z (M+H): 486., 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; FUJIFILM Corporation; FURUYAMA, Hidetomo; KURIHARA, Hideki; TERAO, Takahiro; NAKAGAWA, Daisuke; TANABE, Shintaro; KATO, Takayuki; YAMAMOTO, Masahiko; SEKINE, Shinichiro; MASHIKO, Tomoyuki; INUKI, Shinsuke; UEDA, Satoshi; US2015/322063; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 59702-07-7

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,59702-07-7

EXAMPLE 160 N-(4-fluorobenzyl)-8-hydroxy-5-(4-methyl-3-oxopiperazin-1-yl)-1,6-naphthyridine-7-carboxamide A solution of 5-bromo-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide (0.20 g, 0.53 mmol), 1-methylpiperazin-2-one (0.21 g, 1.86 mmol) and diisopropylethylamine (0.19 mL, 1.06 mmol) in DMPU (2.0 mL) were heated at 135C for 26 hr. Diisopropylethylamine (0.19 mL, 1.06 mmol) was added and the reaction heated at 135C for a further 24 hr. The reaction was cooled to room temperature, neutralized by the addition of TFA and purified by reverse phase HPLC. (Vydak C18, Gradient elution with Water: Acetonitrile 95:5 to 5:95 with 0.1percent TFA at 30 mL/min over 15 mins). Lyophilization of the pure fractions afforded the title compound as an off white solid. 1H NMR (CDCl3, 400 MHz) delta 12.95 (1H, s), 9.18 (1H, dd, J=1.6 and 4.4 Hz), 8.43 (1H, dd, J=1.7 and 8.4 Hz), 8.21 (1H, m), 7.63(1H, dd, J=4.3 and 8.4 Hz), 7.40(2H, m), 7.05(2H, t, J=8.7 Hz), 4.65 (2H, d, J=6.4 Hz), 4.01 (2H, s), 3.61 (2H, t, J=5.7 Hz), 3.34(2H, t, J=5.7 Hz), 2.95 (3H, s) ppm. FAB MS calcd for C21H20FN5O3 410 (MH+), found 410.

59702-07-7 1-Methylpiperazin-2-one 4399042, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Anthony, Neville J.; Gomez, Robert P.; Young, Steven D.; Egbertson, Melissa; Wai, John S.; Zhuang, Linghang; Embrey, Mark; Tran, LeKhanh; Melamed, Jeffrey Y.; Langford, H. Marie; Guare, James P.; Fisher, Thorsten E.; Jolly, Samson M.; Kuo, Michelle S.; Perlow, Debra S.; Bennett, Jennifer J.; Funk, Timothy W.; US2003/55071; (2003); A1;,
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Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 10-(benzyloxy)-4-bromo-2-(4-fluorobenzyl)-8-methyl-7,8- dihydropyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-dione (0.10 g, 0.19 mmol; Example 160, Step 1) and 1-methylpiperazin-2-one (2 mL) was heated in a sealed tube in an oil bath at 100 ¡ãC overnight. The benzyl protecting group was also cleaved in the process. The reaction mixture was subjected to reverse phase preparative HPLC purification. Collection and lyophilization of appropriate fractions provided the title compound. 1H NMR (400 MHz, DMSO-d6) No. 7.33 (dd, J = 8.6,5.7 Hz, 2H), 7.14 (t, J = 9.0 Hz, 2H), 5.08 (s, 2H), 4.49 (br s, 2H), 3.68 (m, 2H), 3.30 (m, 2H), 2.99 (s, 3H), 2.83 (s, 3H). ES MS M+l = 455, 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; MERCK & CO., INC.; WO2005/110414; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

59702-07-7, 1-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2: A mixture of 0.2 g (0.50 mmol) intermediate II.5 step 1 , 70 mg (0.61 mmol) 1 – Methylpiperazin-2-one, 90 mg (0.65 mmol) K2C03 and acetonitrile is heated to 80¡ãC in a pressure tube for 3.5 h. After cooling to RT the solvent is evaporated and DCM and water are added. The organic phase is separated, dried, filtered and evaporated. (0548) Yield: 0.1 g (Yield 59percent), ESI-MS: m/z = 436 M+H+, R,(HPLC) : 0.25 min (HPLC-W), 59702-07-7

As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BLUM, Andreas; WO2015/169677; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics