Category: 59702-07-7

59702-07-7,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.

An oven-dried microwave vial (0.5-2.0 ml_ volume) was charged with (S)-2- cyclopropyl-10-((2,5-dichloropyrimidin-4-yl)amino)-3,3-difluoro-7-methyl-1 ,2,3,4-tetrahydro- [1 ,4]oxazepino[2,3-c]quinolin-6(7/-/)-one (Intermediate A10a; 7 mg, 0.015 mmol), 1- methylpiperazin-2-one (4 mg, 0.037 mmol) and DIPEA (13 uL, 0.075 mmol). The reaction vial was flushed with Ar and sealed with a cap. NMP (0.65 ml_) was added and the reaction mixture was heated at 140C under microwave irradiation for 1 h. The reaction mixture was dissolved in DMSO (0.8 ml_) and directly purified by reverse-phase chromatography (Biotage reverse-phase 12 g Ultra C-18 column; 10-60-80-100% MeOH in H2O (containing 0.1 % formic acid)). The product-containing fractions were combined, passed through an SCX-2 (1 g), additional MeOH (10 ml_) was passed through and the product was eluted with 2 N methanolic ammonia (25 ml_). The solvent was removed in vacuo affording the title compound (5 mg, 57%) as an off-white solid. 1 H NMR (600 MHz, methanol-d?) d 8.04 (d, J = 2.2 Hz, 1 H), 8.01 (s, 1 H), 7.92 (dd, J = 9.1 , 2.2 Hz, 1 H), 7.57 (d, J = 9.1 Hz, 1 H), 4.53- 4.38 (m, 2 H), 4.24 (d, J = 18.2 Hz, 1 H), 4.18 (d, J = 18.2 Hz, 1 H), 3.98-3.92 (m, 1 H), 3.92-3.87 (m, 1 H), 3.73 (s, 3 H), 3.47-3.39 (m, 2 H), 3.35-3.28 (m, 1 H), 2.98 (s, 3 H), 1.42-1.37 (m, 1 H), 0.82-0.75 (m, 1 H) 0.68-0.57 (m, 2 H), 0.37-0.31 (m, 1 H); LCMS (Method X4) RT 2.85 min; m/z calcd for C25H27CIF2N703+ [M+H]+: 546.1832, Found: 546.18342.

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

Reference：
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL; BELLENIE, Benjamin Richard; CHEUNG, Kwai Ming Jack; DAVIS, Owen Alexander; HOELDER, Swen; HUCKVALE, Rosemary; COLLIE, Gavin; MENICONI, Mirco; BRENNAN, Alfie; LLOYD, Matthew Garth; (222 pag.)WO2019/197842; (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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, To 337 (31.8 mg, 0.0684 mmol) was added l-methylpiperazin-2-one (51.5 mg, 0.342 mmol) and Et3N (50 mu) in DMF (1 mL) and heated at 90 °C for 1 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH, 20: 1) to afford 31.8 mg (86percent) of 344. MS (ESI) m/z [M+H]+ 543.1.

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

Reference：
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; CHIOSIS, Gabriela; KANG, Yanlong; PATEL, Hardik J.; PATEL, Maulik; OCHIANA, Stefan; RODINA, Anna; TALDONE, Tony; SHRESTHA, Liza; (288 pag.)WO2015/175707; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7,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.

An oven-dried microwave vial (0.5-2.0 ml_ volume) was charged with (S)-2- cyclopropyl-10-((2,5-dichloropyrimidin-4-yl)amino)-3,3-difluoro-7-methyl-1 ,2,3,4-tetrahydro- [1 ,4]oxazepino[2,3-c]quinolin-6(7/-/)-one (Intermediate A10a; 7 mg, 0.015 mmol), 1- methylpiperazin-2-one (4 mg, 0.037 mmol) and DIPEA (13 uL, 0.075 mmol). The reaction vial was flushed with Ar and sealed with a cap. NMP (0.65 ml_) was added and the reaction mixture was heated at 140C under microwave irradiation for 1 h. The reaction mixture was dissolved in DMSO (0.8 ml_) and directly purified by reverse-phase chromatography (Biotage reverse-phase 12 g Ultra C-18 column; 10-60-80-100% MeOH in H2O (containing 0.1 % formic acid)). The product-containing fractions were combined, passed through an SCX-2 (1 g), additional MeOH (10 ml_) was passed through and the product was eluted with 2 N methanolic ammonia (25 ml_). The solvent was removed in vacuo affording the title compound (5 mg, 57%) as an off-white solid. 1 H NMR (600 MHz, methanol-d?) d 8.04 (d, J = 2.2 Hz, 1 H), 8.01 (s, 1 H), 7.92 (dd, J = 9.1 , 2.2 Hz, 1 H), 7.57 (d, J = 9.1 Hz, 1 H), 4.53- 4.38 (m, 2 H), 4.24 (d, J = 18.2 Hz, 1 H), 4.18 (d, J = 18.2 Hz, 1 H), 3.98-3.92 (m, 1 H), 3.92-3.87 (m, 1 H), 3.73 (s, 3 H), 3.47-3.39 (m, 2 H), 3.35-3.28 (m, 1 H), 2.98 (s, 3 H), 1.42-1.37 (m, 1 H), 0.82-0.75 (m, 1 H) 0.68-0.57 (m, 2 H), 0.37-0.31 (m, 1 H); LCMS (Method X4) RT 2.85 min; m/z calcd for C25H27CIF2N703+ [M+H]+: 546.1832, Found: 546.18342.

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

Reference：
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL; BELLENIE, Benjamin Richard; CHEUNG, Kwai Ming Jack; DAVIS, Owen Alexander; HOELDER, Swen; HUCKVALE, Rosemary; COLLIE, Gavin; MENICONI, Mirco; BRENNAN, Alfie; LLOYD, Matthew Garth; (222 pag.)WO2019/197842; (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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

59702-07-7, To 337 (31.8 mg, 0.0684 mmol) was added l-methylpiperazin-2-one (51.5 mg, 0.342 mmol) and Et3N (50 mu) in DMF (1 mL) and heated at 90 °C for 1 h. Solvent was removed under reduced pressure and the residue was purified by preparatory TLC (CH2Cl2:MeOH, 20: 1) to afford 31.8 mg (86percent) of 344. MS (ESI) m/z [M+H]+ 543.1.

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

Reference：
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; CHIOSIS, Gabriela; KANG, Yanlong; PATEL, Hardik J.; PATEL, Maulik; OCHIANA, Stefan; RODINA, Anna; TALDONE, Tony; SHRESTHA, Liza; (288 pag.)WO2015/175707; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 solution of 1-methylpiperazin-2-one (198 mg, 1.74 mmol) in dichloromethane (4.00 mL) was added to a stirred solution of methyl 2-chloropyrimidine-5-carboxylate (300 mg, 1.74 mmol) in dichloromethane (4.70 mL) at 25¡ã C. The resulting solution was stirred at room temperature for 4 h under nitrogen. The reaction mixture was concentrated and dissolved in ethyl acetate (25 ml) and NaOH (50 ml, 1M aqueous solution). The organic layer was washed with ethyl acetate (25 ml). The organic layers were combined and washed with brine (50 ml), dried using MgSO4, filtered and evaporated to dryness to afford methyl 2-(4-methyl-3-oxopiperazin-1-yl)pyrimidine-5-carboxylate (246 mg, 57percent) as a cream solid. 1H NMR (399.9 MHz, DMSO-d6) delta 2.91 (3H, s), 3.44 (2H, t), 3.83 (3H, s), 4.09 (2H, t), 4.35 (2H, s), 8.86 (2H, s). MS: m/z 501 (2MH+), 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; ASTRAZENECA AB; US2008/153812; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Preparation of l-methyl-4-[2-(4-{l-[3-(trifluoromethyl)[l,2,4]triazolo[4,3- b]pyridazin-6-yl]piperidin-4-yl}phenoxy)ethyl]piperazin-2-one; DIPEA (15.27 mL, 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 l-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-(trifluoromethyl)[l,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

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

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BRADBURY, Robert, Hugh; CARR, Gregory, Richard; RABOW, Alfred, Arthur; RAO KORUPOJU, Srinivasa; TUMMA, Harikrishna; WO2010/92371; (2010); 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.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

To a solution of methyl 2-[1-(3-ethylphenyl)cyclopentyl]ethanimidate hydrochloride (2.0 g) and 1-methylpiperazin-2-one (1.62 g) in THE (150 ml) was added at 22¡ãC diisopropylethyl amine (1.83 g) and after 5 mm acetic acid (426 mg) and stirring was continued at 22¡ãC for 16 h. The mixture can be further processed as described below or the intermediate 4-[2-[1-(3- ethylphenyl)cyclopentyl]ethanimidoyl]-1 -methyl-piperazin-2-one hydrochloride can be isolated by dilution with ethyl ether followed by filtration and drying of the residue.The mixture containing the intermediate was cooled down to -30¡ãC, a solution of lithium hexamethyldisilazide in THF (1M, 50 ml) was added followed by diethyl oxalate (4.15 g) and stirring was continued at -30¡ãC. In case of incomplete conversion a further portion of lithium hexamethyldisilazide and diethyl oxalate has to be added. The mixture was warmed to 22¡ãC, partitioned between aqueous hydrochloric acid (1 N) and dichloromethane, the organic layerwas dried, evaporated, the residue triturated with diethyl ether, filtered and the residue dried to give example 1 (1.40 g) as a white powder. Alternatively, the crude material can purified by preparative HPLC (RP-18, MeCN/H20 containing 0.23percent of HCOOH).MS (ESI, mlz): 382.3 [(M+H)]

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

Reference£º
Patent; SAVIRA PHARMACEUTICALS GMBH; EUROPEAN MOLECULAR BIOLOGY LABORATORY; LERNER, Christian; KREIS, Lukas; WEIKERT, Robert James; NEIDHART, Werner; HILPERT, Hans; (97 pag.)WO2017/158147; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 mixture of ethyl 3-{[(benzyloxy)carbonyl]amino}-7-bromoquinoline-2-carboxylate (250 mg, 0.58 mmol), 1-methylpiperazin-2-one (130 mg, 1.2 mmol), Pd(OAc)2 (20 mg), dicyclohexyl(2′,6′-diisopropoxybiphenyl-2-yl)phosphine (41 mg, 0.087 mmol), and K3PO4 (490 mg, 2.3 mmol) in tert-butyl alcohol (8 mL) was purged with nitrogen then heated at 100¡ã C. in a sealed vial for 3 h. The mixture was then allowed to cool and EtOAc and water were added. The resulting layers were separated and organic layer was concentrated under reduced pressure. To the resulting bright-yellow solid, 2 mL of dioxane, 2 mL of 2 M NaOH were added. The mixture was heated in 80¡ã C. oil bath with stirring for 0.5 h, then allowed to cooled and neutralized with 4 mL of with 1 M Cl. The red solid formed was collected by filtration and air-dried overnight to give the sub-title compound (24 mg, 9.5percent). LCMS calc. for C26H33N8O2 [M+H]+: m/z=489.3. found: 435.2

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

Reference£º
Patent; INCYTE CORPORATION; Li, Yun-Long; Burns, David M.; Feng, Hao; Xue, Chu-Biao; Wang, Anlai; Pan, Jun; US2014/200216; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 202; 4-{7-[2-(4-Methyl-3-oxo-piperazin-1-yl)-ethoxy]-quinazolin-4-yl}-piperidine-1-carboxylic acid (4-pyrrolidin-1-yl-phenyl)-amide; To a solution of 4-[7-(-hydroxy-ethoxy)-quinazolin-4-yl]-piperidine-1-carboxylic acid tert-butyl ester (0.5 mmol), prepared as described in Example 169a, in anhydrous DCM, was added Et3N (1 mmol) and methanesulfonyl chloride (1 mmol) and the mixture was stirred at rt for 2 h. It was then washed with water (3.x.), dried over anhydrous MgSO4, filtered and concentrated in vacuo to obtain crude 4-[7-(3-methanesulfonyloxy-ethoxy)-quinazolin-4-yl]-piperidine-1-carboxylic acid tert-butyl ester. This (0.1 mmol) was dissolved in anhydrous DMSO together with 1-methyl-piperazin-2-one (0.2 mmol) and the mixture was stirred at 100¡ã C. for 2 h and then diluted with water and extracted with DCM. The DCM extract was washed with water (3.x.), dried over anhydrous MgSO4, filtered and concentrated in vacuo. To this was added 3M HCl/MeOH (1 mL) and the mixture was stirred at rt for 2 h and then concentrated in vacuo and the residue was dissolved in a 1:1 mixture of DCM:MeOH, neutralized with excess Et3N and treated with (4-pyrrolidin-1-yl-phenyl)-carbamic acid 4-nitrophenyl ester hydrochloride (0.11 mmol), as prepared by the method outlined in Example 74a. The mixture was stirred at rt overnight and then concentrated in vacuo and partitioned between water and DCM. DCM layer was drawn off, washed with water thrice, then dried over anhydrous MgSO4, filtered and concentrated in vacuo. The residue was purified by Preparative TLC (silica gel; DCM:MeOH, 95:5) followed by a further purification by Preparative HPLC to obtain 5.6 mg (6percent) of the title compound. 1H-NMR (300 MHz, CD3OD): 9.10 (s, 1H), 8.44 (d, 1H), 7.59-7.31 (m, 6H), 4.62 (t, 2H), 4.37 (m, 2H), 4.04-3.93 (m, 4H), 3.78-3.54 (m, 8H), 3.21 (m, 2H), 3.03 (s, 3H), 2.30-2.18 (m, 5H), 2.11-1.91 (m, 4H). LC/MS (ESI): 558.3 (MH)+.

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

Reference£º
Patent; Baindur, Nand; Gaul, Michael David; Kreutter, Kevin Douglas; Baumann, Christian Andrew; Kim, Alexander J.; Xu, Guozhang; Tuman, Robert W.; Johnson, Dana L.; US2006/281772; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

59702-07-7,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.

To a solution of 4-(3-(4-cyanophenyl)imidazo[l,2-a]pyridin-6-yl)benzoic acid (70 mg, 0.206 mmol) in DMF (1.0 mL) were added HATU (1 17 mg, 0.309 mmol), N-methyl morpholine (90 iL, 0.824 mmol) and l-methylpiperazin-2-one (37 mg, 0.247 mmol). The reaction mixture was stirred at room temperature under inert atmosphere for 18 h, then it was diluted with water (15 mL) and extracted with EtOAc (3×30 mL). The combined organic layer was dried over Na2S04 and concentrated under reduced pressure. The residue was purified by column chromatography (silica gel, eluent CHCl3 MeOH 96:4) to afford 4-(6-(4-(4-methyl-3- oxopiperazine-l-carbonyl)phenyl)imidazo[l,2-a]pyridin-3-yl)benzonitrile (64 mg, 57percent, AUC HPLC 98percent) as a white solid. 1H NMR (400 MHz, CD3OD) delta 8.76 (bs, 1H), 7.97-7.89 (m, 4H), 7.88 (s, 1H), 7.84-7.78 (m, 2H), 7.77 (d, J= 1.2 Hz, 2H), 7.64-7.57 (m, 2H), 4.40- 4.10 (m, 2H), 4.10-3.60 (m, 2H), 3.57-3.42 (m, 2H), 3.01 (s, 3H); 13C NMR (100 MHz, CD3OD): delta 171.72, 147.44, 140.53, 135.51, 134.81 , 134.72, 134.38, 129.42, 129.27, 128.56, 128.52, 127.79, 126.58, 122.93, 119.50, 1 18.47, 112.70, 34.68; MS (ESI) m/z 436 [C26H21N502 + H] +.

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

Reference£º
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH; NACRO, Kassoum; DURAISWAMY, Athisayamani, Jeyaraj; CHENNAMANENI, Lohitha, Rao; WO2013/147711; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics