Sep 2021 News Some tips on 1-Isopropylpiperazine

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4318-42-7

To a stirred solution of aryl bromide (0.76 mmol) and amine (0.86 mmol) in dioxane (4 mL), was added XantPhos (0.048 mmol), cesium carbonate (1 .66 mmol) and Pd2(dba)3 (0.024 mmol). The mixture was stirred for 16 h at 90 °C, diluted with water and extracted into DCM (20 mL). The organic layers were passed through a phase separator and concentrated and the crude mixture was purified by flash silica column chromatography. Following method I from compound 15c (250 mg, 0.76 mmol) and /so-propylpiperazine (125 muIota, 0.86 mmol). Purification using flash silica column chromatography (gradient elution /’-hex/EtOAc 0percent to 100percent) gave the title compound as a yellow oil (187 mg, 65percent). LCMS (ES+) 379 (M+H)+

4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; CHDI FOUNDATION, INC.; LUCKHURST, Christopher A.; HAUGHAN, Alan F.; BRECCIA, Perla; STOTT, Andrew J.; BURLI, Roland W.; HUGHES, Samantha J.; MUNOZ-SANJUAN, Ignacio; DOMINGUEZ, Celia; MANGETTE, John E.; WO2012/103008; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 1-Isopropylpiperazine

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

In N2 Under protection, three-necked flask with stirring and the funnel was added dropwise and THF150ml 100mmol isopropyl piperazine, in an ice bath, was slowly added dropwise through a dropping funnel 100mmol butyllithium dropwise after l to room temperature, the reaction after 1h.Under a 71/92 then cooled to 0°C 100mmol cyclohexyl trimethoxysilane, after the completion of the dropwise addition the reaction at room temperature for 8h, and finally through G4Funnel, the solid residue was washed repeatedly with tetrahydrofuran and filtered, the filtrate was collected.With a rotary evaporator to tetrahydrofuran solvent, vacuum distillation, collecting 136 ~ 139°C / 100pa fraction.Vacuum distillation, collecting 136 ~ 139°C/ 100pa distillate, heavy 5.3g, 98.2percent yield,

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference:
Patent; Institute of Chemistry Chinese Academy of Sciences; Li, Huayi; Chang, Hefei; Zhang, Liaoyun; Hu, Youliang; (19 pag.)CN102977133; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of 1-Isopropylpiperazine

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of compound 9 (100mg, 0.23mmol) in CH2Cl2 (10ml) was added oxalyl chloride (0.04ml, 0.50mmol) at 0°C, the reaction mixture was stirred at 0°C for 0.5h and then at room temperature for another 3h. The mixture was added to a solution of various amines (2.2 eq) and Et3N (0.1ml, 0.72mmol) and stirred for 12hat room temperature. After the reaction completed, the mixture was washed by water (3×20ml), brine (2×20ml), dried over anhydrous Na2SO4 and concentrated, the residue was purified by silica gel chromatography (CH2Cl2/MeOH 30/1v/v) to give corresponding diamides 10?26.

4318-42-7, 4318-42-7 1-Isopropylpiperazine 78013, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Mao, Shi-Wei; Chen, Huang; Yu, Li-Fang; Lv, Fang; Xing, Ya-Jing; Liu, Ting; Xie, Jia; Tang, Jie; Yi, Zhengfang; Yang, Fan; European Journal of Medicinal Chemistry; vol. 122; (2016); p. 574 – 583;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

26 Sep 2021 News Downstream synthetic route of 1-Isopropylpiperazine

As the paragraph descriping shows that 4318-42-7 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.,4318-42-7

A mixture of 2-(morpholine-4-carbonyl)-1-(2,2,2-trifluoro-ethyl)-1H-indole-5-carboxylic acid (100 mg, 0.28 mmol) and 1,1′-carbonyl-diimidazole (59 mg, 0.37 mmol) in tetrahydrofuran was stirred at room temperature overnight. 1-Isopropylpiperazine (72 mg, 0.56 mmol) was then added and the mixture was stirred for an additional 40 min. The volatiles were removed in vacuo and the residue was purified by flash chromatography on silica gel with dichloromethane:methanol:ammonia (95:5:0.25 v/v) as eluant, to give 90 mg (68percent) of the desired compound as an off-white solid.MS (TIC): 467.5 (M+H+)

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference:
Patent; Nettekoven, Matthias; Plancher, Jean-Marc; Richter, Hans; Roche, Olivier; Taylor, Sven; US2007/244125; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-Isopropylpiperazine

The synthetic route of 4318-42-7 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

To a mixture of 4-(bromoethyl)benzaldehyde (0.200 g, 1.0 mmol) and K2CO3 (0.277 g, 2.0 mmol) in DMF (5 mL) was added N-isopropylpiperazine (0.129 g, 1.0 mmol) and the reaction was stirred at room temperature for 5 hours, then concentrated in vacuo. The resulting mixture was diluted with H2O and extracted with EtOAc. The organics were washed with brine, dried over anhydrous Na2SO4, filtered, and concentrated in vacuo to afford 4-((4-Isopropylpiperazin-1-yl)methyl)benzaldehyde (0.240 g, 97percent), 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; RVX Therapeutics Inc.; McLure, Kevin G.; Young, Peter R.; US2013/281399; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

26 Sep 2021 News Downstream synthetic route of 1-Isopropylpiperazine

As the paragraph descriping shows that 4318-42-7 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.,4318-42-7

A mixture of 2-(morpholine-4-carbonyl)-1-(2,2,2-trifluoro-ethyl)-1H-indole-5-carboxylic acid (100 mg, 0.28 mmol) and 1,1′-carbonyl-diimidazole (59 mg, 0.37 mmol) in tetrahydrofuran was stirred at room temperature overnight. 1-Isopropylpiperazine (72 mg, 0.56 mmol) was then added and the mixture was stirred for an additional 40 min. The volatiles were removed in vacuo and the residue was purified by flash chromatography on silica gel with dichloromethane:methanol:ammonia (95:5:0.25 v/v) as eluant, to give 90 mg (68percent) of the desired compound as an off-white solid.MS (TIC): 467.5 (M+H+)

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference:
Patent; Nettekoven, Matthias; Plancher, Jean-Marc; Richter, Hans; Roche, Olivier; Taylor, Sven; US2007/244125; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-Isopropylpiperazine

The synthetic route of 4318-42-7 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

To a mixture of 4-(bromoethyl)benzaldehyde (0.200 g, 1.0 mmol) and K2CO3 (0.277 g, 2.0 mmol) in DMF (5 mL) was added N-isopropylpiperazine (0.129 g, 1.0 mmol) and the reaction was stirred at room temperature for 5 hours, then concentrated in vacuo. The resulting mixture was diluted with H2O and extracted with EtOAc. The organics were washed with brine, dried over anhydrous Na2SO4, filtered, and concentrated in vacuo to afford 4-((4-Isopropylpiperazin-1-yl)methyl)benzaldehyde (0.240 g, 97percent), 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; RVX Therapeutics Inc.; McLure, Kevin G.; Young, Peter R.; US2013/281399; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24 Sep 2021 News Brief introduction of 1-Isopropylpiperazine

The synthetic route of 4318-42-7 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Step I: (4-bromophenyl)-(4-isopropylpiperazin-1-yl)methanone (1-13) To a stirred solution of 4-bromobenzoic acid 1-12 at 0° C. (2 g, 9.94 mmol) in a mixture of MeCN:DMF (4:1, 20 mL) were added HATU (4.53 g, 11.93 mmol) and 1-isopropylpiperazine (1.91 g, 14.92 mmol). The reaction mixture was allowed to stir for 30 minutes, and then diisopropylethylamine (3.85 g, 5.2 mL, 29.84 mmol) was added thereto. The resulting reaction mixture was stirred for 16 hours at room temperature. After completion of reaction, the reaction mixture was diluted with water and extracted with ethyl acetate (25 mL*3). The combined organic layer was washed with water and brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The obtained residue was purified by silica gel (60-120 mesh size) column chromatography using 0-5percent methanol in dichloromethane as eluent to give the desired product 1-13 (3.0 g, 97percent) as brown solid; LCMS: m/z 312.00 (M++1)., 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; BHOSALE, Sandeep; NAIK, Keshav; SALUNKHE, Videsh; MUNOT, Yogesh; BHUNIYA, Debnath; (132 pag.)US2017/8885; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24 Sep 2021 News Brief introduction of 1-Isopropylpiperazine

The synthetic route of 4318-42-7 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.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

Step I: (4-bromophenyl)-(4-isopropylpiperazin-1-yl)methanone (1-13) To a stirred solution of 4-bromobenzoic acid 1-12 at 0° C. (2 g, 9.94 mmol) in a mixture of MeCN:DMF (4:1, 20 mL) were added HATU (4.53 g, 11.93 mmol) and 1-isopropylpiperazine (1.91 g, 14.92 mmol). The reaction mixture was allowed to stir for 30 minutes, and then diisopropylethylamine (3.85 g, 5.2 mL, 29.84 mmol) was added thereto. The resulting reaction mixture was stirred for 16 hours at room temperature. After completion of reaction, the reaction mixture was diluted with water and extracted with ethyl acetate (25 mL*3). The combined organic layer was washed with water and brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The obtained residue was purified by silica gel (60-120 mesh size) column chromatography using 0-5percent methanol in dichloromethane as eluent to give the desired product 1-13 (3.0 g, 97percent) as brown solid; LCMS: m/z 312.00 (M++1)., 4318-42-7

The synthetic route of 4318-42-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; KOUL, Summon; KURHADE, Suresh; BHOSALE, Sandeep; NAIK, Keshav; SALUNKHE, Videsh; MUNOT, Yogesh; BHUNIYA, Debnath; (132 pag.)US2017/8885; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

23 Sep 2021 News Downstream synthetic route of 1-Isopropylpiperazine

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

4318-42-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4318-42-7,1-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of the intermediates 3a-3e (5 mmol) and corresponding secondary amine 4a-4g (5.5 mmol) was added in CH3CN (20 ml) at the presence of anhydrous K2CO3 (6 mmol). The mixture was heated at 65 °C for 6-10 h. The solvent was evaporated in vacuo. The residue was dissolved in CH2Cl2 (25 mL), washed with water (20 mL × 3), and the combined organic phases were washed with saturated aqueous NaCl (30 mL), dried over sodium sulfate, and filtered. The solvent was evaporated under reduced pressure. The residue was purified on a silica gel chromatography using mixtures of petroleum/acetone as eluent to get the target products TM-1~TM-28.

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference:
Article; Sang, Zhipei; Wang, Keren; Wang, Huifang; Yu, Lintao; Wang, Huijuan; Ma, Qianwen; Ye, Mengyao; Han, Xue; Liu, Wenmin; Bioorganic and Medicinal Chemistry Letters; vol. 27; 22; (2017); p. 5053 – 5059;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics