7 Sep 2021 News Brief introduction of 1-Methanesulfonylpiperazine

The synthetic route of 55276-43-2 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.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

Step 1 A solution of 4-fluoro-2-nitrobenzaldehyde (0.20 g, 1.2 mmol) in DMSO (3.5 mL) was added with 1-methanesulfonylpiperazine (0.71 g, 3.5 mmol), followed by stirring at 100 C for 1 hour. The reaction mixture was added with water and the organic layer was extractd with hexane/ethyl acetate (4/1) to remove impurities. The aqueous layer was extracted with ethyl acetate and the obtained organic layer was washed with water and saturated brine, dried over anhydrous magnesium sulfate and evaporated under reduced pressure to obtain 4-(4-methanesulfonylpiperazin-1-yl)-2-nitrobenzaldehyde (0.36 g, 96%). 1H-NMR (270 MHz, DMSO-d6) delta 2.92 (s, 3H), 3.23 (t, J = 5.1 Hz, 1H), 3.63 (t, J = 5.1 Hz, 1H), 7.31 (dt, J = 8.9 Hz, 2.4 Hz, 1H), 7.49 (d, J = 2.4 Hz, 1H), 7.85 (d, J = 8.9 Hz, 1H), 9.86 (s, 1H). APCI-MS (m/z); 314 [M+H]+, 55276-43-2

The synthetic route of 55276-43-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; KYOWA HAKKO KOGYO CO., LTD.; EP1847532; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3 Sep 2021 News Some tips on 1-Methanesulfonylpiperazine

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

55276-43-2,55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(S)-Epichlorohydrin (48.0 mL, 0.612 mol) was added to a stirred solution of piperazine N-methylsulfonamide (87.3 g, 0.532 mol) in ethanol (1.33 L) at room temperature. The reaction mixture was stirred for 18 h and the white solid precipitate which formed was collected by filtration and washed with ethanol to provide the title intermediate (107.7 g) as a white solid which was used without further purification. (m/z): [M+H]+ calcd for C8H17ClN2O3S, 257.07; found, 257.2. 1H-NMR (DMSO): delta(ppm) 5.09 (d, 1H), 3.84 (m, 1H), 3.65 (dd, 1H), 3.55 (dd, 1H), 3.09 (m, 4H), 2.37 (dd, 1H), 2.86 (s, 3H), 2.50-2.58 (m, 4H), 2.45 (dd, 1H).

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Theravance, Inc.; US2006/276482; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

3 Sep 2021 News Some tips on 1-Methanesulfonylpiperazine

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

55276-43-2,55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(S)-Epichlorohydrin (48.0 mL, 0.612 mol) was added to a stirred solution of piperazine N-methylsulfonamide (87.3 g, 0.532 mol) in ethanol (1.33 L) at room temperature. The reaction mixture was stirred for 18 h and the white solid precipitate which formed was collected by filtration and washed with ethanol to provide the title intermediate (107.7 g) as a white solid which was used without further purification. (m/z): [M+H]+ calcd for C8H17ClN2O3S, 257.07; found, 257.2. 1H-NMR (DMSO): delta(ppm) 5.09 (d, 1H), 3.84 (m, 1H), 3.65 (dd, 1H), 3.55 (dd, 1H), 3.09 (m, 4H), 2.37 (dd, 1H), 2.86 (s, 3H), 2.50-2.58 (m, 4H), 2.45 (dd, 1H).

55276-43-2 1-Methanesulfonylpiperazine 709161, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Theravance, Inc.; US2006/276482; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-Methanesulfonylpiperazine

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference:
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-Methanesulfonylpiperazine

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference:
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-Methanesulfonylpiperazine

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference:
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about 1-Methanesulfonylpiperazine

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

55276-43-2, 1-Methanesulfonylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Bromo-1-chlorophthalazine (18 mg, 74 umol) and 1-(methylsulfonyl)piperazine (91 mg, 554 mumol) were dissolved in dichloromethane/methanol when the reaction mixture was concentrated by evaporation under a nitrogen line. The concentrate was heated to 120 C. for 6 h to give the title compound. MS (ES+): 373 (M+H)+., 55276-43-2

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference:
Patent; Amgen Inc.; US2006/199817; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-Methanesulfonylpiperazine

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference:
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 1-Methanesulfonylpiperazine

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

55276-43-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred suspension of N-methanesulfonylpiperazine (1.0 g, 6.1 mmol) in isopropanol (15 mL) at rt was added trimethylsilylisocyanate (1.4 mL, 11 mmol) and the resulting suspension stirred overnight before the precipitate was filtered and dried to give 4-methanesulfonyl-piperazine-1-carboxylic acid amide (1.35 g, quant.) as a solid; 1H-NMR (300 MHz, d6-DMSO) 6.10 (2H, s), 3.37-3.40 (4H, m), 3.03-3.06 (4H, m), 2.90 (3H, s).

As the paragraph descriping shows that 55276-43-2 is playing an increasingly important role.

Reference:
Patent; Schering Aktiengesellschaft; EP1657241; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of 55276-43-2

The synthetic route of 55276-43-2 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.55276-43-2,1-Methanesulfonylpiperazine,as a common compound, the synthetic route is as follows.,55276-43-2

Example 17 (2R,3R)-2-(2,4-Difluorophenyl)-3-[4-(methanesulphonyl)piperazin-1-yl]-1-(1H-1,2,4-triazol-1-yl)butan-2-ol: The epoxide IV (300 mg, 1.19 mmol) and LiClO4 (235 mg, 1.43 mmol) were dissolved in 12 mL dry acetonitrile and 1-methanesulfonylpiperazine (190 mg, 1.79 mmol) was added. The mixture was heated to reflux for 4 days, cooled and the solvent evaporated. The residue was dissolved in dichloromethane and then washed with water and brine. The solution was dried over Na2 SO4 and the solvent evaporated. The crude reaction products were eluted through a silica gel column using 3% MeOH/97% EtOAc as eluent to give the title compound (180 mg, 36%) as a colorless solid. m.p.: 83-85 C. 1 H NMR (CDCl3) delta: 0.91 (d, J=6.4 Hz, 3H), 2.56-2.61 (m, 2H), 2.80 (s, 3H), 3.02-3.18 (m, 3H), 3.22-3.30 (m, 4H), 4.89 (s, 2H), 4.93 (s, 1H), 6.66-6.79 (m, 2H), 7.35-7.48 (m, 1H), 7.79 (s, 1H), 7.88 (s, 1H). FAB-MS: 415.9 (MH+), C17 H23 F2 N5 O3 S 415.45

The synthetic route of 55276-43-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Synphar Laboratories, Inc.; Taiho Pharmaceuticals Co., Ltd.; US6153616; (2000); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics