Month: August 2020

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 119 Preparation of rac-6-chloro-3-(3-chloro-benzyl)-3-[4-(4-trifluoromethyl-phenyl)-piperazin-yl]-1,3-dihydro-indol-2-one The mixture of rac-3-bromo-6-chloro-3-(3-chloro-benzyl)-1,3-dihydro-indol-2-one (100 mg, 0.270 mmol), 1-(4-trifluoromethyl-phenyl)-piperazine (75 mg, 0.324 mmol) and DIPEA (42 mg, 0.324 mmol) In acetonitrile (3 mL) was stirred at room temperature for overnight. The crude was concentrated and the residue was purified with preparative HPLC to give 76 mg of rac-6-chloro-3-(3-chloro-benzyl)-3-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-1,3-dihydro-indol-2-one as a white solid. MS: 520 (M+H)+. H1-NMR (400 MHz, CDCl3) delta 7.584 (s, 1H), 7.493 (d, 2H), 7.240 (d, 1H), 7.081 (t, 2H), 7.011 (t, 1H), 6.908 (d, 3H), 6.766 (d, 1H), 6.684 (d, 1H), 3.431 (d, 1H), 3.329-3.206 (m, 5H), 2.947 (t, 4H).

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chen, Li; Yang, Song; Zhang, Jing; Zhang, Zhuming; US2008/81810; (2008); A1;,
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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 4-methyl-2-piperazinone (26.16 mg, 0.23 mmol) in N,N-dimethylformamide (3mL) was added sodium hydride (18.34 mg, 60% purity, 0.46 mmol) at 0 C. The reaction was stirred for 20 minutes at 0 C. 2-[[8-Chloro-6-(chloromethyl)-7-fluoro-3-isoquinolyl]amino]-6-isopropyl-5,8-dihydro-4H-pyrazolo[1,5-d][1,4]diazepin-7-one (50 mg, 0.11 mmol) was added and stirred at 25 C. for 1 hour. The reaction was quenched with water, extracted with ethyl acetate, dried with anhydrous sodium sulfate. After filtration, the filtrate was concentrated under vacuum. The residue was purified by reverse phase chromatography ( acetonitrile 0-40/0.1% sodium bicarbonate in water) to afford 2-[[8-chloro-7-fluoro-6-[(4-methyl-2-oxo-piperazin-1-yl)methyl]-3-isoquinolyl]amino]-6-isopropyl-5,8-dihydro-4H-pyrazolo[1,5-d][1,4]diazepin-7-one (9 mg, 0.018 mmol) as a yellow solid. LCMS (ESI) [M+H]+=514.

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

Reference£º
Patent; Genentech, Inc.; Chan, Bryan; Drobnick, Joy; Gazzard, Lewis; Heffron, Timothy; Liang, Jun; Malhotra, Sushant; Mendonca, Rohan; Rajapaksa, Naomi; Stivala, Craig; Tellis, John; Wang, Weiru; Wei, BinQing; Zhou, Aihe; Cartwright, Matthew W.; Lainchbury, Michael; Gancia, Emanuela; Seward, Eileen; Madin, Andrew; Favor, David; Fong, Kin Chiu; Hu, Yonghan; Good, Andrew; US2018/282282; (2018); A1;,
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Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Piperazin-1-yl-ethanol (8.2g, 63.1 mmol) was added to a solution of 4,6-dichloro-2- methylpyrimidine (5.2g, 31.9 mmol) in dichloromethane (80 ml) at rt. The mixture was stirred for two hours and triethylamine (0.9 ml) was added. The mixture was stirred at rt for 20h. The resultant solid was filtered. The cake was washed with dichloromethane (20 ml). The filtrate was concentrated to give an oil. This oil was dried under high vacuum for 20h to give a solid. This solid was stirred with heptane (50 ml) at rt for 5h. Filtration gave 7C (8.13g) as a white solid

The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2005/77945; (2005); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

EXAMPLE 4 In a reaction vessel, a mixture of 11-piperazinyldibenzo[b,f][1,4]-thiazepine (10 Kg), 2-(2-chloroethoxy)ethanol (6.3 kg), 5.4 kg triethyl amine and 0.2 kg sodium iodide was heated under mixing to about 85 C. The reaction mixture was maintained at about 80 to 85 C. for about 3 hours. Starting 11-piperazinyldibenzo[b,f][1,4]-thiazepine was about 0.1% by HPLC. Maintained for another 2 hours till 11-piperazinyldibenzo[b,f][1,4]-thiazepine was about less than 0.05% by HPLC analysis. The reaction mass was cooled to about 30 C. and added 40 litres of water and aqueous layer extracted with methylene chloride. The organic layer was washed with water and concentrated under reduced pressure. The oily residue was so obtained suspended in 100 litres of ethanol (commercial) and 3.3 kg fumaric acid was added. The mixture was stirred for about 6 hours and cooled to about 15 C. The precipitated quetiapine hemi-fumarate salt was filtered and dried to give 12 Kg (yield 80% and purity 99.8% by HPLC analysis).

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Patent; Kumar, Ashok; Singh, Dharmendra; Patil, Swapnali Hemant; Mahale, Ganesh Devidas; Sawant, Uttamrao Arjunrao; Jadhav, Balasaheb Ganpat; Rana, Ragneshkumar; US2007/293471; (2007); A1;,
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Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (2 R,5R)-5-hydroxymethyl-2-methyl-piperazine- 1 -carboxylic acid tert-butyl ester (3.48 g, 15.1 mmol), benzaldehyde (1.76 g, 16.6 mmol), sodium triacetoxyborohydride (3.84 g, 18.1 mmol) and 1 ,2-dichloroethane (30 mL) was stirred at 20 c for 18 h, then partitionedbetween saturated aqueous NaHCO3 (150 mL) and DCM (3 x 50 mL). Combined organic extracts were dried (Na2SO4) then evaporated in vacuo to give an oil. Chromatography (Si02, 0 – 30% EtOAc in petrol) gave the title compound (4.588 g, 74%) as a colourless solid. MS: [M+H] = 321.

As the paragraph descriping shows that 1403898-64-5 is playing an increasingly important role.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; MILLEMAGGI, Alessia; HOWARD, Steven; SAXTY, Gordon; HEIGHTMAN, Thomas Daniel; WO2014/60768; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Example 19Synthesis of provide 4-(S-C6.7-dimethoxycinnolin-4-yl^pyridin-2-gammalVl methylpiperazin-2-one[00205] In a microwave vial was placed 4-(6-fluoropyridin-3-yl)-6,7- dimethoxycinnoline (0.0652 g, 0.229 mmol) in 2 ml DMSO. 1 -Methylpiperazin-2-one hydrochloride (0.3626 g, 2.29 mmol) and potassium carbonate (0.147 ml, 2.40 mmol) was added and the temperature was brought to 90 0C to stir overnight. The reaction solution was allowed to cool to room temperature. The solution was moved to a separatory funnel and deionized water and ethyl acetate were added. The aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with water, brine, dried with MgSO4, filtered, and concentrated. The crude product was adsorbed onto a plug of silica gel and chromatographed through a Biotage pre-packed silica gel column (25M), eluting with a gradient of 1% to 5% MeOH in CH2Ch, to provide 4-(5-(6,7-dimethoxycinnolin-4-yl)- pyridin-2-yl)-l -methylpiperazin-2-one (0.0413 g).

The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AMGEN INC.; MEMORY PHARMACEUTICALS CORPORTION; WO2007/98169; (2007); A1;,
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Piperazines – an overview | ScienceDirect Topics

59878-57-8, 1-(Cyclopropylcarbonyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 200 mL reaction flask, ethyl 2-(2-(4-fluoro-3-carboxyphenyl)acetyl)benzoate (Formula I, R=Et) (5 g, 15.14 mmol)And acetonitrile (100mL), after the addition is completed, the system is stirred until the system is dissolved.Additional 1-cyclopropyl-formylpiperazine (2.57 g, 16.67 mmol) and EDCI (3.50 g, 18.31 mmol) were added.Subsequently, DIPEA (2.40 g, 18.5 mmol) was added dropwise to the system, and the reaction temperature was controlled to be no higher than 35 C during the dropwise addition.After the addition was completed, the system was kept at 30 ¡À 5 C overnight. After the reaction is completed, the system removes the solvent under high vacuum.Ethyl acetate (150 mL) and H 2O (150 mL) were directly added to the residue, and the mixture was stirred, and the organic phase was separated.The aqueous phase was extracted twice with ethyl acetate (2¡Á100 mL), and the organic phase was combined.The residue was purified by column chromatography (ethyl acetate / n-heptane = 5 / 1-2 / 1) to give a pale yellow solid (formula IV, R = Et) (6.02g, 85.2%).

The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Jiangsu Jun Ruo Pharmaceutical Co., Ltd.; Haimen Baikang Bio-pharmaceutical Co., Ltd.; Nanjing Jun Ruo Bio-pharmaceutical Institute Co., Ltd.; Wei Wanguo; Xu Zichen; Fang Xianjie; Zhu Xinlei; Liu Rufeng; Yi Mingyue; Zhou Chenglong; Liu Jie; Song Yaojie; (7 pag.)CN110078671; (2019); A;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

Step 2. 4-(4-Amino-phenyl)-piperazine-1-carboxylic acid tert-butyl ester [0166] A mixture of 4- (4-NITRO-PHENYL)-PIPERAZINE-1-CARBOXYLIC acid TERT-BUTYL ester (11) (18. 9 MMOL), 10% palladium-on-carbon (600mg), ethanol (100 mL), and ethyl acetate (100 mL) is hydrogenated at room temperature and 40 psi for 2 hrs. The mixture is filtered through celite, washing with ethyl acetate (2 x 100 mL), and concentrated in vacuo to give 4- (4-AMINO-PHENYL)-PIPERAZINE-1-CARBOXYLIC acid tert-butyl ester (12) as a brown oil.

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CELLULAR GENOMICS, INC.; WO2005/14599; (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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The 4- chloropyrimidine SG2-022 was prepared using the previously reported method.1 A solution of 2,4-dichloro-5-trifluoromethylpyrimidine (120 mg, 0.550 mmol) in i-BuOH/DCM (1:1, 4 mL) was cooled to 0 C. Zinc chloride (1 M in diethyl ether, 0.633 mL, 0.633 mmol) was added dropwise over 10 minutes at 0 C and the solution stirred at the same temperature for 30 minutes. A solution of iPatent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas J.; LAWRENCE, Harshani R.; (293 pag.)WO2017/66428; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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