29 Sep 2021 News Some tips on 2-Methylpiperazine

109-07-9 2-Methylpiperazine 66057, 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

3.49 g (17.0 MMOL) 4-CHLOROBENZYLBROMIDE was added dropwise to a mixture of 2.04 G (20.4 MMOL) 2-Methyl piperazine and 2.40 ml (17 MMOL) triethylamine in 60 ml DMF at room temperature. The reaction mixture was stirred for 16 hours at room temperature, the poured onto aq. sodium bicarbonate solution and extracted with ethylacetate. Purification of the crude product by flash chromatography gave 2.26 g (10.1 mmol, 59 %) of 1- (4-chloro- benzyl)-3-methyl-piperazine as colorless oil. 1H-NMR (400 MHz, DMSO-d6): 0.91 (d, 3H), 1.56 (t, 1H), 1.90 (TD, 1H), 1.91-2. 03 (m, 1 H), 2.56-2. 74, m, 4H), 2.79 (dt, 1 H), 3.40 and 3.44 (AB-Sys., 2H), 7.33 (d, 2H), 7.40 (d, 2H). MS (ESI+) : 225 [M+H] +, 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/37796; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 2-Methylpiperazine

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 26 6-(3-methylpiperazinyl)-1-triisopropylsilyl-indole (compound 43) From 6-Bromo-1-triisopropylsilyl-indole (400 mg, 1.14 mmol), 2-methylpiperazine (1.36 mg, 13.6 mmol), NaOtBu (0.153 mg, 1.59 mmol), tBu3P (12 mg) and Pd(OAc)2 (3 mg) in xylene (1 ml) under argon.. The reaction mixture was heated to 120 C. (59%).

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference:
Patent; NPS Allelix Biopharmaceuticals, Inc.; US6716837; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of 2-Methylpiperazine

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 26 6-(3-methylpiperazinyl)-1-triisopropylsilyl-indole (compound 43) From 6-Bromo-1-triisopropylsilyl-indole (400 mg, 1.14 mmol), 2-methylpiperazine (1.36 mg, 13.6 mmol), NaOtBu (0.153 mg, 1.59 mmol), tBu3P (12 mg) and Pd(OAc)2 (3 mg) in xylene (1 ml) under argon.. The reaction mixture was heated to 120 C. (59%).

109-07-9, As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference:
Patent; NPS Allelix Biopharmaceuticals, Inc.; US6716837; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of 2-Methylpiperazine

109-07-9, The synthetic route of 109-07-9 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 2 1-Cyclopropyl-6,8-difluoro-5-methyl-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid: 1-Cyclopropyl-6,7,8-trifluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.50 g) and 2-methylpiperazine (0.54 g) were allowed to react in the same manner as described in Example 1 to give 1-cyclopropyl-6,8-difluoro-5-methyl-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.40 g). m.p. 188-191 C.

109-07-9, The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Dainippon Pharmaceutical Co., Ltd.; EP319906; (1990); A3;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of 2-Methylpiperazine

109-07-9, The synthetic route of 109-07-9 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 2 1-Cyclopropyl-6,8-difluoro-5-methyl-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid: 1-Cyclopropyl-6,7,8-trifluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.50 g) and 2-methylpiperazine (0.54 g) were allowed to react in the same manner as described in Example 1 to give 1-cyclopropyl-6,8-difluoro-5-methyl-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.40 g). m.p. 188-191 C.

109-07-9, The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Dainippon Pharmaceutical Co., Ltd.; EP319906; (1990); A3;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of 2-Methylpiperazine

109-07-9, The synthetic route of 109-07-9 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.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 2 1-Cyclopropyl-6,8-difluoro-5-methyl-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid: 1-Cyclopropyl-6,7,8-trifluoro-5-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.50 g) and 2-methylpiperazine (0.54 g) were allowed to react in the same manner as described in Example 1 to give 1-cyclopropyl-6,8-difluoro-5-methyl-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (0.40 g). m.p. 188-191 C.

109-07-9, The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Dainippon Pharmaceutical Co., Ltd.; EP319906; (1990); A3;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

13 Sep 2021 News Brief introduction of 2-Methylpiperazine

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Synthesis of 3-methyl-1-thiazol-2-ylpiperazine 30.06 g (300.0 mmol) of 2-methylpiperazine were combined with 4.51 ml (50.0 mmol) of 2-bromothiazole. This mixture was fused and refluxed 5 min. The reaction mixture was cooled and taken up in 10% strength hydrochloric acid and washed with EA. The aqueous phase was set to pH>12 with a 10% strength aq. NaOH solution and then extracted with EA. The organic phase was dried over MgSO4 and conc. in vacuo. There were obtained 8.26 g (45.1 mmol, 90%) of 3-methyl-1-thiazol-2-ylpiperazine., 109-07-9

The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Gruenenthal GmbH; US2007/112011; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of 2-Methylpiperazine

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 9 In a 100 ml four-neck flask, 5.06 g (= 0.0505 mole) of racemic 2-methylpiperazine was placed, and 50.00 g of 1-butanol (water content 0.05 wtpercent) was added for dissolution. After cooling down to 0°C, 10.91 g (= 0.0500 mole, 0.99 molar time) of di-tert-butyl dicarbonate was added dropwise with the liquid temperature kept in a range from 5 to 15°C. Then, stirring was carried out at 5 to 10°C for 2 hours. The reaction solution was analyzed, and as a result, the conversion of 2-methylpiperazine was 94.7percent, while the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 89.3percent (reaction yield 84.6percent).Example 10 An experiment was carried out as described for Example 9, except that the amount of di-tert-butyl dicarbonate used was changed to 11.97 g (= 0.0548 mole, 1.10 molar times). As a result, the conversion of 2-methylpiperazine was 100.0percent, and the selectivity of 1-tert-butoxycarbonyl-3-methylpiperazine was 81.5percent (reaction yield 81.5percent)., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Brief introduction of 2-Methylpiperazine

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 In a 100 ml four-neck flask, 5.00 g (= 0.0499 mole) of racemic 2-methylpiperazine was placed, and 44 g of 1-butanol (water content 0.05 wt%) was added for dissolution. The solution was cooled to 0C, and 8.47 g of benzyl chlorocarbonate (= 0.0489 mole, purity by HPLC determination analysis 98.5 wt%, 0.98 molar time) was added dropwise in a liquid temperature range from 0 to 8C. Then, stirring was carried out at 0 to 5C for 2 hours, and the reaction solution was partially sampled and determined by the internal standard method (internal standard: anisole). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 83.9% (based on the amount of 2-methylpiperazine). The reaction solution was further stirred at room temperature for 12 hours and analyzed. As a result, the reaction yield was 85.1%. Example 3 A reaction was performed as described for Example 1, except that the amount of benzyl chlorocarbonate used was changed from 8.47 g to 10.1 g (= 0.0597 mole, 1.17 molar times). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 93.8% (based on the amount of 2-methylpiperazine) after lapse of 2 hours at 0 to 5C. Stirring was carried out at room temperature for further 12 hours, being followed by analysis. As a result, the reaction yield was 95.1%., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference:
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Brief introduction of 2-Methylpiperazine

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

109-07-9, 2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 In a 100 ml four-neck flask, 5.00 g (= 0.0499 mole) of racemic 2-methylpiperazine was placed, and 44 g of 1-butanol (water content 0.05 wt%) was added for dissolution. The solution was cooled to 0C, and 8.47 g of benzyl chlorocarbonate (= 0.0489 mole, purity by HPLC determination analysis 98.5 wt%, 0.98 molar time) was added dropwise in a liquid temperature range from 0 to 8C. Then, stirring was carried out at 0 to 5C for 2 hours, and the reaction solution was partially sampled and determined by the internal standard method (internal standard: anisole). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 83.9% (based on the amount of 2-methylpiperazine). The reaction solution was further stirred at room temperature for 12 hours and analyzed. As a result, the reaction yield was 85.1%. Example 3 A reaction was performed as described for Example 1, except that the amount of benzyl chlorocarbonate used was changed from 8.47 g to 10.1 g (= 0.0597 mole, 1.17 molar times). As a result, the reaction yield of 1-benzyloxycarbonyl-3-methylpiperazine was 93.8% (based on the amount of 2-methylpiperazine) after lapse of 2 hours at 0 to 5C. Stirring was carried out at room temperature for further 12 hours, being followed by analysis. As a result, the reaction yield was 95.1%., 109-07-9

As the paragraph descriping shows that 109-07-9 is playing an increasingly important role.

Reference:
Patent; Toray Fine Chemicals Co., Ltd.; EP1548010; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics