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

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

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.,5625-67-2

Example 29 Step 1: Piperazin-2-one (1 g, 10 mmol) was dissolved in CH2CI2 (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 (CDC13, 300 MHz) 8 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).

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

Reference:
Patent; SCHERING CORPORATION; PHARMACOPEIA DRUG DISCOVERY, INC; WO2005/16876; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

8 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.

5625-67-2,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.

1 Syntheis of 4-tert-Butoxycarbonyl-2-oxopiperazine Di-tert-butyl dicarbonate (10.4 g, 47.6 mmol) was added to a stirred solution of 2-oxopiperazine (4.77 g, 47.6 mmol) in ethanol (100 ml) at room temperature. After stirring at room temperature for 1 hour, the reaction mixture was concentrated in vacuo to give 4-tert-butoxycarbonyl-2-oxopiperazine as colorless crystals (8.00 g, 84%), which were collected by filtration and washed with hexane. 1H-NMR (200 MHz, CDCl3) delta: 6.90-6.56 (1H, m), 4.09 (2H, s), 3.64 (2H, t, J=5.2 Hz), 3.44-3.34 (2H, m), 1.48 (9H, s). IR (KBr): 3265, 3195, 2981, 1691, 1666, 1635, 1419, 1398, 1365, 1338, 1243, 1176, 1131, 1002 cm-1.

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

Reference:
Patent; Takeda Chemical Industries, Ltd.; US6235731; (2001); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

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.

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, then water and ethyl acetate were added to the residue thus obtained, and the mixture was partitioned. The organic layer was washed sequentially with water and saturated brine, and then the washing water layers were combined and extracted again with ethyl acetate. The combined organic layers were dried over anhydrous magnesium sulfate. After separating the organic layer by filtration, the solvent was evaporated under reduced pressure, and a residue thus obtained was solidified from ethyl acetate-hexane, 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)., 5625-67-2

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

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1803719; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

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.

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, then water and ethyl acetate were added to the residue thus obtained, and the mixture was partitioned. The organic layer was washed sequentially with water and saturated brine, and then the washing water layers were combined and extracted again with ethyl acetate. The combined organic layers were dried over anhydrous magnesium sulfate. After separating the organic layer by filtration, the solvent was evaporated under reduced pressure, and a residue thus obtained was solidified from ethyl acetate-hexane, 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)., 5625-67-2

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

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1803719; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 mixture of piperazine-2-one (1.037 g, 10.4 mmol) in 52 mL of CH2Cl2, was added BOC2O (2.5 g, 11.4 mmol). The reaction became homogeneous after 3 hours when the starting material was completely consumed. The reaction was diluted with CH2Cl2 and the organic layer was washed with water. The solvent was removed in vacuo to yield quantitative amount of product 33 as a white solid. 1H NMR (300 MHz, CDCl3) delta 1.48 (s, 9H), 3.35-3.44 (m, 2H), 3.64 (t, 2H, J= 5 Hz), 4.10 (s, 2H), 6.41 (br s, 1H).

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

Reference:
Patent; Gilead Sciences, Inc.; WO2004/35576; (2004); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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, [Referential Example 90]; 4-Methyl-3-oxopiperazine-1-carboxylic acid tert-butyl ester; 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester ; Triethylamine (3.9 mL) and di-tert-butyl dicarbonate (6.31 g) were added to 2-oxopiperazine (2.61 g) in a mixture of tetrahydrofuran (40 mL) and methanol (50 mL) at room temperature, followed by stirring for 3 hours. The solvent was evaporated under reduced pressure. To the residue, diethyl ether was added, and the precipitated solid was recovered by filtration, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester (4.54 g, 87%).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). LC-MSm/z: 201(M+H)+.

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

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1591443; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 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,5625-67-2

A 2-L Erlenmeyer flask was charged with 2-piperazinone (36.5 g, 364 mmol, Sigma- Aldrich, St. Louis, MO), sodium carbonate (116 g, 1093 mmol), 600 mL of dioxane, and 150 mL of water. To this was slowly added benzyl chloroformate (62.1 g, 364 mmol, Sigma-Aldrich, St. Louis, MO) at room temperature over 20 min. After the addition was complete, the mixture was stirred for 2 h and then diluted with water and extracted with EtOAc (2 L). The combined organic extracts were dried (MgS04), filtered, and concentrated to give a white solid. To this solid was added 500 mL of DCM, triethylamine (128 mL, 911 mmol), DMAP (4.45 g, 36.4 mmol), and di-tert-butyl dicarbonate (119 g, 546 mmol, Sigma-Aldrich, St. Louis, MO). After 1 h at room temperature, the mixture was diluted with water and the organics were separated. The organics were dried (MgS04), filtered, and concentrated to give a brown oil. To this oil was added 100 mL of DCM followed by 1 L of hexane. The resulting white solid was collected by filtration to give 4-benzyl 1-tert-butyl 2-oxo-l,4- piperazinedicarboxylate (101 g).

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

Reference:
Patent; AMGEN INC.; ASHTON, Kate; BOURBEAU, Matthew, Paul; HONG, Fang-Tsao; LIU, Longbin; NISHIMURA, Nobuko; NORMAN, Mark, H.; POON, Steve, F.; STEC, Markian, M.; ST. JEAN, David, J., JR; TAMAYO, Nuria, A.; YANG, Kevin, C.; WO2013/123444; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of 5625-67-2

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

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

EXAMPLE 2 t-Butyl 3-Oxo-1-piperazinecarboxylate (2) To a mixture of piperazinone 1 (1.0 g, 1.0*10-2 mole) and sieve dried THF (15 ml) is added dropwise a solution of di-tert-butyl dicarbonate (2.4 g, 1.1*10-2 mole) and sieve dried THF (5 ml). Evolution of CO2 occurs immediately and the starting material slowly dissolves. After stirring at room temperature overnight the solvent is evaporated at reduced pressure affording 2 as a beige solid which crystallized from ethyl acetate/hexane as colorless plates: 1.2 g (60%), m.p. 159-161 C.

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

Reference:
Patent; Richardson-Merrell Inc.; US4341698; (1982); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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, [Referential Example 90]; 4-Methyl-3-oxopiperazine-1-carboxylic acid tert-butyl ester; 1) 3-Oxopiperazine-1-carboxylic acid tert-butyl ester ; Triethylamine (3.9 mL) and di-tert-butyl dicarbonate (6.31 g) were added to 2-oxopiperazine (2.61 g) in a mixture of tetrahydrofuran (40 mL) and methanol (50 mL) at room temperature, followed by stirring for 3 hours. The solvent was evaporated under reduced pressure. To the residue, diethyl ether was added, and the precipitated solid was recovered by filtration, to thereby give 3-oxopiperazine-1-carboxylic acid tert-butyl ester (4.54 g, 87%).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). LC-MSm/z: 201(M+H)+.

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

Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1591443; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics