24 Sep 2021 News Simple exploration of 1-(Methylsulfonyl)piperazine hydrochloride

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 0.20 mL of 2 N NaOH was added to a solution of 31 (46 mg, 0.10 mmol), prepared in a similar manner as described for 10c, in 2 mL of THF. The resulting medium was refluxed for 5 h. Additional 0.20 mL of 2 N NaOH was added to the reaction solution. Then the reaction was stirred for another 3 h under reflux. After concentration, the remaining residue was acidified to pH 2-3 by adding 1 N HCl and extracted with EA. The organic layer was dried over anhydrous Na2SO4 and concentrated under vacuum to give a crude acid (43 mg). The crude acid was dissolved in 2 mL of DMF and the solution was cooled in an ice bath. To the solution was successively added HATU (0.10 mmol), DIPEA (36 muL, 0.20 mmol) and dimethylamine hydrochloride (10 mg, 0.12 mmol). The resulting medium was stirred at room temperature for 1 h and quenched with 2 mL of saturated NaHCO3. The mixture was extracted with 50 mL of EA. The organic layer was washed with water (2 × 10 mL), brine, dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was purified by flash column chromatography (0-3% MeOH/EA gradient) to afford compound 10g in 48% yield., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Zhang, Dengyou; Zhang, Xiaowei; Ai, Jing; Zhai, Yun; Liang, Zhongjie; Wang, Ying; Chen, Yi; Li, Chunpu; Zhao, Fei; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6804 – 6820;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24 Sep 2021 News Simple exploration of 1-(Methylsulfonyl)piperazine hydrochloride

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 0.20 mL of 2 N NaOH was added to a solution of 31 (46 mg, 0.10 mmol), prepared in a similar manner as described for 10c, in 2 mL of THF. The resulting medium was refluxed for 5 h. Additional 0.20 mL of 2 N NaOH was added to the reaction solution. Then the reaction was stirred for another 3 h under reflux. After concentration, the remaining residue was acidified to pH 2-3 by adding 1 N HCl and extracted with EA. The organic layer was dried over anhydrous Na2SO4 and concentrated under vacuum to give a crude acid (43 mg). The crude acid was dissolved in 2 mL of DMF and the solution was cooled in an ice bath. To the solution was successively added HATU (0.10 mmol), DIPEA (36 muL, 0.20 mmol) and dimethylamine hydrochloride (10 mg, 0.12 mmol). The resulting medium was stirred at room temperature for 1 h and quenched with 2 mL of saturated NaHCO3. The mixture was extracted with 50 mL of EA. The organic layer was washed with water (2 × 10 mL), brine, dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was purified by flash column chromatography (0-3% MeOH/EA gradient) to afford compound 10g in 48% yield., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Zhang, Dengyou; Zhang, Xiaowei; Ai, Jing; Zhai, Yun; Liang, Zhongjie; Wang, Ying; Chen, Yi; Li, Chunpu; Zhao, Fei; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6804 – 6820;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-(Methylsulfonyl)piperazine hydrochloride

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(5-Chloro-2-methyl-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (100 mg) is added to a mixture of 1-(methylsulfonyl)piperazine hydrochloride (70 mg), Pd2(dba)3 (65 mg), Xantphos (123 mg), and potassium tert-butylate (75 mg) in toluene (4 mL) under an argon atmosphere. The reaction mixture is stirred in an oil bath at 105 C. over night. After cooling to room temperature water is added and the mixture is extracted with ethyl acetate. The combined extracts are concentrated in vacuo and the residue is chromatographed on silica gel (cyclohexane/ethyl acetate 50:50?0:100) to give the title compound. LC (method 1): tR=1.03 min; Mass spectrum (ESI+): m/z=481 [M+H]+., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2012/322784; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 1-(Methylsulfonyl)piperazine hydrochloride

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(5-Chloro-2-methyl-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (100 mg) is added to a mixture of 1-(methylsulfonyl)piperazine hydrochloride (70 mg), Pd2(dba)3 (65 mg), Xantphos (123 mg), and potassium tert-butylate (75 mg) in toluene (4 mL) under an argon atmosphere. The reaction mixture is stirred in an oil bath at 105 C. over night. After cooling to room temperature water is added and the mixture is extracted with ethyl acetate. The combined extracts are concentrated in vacuo and the residue is chromatographed on silica gel (cyclohexane/ethyl acetate 50:50?0:100) to give the title compound. LC (method 1): tR=1.03 min; Mass spectrum (ESI+): m/z=481 [M+H]+., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2012/322784; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 161357-89-7

161357-89-7, As the paragraph descriping shows that 161357-89-7 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

To a suspension of Example 1285A (0.091 g, 0.21 1 mmol) and l-(methylsulfonyl)piperazine hydrochloride (0.057 g, 0.284 mmol) in 1,4-dioxane (1 mL), N-ethyl-N-isopropylpropan-2-amine (0.2 mL, 1.145 mmol) was added. The mixture was stirred for 72 hours at room temperature. The solvent was removed and the product was purified by flash chromatography on silica gel (AnaLogix IntelliFlash) eluting with a gradient of 0-50% ethyl acetate in heptanes to afford the title compound. MS (ESI+) m/z: 40.3.8 (M+H)+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference:
Patent; ABBVIE INC.; ABBVIE PHARMACEUTICAL TRADING (SHANGHAI) CO., LTD.; TONG, Yunsong; BRUNCKO, Milan; CLARK, Richard F.; CURTIN, Michael L.; FLORJANCIC, Alan S.; FREY, Robin R.; GONG, Jianchun; HANSEN, Todd M.; JI, Zhiqin; LAI, Chunqiu; MASTRACCHIO, Anthony; MICHAELIDES, Michael; MIYASHIRO, Juliem; RISI, Roberto M.; SONG, Xiaohong; TAO, Zhi-fu; WOODS, Keith W.; ZHU, Guidong; PENNING, Thomas; SOUERS, Andrew; GOSWAMI, Rajeev; IQUTURI, Omprakash Reddy; DABBEERU, Madhu Babu; WO2014/139328; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 161357-89-7

161357-89-7, As the paragraph descriping shows that 161357-89-7 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

To a suspension of Example 1285A (0.091 g, 0.21 1 mmol) and l-(methylsulfonyl)piperazine hydrochloride (0.057 g, 0.284 mmol) in 1,4-dioxane (1 mL), N-ethyl-N-isopropylpropan-2-amine (0.2 mL, 1.145 mmol) was added. The mixture was stirred for 72 hours at room temperature. The solvent was removed and the product was purified by flash chromatography on silica gel (AnaLogix IntelliFlash) eluting with a gradient of 0-50% ethyl acetate in heptanes to afford the title compound. MS (ESI+) m/z: 40.3.8 (M+H)+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference:
Patent; ABBVIE INC.; ABBVIE PHARMACEUTICAL TRADING (SHANGHAI) CO., LTD.; TONG, Yunsong; BRUNCKO, Milan; CLARK, Richard F.; CURTIN, Michael L.; FLORJANCIC, Alan S.; FREY, Robin R.; GONG, Jianchun; HANSEN, Todd M.; JI, Zhiqin; LAI, Chunqiu; MASTRACCHIO, Anthony; MICHAELIDES, Michael; MIYASHIRO, Juliem; RISI, Roberto M.; SONG, Xiaohong; TAO, Zhi-fu; WOODS, Keith W.; ZHU, Guidong; PENNING, Thomas; SOUERS, Andrew; GOSWAMI, Rajeev; IQUTURI, Omprakash Reddy; DABBEERU, Madhu Babu; WO2014/139328; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 161357-89-7

161357-89-7, As the paragraph descriping shows that 161357-89-7 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

To a suspension of Example 1285A (0.091 g, 0.21 1 mmol) and l-(methylsulfonyl)piperazine hydrochloride (0.057 g, 0.284 mmol) in 1,4-dioxane (1 mL), N-ethyl-N-isopropylpropan-2-amine (0.2 mL, 1.145 mmol) was added. The mixture was stirred for 72 hours at room temperature. The solvent was removed and the product was purified by flash chromatography on silica gel (AnaLogix IntelliFlash) eluting with a gradient of 0-50% ethyl acetate in heptanes to afford the title compound. MS (ESI+) m/z: 40.3.8 (M+H)+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference:
Patent; ABBVIE INC.; ABBVIE PHARMACEUTICAL TRADING (SHANGHAI) CO., LTD.; TONG, Yunsong; BRUNCKO, Milan; CLARK, Richard F.; CURTIN, Michael L.; FLORJANCIC, Alan S.; FREY, Robin R.; GONG, Jianchun; HANSEN, Todd M.; JI, Zhiqin; LAI, Chunqiu; MASTRACCHIO, Anthony; MICHAELIDES, Michael; MIYASHIRO, Juliem; RISI, Roberto M.; SONG, Xiaohong; TAO, Zhi-fu; WOODS, Keith W.; ZHU, Guidong; PENNING, Thomas; SOUERS, Andrew; GOSWAMI, Rajeev; IQUTURI, Omprakash Reddy; DABBEERU, Madhu Babu; WO2014/139328; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 0.20 mL of 2 N NaOH was added to a solution of 31 (46 mg, 0.10 mmol), prepared in a similar manner as described for 10c, in 2 mL of THF. The resulting medium was refluxed for 5 h. Additional 0.20 mL of 2 N NaOH was added to the reaction solution. Then the reaction was stirred for another 3 h under reflux. After concentration, the remaining residue was acidified to pH 2-3 by adding 1 N HCl and extracted with EA. The organic layer was dried over anhydrous Na2SO4 and concentrated under vacuum to give a crude acid (43 mg). The crude acid was dissolved in 2 mL of DMF and the solution was cooled in an ice bath. To the solution was successively added HATU (0.10 mmol), DIPEA (36 muL, 0.20 mmol) and dimethylamine hydrochloride (10 mg, 0.12 mmol). The resulting medium was stirred at room temperature for 1 h and quenched with 2 mL of saturated NaHCO3. The mixture was extracted with 50 mL of EA. The organic layer was washed with water (2 × 10 mL), brine, dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was purified by flash column chromatography (0-3% MeOH/EA gradient) to afford compound 10g in 48% yield., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Zhang, Dengyou; Zhang, Xiaowei; Ai, Jing; Zhai, Yun; Liang, Zhongjie; Wang, Ying; Chen, Yi; Li, Chunpu; Zhao, Fei; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6804 – 6820;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 0.20 mL of 2 N NaOH was added to a solution of 31 (46 mg, 0.10 mmol), prepared in a similar manner as described for 10c, in 2 mL of THF. The resulting medium was refluxed for 5 h. Additional 0.20 mL of 2 N NaOH was added to the reaction solution. Then the reaction was stirred for another 3 h under reflux. After concentration, the remaining residue was acidified to pH 2-3 by adding 1 N HCl and extracted with EA. The organic layer was dried over anhydrous Na2SO4 and concentrated under vacuum to give a crude acid (43 mg). The crude acid was dissolved in 2 mL of DMF and the solution was cooled in an ice bath. To the solution was successively added HATU (0.10 mmol), DIPEA (36 muL, 0.20 mmol) and dimethylamine hydrochloride (10 mg, 0.12 mmol). The resulting medium was stirred at room temperature for 1 h and quenched with 2 mL of saturated NaHCO3. The mixture was extracted with 50 mL of EA. The organic layer was washed with water (2 × 10 mL), brine, dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was purified by flash column chromatography (0-3% MeOH/EA gradient) to afford compound 10g in 48% yield., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Zhang, Dengyou; Zhang, Xiaowei; Ai, Jing; Zhai, Yun; Liang, Zhongjie; Wang, Ying; Chen, Yi; Li, Chunpu; Zhao, Fei; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6804 – 6820;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Analyzing the synthesis route of 161357-89-7

The synthetic route of 161357-89-7 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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

Example 2 6-(4-Methanesulfonyl-piperazin-l-vI)-2-morphoHn-4-yl-[4,5’lbipyriinidinyl-2′-ylamine (4) A mixture of Intermediate Al (198mg), Intermediate G (230mg) and potassium carbonate (293mg) was stirred in acetonitrile (10ml) at room temperature. After 24 hours the reaction mixture was diluted with ethyl acetate, washed with water, dried (MgSO4) and the solvent removed in vacuo. The residue was recrystallised from ethyl acetate/hexane to yield 4-[4-chloro-6-(4-methanesulfonyl-piperazin-l-yl)-yrimidin-2- yl]-morpholine (206mg). Reaction of 4-[4-chloro-6-(4-methanesulfonyl-piperazin- 1 -yl)-yrimidin-2-yl]- morpholine with 2-aminopyrimidine-5-boronic acid, pinacol ester using standard Suzuki conditions yielded the desired title compound. IH NMR (400MHz, CDCl3) 2.80 (3H,s), 3.28-3.24 (4H,m), 3.82-3.75 (12H,m), 5.20 (2H,s,br.), 6.16 (lH,s), 8.91 (2H,s)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; WO2009/66084; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics