Some tips on 5464-12-0

5464-12-0, Big data shows that 5464-12-0 is playing an increasingly important role.

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step L: 2, 6-Dichloro-4-[ 4-chloro-6- ( 4-fluorophenyl) thienof 2, 3-dJpyrimidin-5-ylJ-3, 5- dimethyl-phenol and 4-f 4-bromo-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-5-yl]-2, 6- dichloro-3, 5 -dimethyl-phenol (0234) To a stirred solution of 700 mg compound of Step K above (1.50 mmol, 1.0 eq.) in 15 mL dichloromethane, 3.0 mL boron tribromide (1M in dichloromethane) (3.0 mmol, 2.0 eq.) was added at 0 ¡ãC and the mixture was allowed to warm up to room temperature and it was stirred until no further conversion was observed. The mixture was quenched with saturated aqueous NH4C1 and extracted with dichloromethane. The combined organic phases were dried over Na2S04 and concentrated under reduced pressure. The residue was purified via flash chromatography using heptane and ethyl acetate as eluents to obtain 2,6-dichloro-4- [4-chloro-6-(4-fluorophenyl)thieno[2,3-(i]pyrimidin-5-yl]-3,5-dimethyl-phenol and 4-[4- bromo-6-(4-fluorophenyl)thieno[2,3- ]pyrimidin-5-yl]-2,6-dichloro-3,5-dimethyl-phenol as a 37:63 mixture of products. (0235) 1H NMR (400 MHz, DMSO-d6): 10.14 (br s, 1H), 9.01 (s, 1H), 7.40-7.23 (m, 4H), 1.95 (s, 6H) and 10.14 (br s, 1H), 8.93 (s, 1H), 7.40-7.23 (m, 4H), 1.93 (s, 6H) (0236) HRMS (M+H)+ = 452.9800 and 496.9287 Step M: 4-Chloro-5-[3,5-dichloro-2,6-dimethyl-4-[2-(4-methylpiperazin-l- yl) ethoxy] phenyl] -6- ( 4-fluorophenyl) thienof 2, 3-dJpyrimidine and 4-bromo-5-[ 3, 5- dichloro-2, 6-dimethyl-4-[ 2- ( 4-methylpiperazin-l-yl) ethoxy] phenyl] -6- ( 4- fluorophenyl) thienof 2, 3-d]pyrimidine (0238) 300 mg mixture of 2,6-dichloro-4-[4-chloro-6-(4-fluorophenyl)thieno[2,3-5464-12-0, Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; PACZAL, Attila; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; MARAGNO, Ana Leticia; GENESTE, Olivier; DEMARLES, Didier; BALINT, Balazs; SIPOS, Szabolcs; (81 pag.)WO2017/125224; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 5464-12-0

As the paragraph descriping shows that 5464-12-0 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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

4-Nitropyrazole (2.81 g, 13.88 mmol) and 1-hydroxyethyl-4-methylpiperazine (1.0 g, 6.94 mmol) were dissolved in anhydrous tetrahydrofuran (50 mL), and a solution of triphenylphosphine (3.64 g, 13.88 mmol) and diisopropyl azodicarboxylate (2.81 g, 13.88 mmol) in anhydrous tetrahydrofuran (6 mL) was added dropwise under nitrogen gas atmosphere. The reaction solution was stirred at room temperature for 1 hour, and then 1N hydrochloric acid (30 mL) and water (50 mL) was added. The aqueous phase was extracted with ethyl acetate (50 mL*2). The combined organic phase was dried over anhydrous sodium sulfate, filtered and the filtrate was concentrated. The residue was purified by silica gel column chromatography (dichloromethane: methanol=10:1) to give compound 22-c (1.0 g, yield 60.2percent). LC-MS (ESI): m/z=240.2[M+H]+., 5464-12-0

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.; XU, Zusheng; ZHANG, Nong; WANG, Tinghan; SUN, Qingrui; WANG, Yuguang; (90 pag.)US2018/208604; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 5464-12-0

5464-12-0, Big data shows that 5464-12-0 is playing an increasingly important role.

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

c. 5-tert-Butyl-2-{4-[2-(4-methyl-piperazin-1-yl)-ethoxy]-phenyl}-2H-pyrazol-3-ylamine (Intermediate 13c) To a solution of Intermediate 13b (1.15 g, 5.0 mmol), 2-(4-methyl-piperazin-1-yl)-ethanol (864 mg, 6.0 mmol), and triphenylphosphine (2.62 g, 10.0 mmol) in THF (10 mL), was added diisopropyl azodicarboxylate (2.0 g, 10.0 mmol) dropwise and stirred for 75 min. The mixture was diluted with diethyl ether (50 mL) and extracted with 10percent aqueous citric acid soln (2*). The combined aqueous layers were basified with solid potassium carbonate until pH=9. The aqueous layer was then extracted with ethyl acetate (3*). The combined ethyl acetate layers were washed with brine, dried (NaSO4) and evaporated in vacuo. Purification by FCC using 0-12percent [9:1 MeOH/880 ammonia] in DCM. The resulting product was crystallised (diethyl ether) to give the title compound (270 mg, 0.756 mmol, 15percent). LCMS (Method 1): Rt 2.31, 1.72 min, m/z 358/359 [MH+].

5464-12-0, Big data shows that 5464-12-0 is playing an increasingly important role.

Reference£º
Patent; Chiesi Farmaceutici S.p.A.; Van Niel, Monique Bodil; Ray, Nicholas Charles; Cridland, Andrew Peter; Hurley, Christopher; Alcaraz, Lilian; Panchal, Terry Aaron; Jennings, Andrew Stephen Robert; Armani, Elisabetta; US2013/150361; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 5464-12-0

As the paragraph descriping shows that 5464-12-0 is playing an increasingly important role.

5464-12-0,5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

300 mg mixture of 2,6-dichloro-4-[4-chloro-6-(4-fluorophenyl)thieno[2,3-Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; DEMARLES, Didier; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; SIPOS, Szabolcs; PACZAL, Attila; BALINT, Balazs; (74 pag.)WO2016/207225; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 5464-12-0

The synthetic route of 5464-12-0 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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

Example 7 N-((1S,2R)-2-{[(cyanomethyl)amino]carbonyl}cyclohexyl)-6-[2-(4-methylpiperazin-1-yl)ethoxy]-1H-indole-2-carboxamide To 85 mg (0.25 MM) 6-Hydroxy-1H-indole-2-carboxylic acid [2-(cyanomethyl-carbamoyl)-cyclohexyl]-amide in 5 ml dichloromethane at 0¡ã C. was added 144 mg (1 MM) 2-(4-Methyl-piperazin-1-yl)-ethanol, 262 mg (1 MM) triphenylphosphine and 131 mg (0.75 MM) DEAD. After several hours the mixture was allowed to warm to room temperature and stir overnight.The reaction mixture was purified directly on a preparative TLC plate and eluted with 10percent methanol/dichloromethane.The product was then partitioned between 1 M HCl and ethyl acetate, the aqueous layer was neutralized and extracted with ethyl acetate, dried over magnesium sulfate and stripped to give 18.9 mg 6-[2-(4-Methyl-piperazin-1-yl)-ethoxy]-1H-indole-2-carboxylic acid [2-(cyanomethyl-carbamoyl)-cyclohexyl]-amide. Similarly prepared were: N-((1S,2R)-2-{[(cyanomethyl)amino]carbonyl}cyclohexyl)-1-methyl-6-(2-morpholin-4-ylethoxy)-1H-indole-2-carboxamide using Mitsunobu coupling with 2-Morpholin-4-yl-ethanol. N-((1S,2R)-2-{[(cyanomethyl)amino]carbonyl}cyclohexyl)-6-(2-morpholin-4-ylethoxy)-1H-indole-2-carboxamide using Mitsunobu coupling with 2-morpholin-4-yl-ethanol., 5464-12-0

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bamberg, Joe Timothy; Gabriel, Tobias; Krauss, Nancy Elisabeth; Mirzadegan, Taraneh; Palmer, Wylie Solang; Smith, David Bernard; US2004/77646; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 5464-12-0

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Method 20 Synthesis of 3-[1-(4-iodophenyl)-1,2-dimethyl-propyl]-1-[2-(4-methylpiperazin-1-yl)ethyl]indole (Intermediate 26) To a solution of I-11 (150 mg, 0.39 mmol) in anhydrous DMF (4.5 mL) is added NaH (60percent dispersion in mineral oil) (18 mg, 0.46 mmol). The mixture is stirred at room temperature for 10 minutes and then methanesulfonyl chloride (0.032 mL, 0.42 mmol) is added and stifling continued for 18 h. The reaction is retreated with more methane sulfonyl chloride (0.03 mL) and NaH (60percent dispersion in mineral oil) (18 mg) and stirring is continued for another 2 h before quenching with water. The reaction is partitioned between saturated aqueous NaHCO3 and DCM. The combined organics are washed with brine, dried over anhydrous Na2SO4, and concentrated in vacuo to give I-25 (193 mg). To a solution of 1-(2-hydroxyethyl)-4-methylpiperazine (54 mg, 0.37 mmol) in toluene (3 mL) is added NaH (60percent dispersion in mineral oil) (18 mg, 0.45 mmol) and the suspension stirred at room temperature for 10 min. A solution of I-25 (175 mg, 0.37 mmol) in toluene (1.5 mL) is added and the reaction heated to 110¡ã C. for 3 h. A further 1 eq of 1-(2-hydroxyethyl)-4-methylpiperazine and 1.2 eq of NaH are added and heating continued for 3 h. The reaction is quenched by dropwise addition of water and extracted with DCM. The combined organics are washed with water and brine, and dried over anhydrous Na2SO4. The solvent is removed in vacuo and the crude material purified by flash chromatography (SiO2, 2percent MeOH in DCM) to give the title intermediate I-26 (52 mg) m/z 516.1 [M+H].

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BARTOLOZZI, Alessandra; CHEN, Zhidong; DINES, Jonathon Alan; LO, Ho Yin; LOKE, Pui Leng; OLAGUE, Alan; RIETHER, Doris; TYE, Heather; WU, Lifen; ZINDELL, Renee M.; US2013/196967; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics