28 Sep 2021 News Some tips on Piperazin-2-one

The synthetic route of 5625-67-2 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, STEP 1 Piperazin-2-one (1 g, 10 mmol) was dissolved in CH2C12 (40 ML), and BOC20 (2.4 g, 11 mmol, 1.1 eq), Et3N (2.02 g, 20 mmol, 2 eq) and DMAP (0.024 g, 0.2 mmol, 2 mol%) were added. After the mixture was stirred at RT for 16 h, it was acidified with 1 N HCI. The organic layer was separated, washed with saturated NAHC03, brine, dried (Na2SO4), and concentrated in vacuo to give the product (1.8 g, 90%) as a white SOLID. H NMR (CDCI3, 300 MHz) No. 6. 70 (1 H, bs), 4.08 (2H, s), 3.62 (2H, t, J = 6. 0 Hz), 3.37 (2H, m), 1.46 (9H, s).

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SCHERING CORPORATION; PHARMACOPEIA DRUG DISCOVERY, INC.; WO2005/14540; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

28 Sep 2021 News New learning discoveries about Piperazin-2-one

5625-67-2, 5625-67-2 Piperazin-2-one 231360, 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

Reference Example 50: 3 -Oxo-4-(2-trimethylsilanyl-ethoxymethyl)-piperazine-l -carboxylic acid benzyl ester.; Piperazin-2-one (2.00 g, 20.0 mmol) was dissolved in H2O (10 ml) – 1,4-dioxane (10 ml); and NaHCO3 (1.85 g, 22.0 mmol) and benzylchloroformate (3.42 g, 20.0 mmol) was added thereto. After stirring at room temperature for 13 h, the reaction mixture was diluted with H2O and EtOAc. The aqueous layer was extracted with EtOAc and the combined organic layer was washed with brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure to obtain crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester as pale brown oil. This oil was used for the next step without further purification. The crude 3 -Oxo-piperazine-1 -carboxylic acid benzyl ester was dissolved in DMF (40 ml) and NaH (55% in oil, 1.05 g, 24.0 mmol) and SEMCl (5.01 g, 30.0 mmol) was added thereto at room temperature. After stirring at 500C for 18 h, the reaction mixture was diluted with EtOAc. The mixture was washed with H2O and brine, dried over MgSOphi The desiccant was removed through filtration and the filtrate was concentrated under reduced pressure. The EPO residue was purified by silica gel column chromatography (hexane / EtOAc = 8 / 2 to 5 / 5, to obtain the intended compound as a colorless oil.

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; MERCK & CO., INC.; BANYU PHARMACEUTICAL CO., LTD.; WO2007/11809; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of Piperazin-2-one

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5625-67-2, Reference Example 3 4-(Tert-butoxycarbonyl)-2-piperazinone To a mixture of 2-piperazinone (3.00 g) and acetonitrile (50 ml) was added dropwise di-tert-butylbicarbonate (7.20 g), and the mixture was stirred at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure, and precipitated crystals were washed with ether to give colorless crystals of the title compound (4.77 g). 1H-NMR (CDCl3) delta: 1.48 (9H, s), 3.33-3.43 (2H, m), 3.64 (2H, t, J=5.3 Hz), 4.09 (2H, s), 6.40-6.70 (1H, br). IR (KBr): 1696, 1667, 1400, 1341, 1130 cm-1.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference:
Patent; Takeda Chemical Industries, Ltd.; US6403595; (2002); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24 Sep 2021 News Simple exploration of Piperazin-2-one

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

5625-67-2,5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added to a mixed solution of piperazin-2-one (2.5 g) in tetrahydrofuran (50 mL) and methanol (50 mL) at room temperature, and the resultant mixture was stirred for 4 hours. The reaction solvent was evaporated under reduced pressure, water and ethyl acetate were added to the residue thus obtained, and the mixture was partitioned. The organic layer was washed with water and saturated saline in this order, and then the washing water layer was combined for further extraction with ethyl acetate. The organic layers were combined and dried over anhydrous magnesium sulfate. After separation by filtration, a residue obtained by evaporating the solvent under reduced pressure was solidified using ethyl acetate-hexane, thus to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (3.6 g, 72%). 1H-NMR(400MHz, CDCl3)delta: 1.48(9H, s), 3.37-3.40(2H, m), 3.62-3.65(2H, m), 4.01(2H, s), 6.32(1H, br s).1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester To a mixed solution of piperazin-2-one (5.07 g) in tetrahydrofuran (50 mL) and methanol (50 mL), triethylamine (7.76 mL) and di-tert-butyl dicarbonate ester (12.17 g) were added at room temperature, and the resultant mixture was stirred for 4 hours. The solvent of the reaction solution was evaporated under reduced pressure, diethyl ether was added to a residue thus obtained, and the precipitated solid was filtered, to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (9.36 g, 92%). 1H-NMR(400MHz, DMSO-d6)delta: 1.40(9H, s), 3.15(2H, br), 3.45(2H, br), 3.81(2H, br), 8.03(1H, br). ESI-MSm/z: 201(M+H)+.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

24 Sep 2021 News Simple exploration of Piperazin-2-one

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

5625-67-2,5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester Triethylamine (3.83 mL) and di-tert-butoxydicarbonate (6.32 mL) were added to a mixed solution of piperazin-2-one (2.5 g) in tetrahydrofuran (50 mL) and methanol (50 mL) at room temperature, and the resultant mixture was stirred for 4 hours. The reaction solvent was evaporated under reduced pressure, water and ethyl acetate were added to the residue thus obtained, and the mixture was partitioned. The organic layer was washed with water and saturated saline in this order, and then the washing water layer was combined for further extraction with ethyl acetate. The organic layers were combined and dried over anhydrous magnesium sulfate. After separation by filtration, a residue obtained by evaporating the solvent under reduced pressure was solidified using ethyl acetate-hexane, thus to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (3.6 g, 72%). 1H-NMR(400MHz, CDCl3)delta: 1.48(9H, s), 3.37-3.40(2H, m), 3.62-3.65(2H, m), 4.01(2H, s), 6.32(1H, br s).1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester To a mixed solution of piperazin-2-one (5.07 g) in tetrahydrofuran (50 mL) and methanol (50 mL), triethylamine (7.76 mL) and di-tert-butyl dicarbonate ester (12.17 g) were added at room temperature, and the resultant mixture was stirred for 4 hours. The solvent of the reaction solution was evaporated under reduced pressure, diethyl ether was added to a residue thus obtained, and the precipitated solid was filtered, to obtain 3-oxopiperazine-1-carboxylic acid tert-butyl ester (9.36 g, 92%). 1H-NMR(400MHz, DMSO-d6)delta: 1.40(9H, s), 3.15(2H, br), 3.45(2H, br), 3.81(2H, br), 8.03(1H, br). ESI-MSm/z: 201(M+H)+.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1785418; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of Piperazin-2-one

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-2-one (1.0 g, 10 mmol) was suspended in 10 mL DCM and Boc2O was slowly added. After the addition was completed, it was allowed to stand overnight at room temperature.After completion of the reaction, it was washed three times with 0.1 N diluted hydrochloric acid, 20 ml each time, and washed three times with 20 ml of saturated potassium carbonate each time.Finally, the dichloromethane was dried over anhydrous sodium sulfate.The solution was removed under vacuum to give a white solid.

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Shaoxing University; Hu Chunqi; Li Xin; Shi Yaru; Du Wenting; Tong Jie; Su Wanting; Xia Weiqi; (20 pag.)CN108610332; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of Piperazin-2-one

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5625-67-2

To a stirred solution of W-1 (20.0 g, 0.200 mol) in DCM, is added Boc anhydride (43.6 g, 0.200 mol), and TEA (40.4 g, 0.400 mol). The mixture is stirred at about 25 C. for about 18 hours. The mixture is concentrated and the residue dissolved in EtOAc then extracted with water. The organic layer is concentrated and the residue is purified by silica gel chromatography to give W-2.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Boehringer Ingelheim International GmbH; BYLOCK, Lars Anders; US2013/236468; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of Piperazin-2-one

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5625-67-2

To a stirred solution of W-1 (20.0 g, 0.200 mol) in DCM, is added Boc anhydride (43.6 g, 0.200 mol), and TEA (40.4 g, 0.400 mol). The mixture is stirred at about 25 C. for about 18 hours. The mixture is concentrated and the residue dissolved in EtOAc then extracted with water. The organic layer is concentrated and the residue is purified by silica gel chromatography to give W-2.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Boehringer Ingelheim International GmbH; BYLOCK, Lars Anders; US2013/236468; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of Piperazin-2-one

As the paragraph descriping shows that 5625-67-2 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Piperazine-2-one (1.0 g, 10 mmol) was suspended in 10 mL DCM and Boc2O was slowly added.After the addition was completed, the reaction was allowed to stand at room temperature overnight.After completion of the reaction, it was washed three times with 0.1 N diluted hydrochloric acid, 20 ml each time, and washed three times with saturated potassium carbonate, 20 ml each time.Finally, anhydrous sodium sulfate was added and the solution was removed in vacuo to give a white solid.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference:
Patent; Shaoxing University; Hu Chunqi; Li Xin; Shi Yaru; Du Wenting; Tong Jie; Su Wanting; Xia Weiqi; (21 pag.)CN108610333; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of Piperazin-2-one

As the paragraph descriping shows that 5625-67-2 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.5625-67-2,Piperazin-2-one,as a common compound, the synthetic route is as follows.

5625-67-2, Piperazine-2-one (1.0 g, 10 mmol) was suspended in 10 mL DCM and Boc2O was slowly added.After the addition was completed, the reaction was allowed to stand at room temperature overnight.After completion of the reaction, it was washed three times with 0.1 N diluted hydrochloric acid, 20 ml each time, and washed three times with saturated potassium carbonate, 20 ml each time.Finally, anhydrous sodium sulfate was added and the solution was removed in vacuo to give a white solid.

As the paragraph descriping shows that 5625-67-2 is playing an increasingly important role.

Reference:
Patent; Shaoxing University; Hu Chunqi; Li Xin; Shi Yaru; Du Wenting; Tong Jie; Su Wanting; Xia Weiqi; (21 pag.)CN108610333; (2018); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics