Category: 78551-60-7

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78551-60-7, To a solution of the product of Step 8 (261 mg, 0.900 mmol) in anhydrous THF(5 ml) in a dry ice-acetone bath was added 2M LDA (0.45 ml) and the mixture wasstirred for 1 h. A solution of the above aldehyde in THF (5 ml) was added and themixture was stirred in the dry ice-acetone bath for 2 h. The reaction was quenchedwith saturated NH4CI (4 ml), diluted with CH2CI2 (50 ml), and washed with water (30ml). The organic layer was extracted with saturated NH4CI and brine, dried (MgSO4),concentrated, and purified by PTLC (5% MeOH/CH2CI2) to give the product (100 mg,48%). MS m/e 699 (M+H)+

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SCHERING CORPORATION; WO2006/14944; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,78551-60-7

To a solution of oxalyl chloride (214 mg, 1.65 mmol) in CH2CI2 (2.5 ml) in a dryice-acetone bath was added DMSO (356 mg, 4.56 mmol). After 5 min, a solution ofthe product of Step 7 (508 mg, 1.41 mmol) in CH2CI2 (3.5 ml) was added and themixture was stirred for 1 h. Triethylamine (700 nl, 5.02 mmol) was added and themixture was stirred for 15 min. The mixture was warmed to RT and stirred for 15 min.Water (30 ml) and CH2CI2 (40 ml) were added and the aqueous layer was extractedwith CH2CI2 (30 ml). The combined organic layer was washed with brine (50 ml),dried (MgSO/O, and concentrated to give the aldehyde, which was not further purified.To a solution of diisopropylamine (188 mg, 1.86 mmol) in THF (2.5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (1.40 ml, 2.24 mmol).After 5 min the mixture was put in an ice-water bath and stirred for 20 min. Thesolution was cooled in the dry ice-acetone bath again and a solution of the product ofPreparative Example 1, Step 5 (460 mg, 1.59 mmol) in THF (4 ml) was added. Themixture was stirred for 1 h. A solution of the above aldehyde in THF (4 ml) wasadded and the mixture was stirred for 1.5 h. The reaction was quenched with water(40 ml) and extracted with ether (50 ml). The aqueous layer was extracted with ether(3×40 ml). The combined organic layer was washed with brine (50 ml), dried(MgSO4), concentrated, and purified by PTLC (40% EtOAc/Hexanes) to give: fraction1 (137 mg, 15%). MS m/e 648 (M+H)+; fraction 2 (148 mg, 16%). MS m/e 648 (M+H)+

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SCHERING CORPORATION; WO2006/14762; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

78551-60-7, Preparation 46: (‘S)-2-[?S2S)-2-amino-l-hvdroxy-3-phenylpropyl”|-4-benzyl-3-oxo-piperazine-l- carboxylic acid t-butyl ester Step A: (S)-4-benzyl-2-|Tl S,2SV2-(dibenzylamino)-l-hvdroxy-3-phenylpropyl]-3-oxo-piperazine- 1-carboxylic acid t-butyl esterDsopropylamine (1.42 mL, 10.08 mmol) was dissolved in anhydrous tetrahydrofuran (10 mL) and the mixture was cooled to -78 C. n-butyl Miium (2.5 M n-hexane solution, 3.9 mL) was added dropwise to the resulting solution. The mixture was stirred for 5 min and then stirred on an ice bath for 30 min. The reaction mixture was cooled to -78 C, and a solution of t-butyl 4-benzyl- 3-oxopiperazine-l-carboxylate (B) (2.44 g, 8.40 mmol) in 15 mL of anhydrous tetrahydrofuran was added dropwise thereto, followed by stirring at that temperature for 1.5 hours. Thereafter, a solution of 2(S)-2-(dibenzylamino)-3-phenylpropanal (A) (2.99 g, 9.07 mmol) in anhydrous tetrahydrofuran (15 mL) was added to the reaction mixture which was gradually warmed to room temperature. After stirring at room temperature for 16 hours, the reaction was terminated with addition of water, followed by extraction with saturated ammonium chloride (aqueous) and diethyl ether. The organic layer was taken, dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. The residue was purified by column chromatography (EtOAc/n-Hex = 1/5) to afford the title compound (1.92 g, 24%).

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; LG LIFE SCIENCES, LTD.; WO2009/38411; (2009); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7,78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of diisopropylamine (667 mg, 6.59 mmol) in THF (5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (4.13 ml, 6.61 mmol).After 5 min the mixture was put in an ice-water bath and stirred for 20 min. Thesolution was cooled in the dry ice-acetone bath again and a solution of the product ofPreparative Example 1, Step 8 (1.74 g, 5.99 mmol) in THF (20 ml) was added. Themixture was stirred for 1 h. A solution of the above aldehyde in THF (30 ml) wasadded and the mixture was allowed to warm up to RT slowly and stirred for 16 h. Thereaction was quenched with saturated NH4CI (20 ml) and extracted with ether (3x100ml). The combined organic layer was washed with 5% citric acid, saturated NaHCO3,and brine, dried (Na2SO4), concentrated, and purified by column chromatography(gradient EtOAc/Hexanes 0-40%) to give the product (1.20 g, 35%). MS m/e 694

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SCHERING CORPORATION; WO2006/14944; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 24:4-benzyl-4,7-diaza-spiro[2.5]octane-7-carboxylic acid tert-butyl esterTo EtMgBr (344 mL) in THF cooled to -78C was added Ti(0’Pr)4 (39 g, 137.93 mmol), followed by commercially available 4-benzyl-3-oxo-piperazine-l-carboxylic acid tert- butyl ester (40 g, 137.93 mmol) and the resultant reaction mixture was heated to reflux for 1 h. After cooling the reaction mixture to 5C, another portion of EtMgBr (344 ml) and Ti(0’Pr)4 (39 g, 137.93 mmol) was added. The mixture was stirred for 16 h at RT. The reaction mixture was quenched with NH4CI solution and stirred for 15 min and filtered through a celite bed and washed with EtOAc. The aqueous layer was again extracted with EtOAc (3 x). The combined EtOAc layers were washed with water and dried over Na2S04 and concentrated under reduced pressure. Purification by column chromatography to afforded the title compound as a solid (24 g, 58%).XH NMR (300 MHz, DMSO) delta = 7.20 (m, 5H), 3.80 (s, 2H), 3.40 (m, 2H), 3.22 (m, 2H), 2.63 (m, 2H), 1.38 (s, 9H), 0.58 (br, 4H), 78551-60-7

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; LEO PHARMA A/S; SCHOU, S°ren Christian; GREVE, Daniel Rodriguez; NIELSEN, Simon Feldbaek; JENSEN, Jens Bj°rn; DACK, Kevin Neil; WO2012/93169; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The product of part a) (420 mg) was stirred in TFA (10 ml) for 30 min, then 0 concentrated in vacuo to give the sub-title compound as an oil (415 mg). EPO MS: ESI (+ve): 191 (M+H), 78551-60-7

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/56752; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,78551-60-7

To a solution of oxalyl chloride (1.08 g, 8.30 mmol) in CH2CI2 (7 ml) in a dryice-acetone bath was added DMSO (1.14 g, 14.6 mmol). After 5 min, a solution ofthe product of Step 3 (3.01 g, 7.34 mmol) in CH2CI2 (7 ml) was added and the mixturewas stirred for 1 h. Diisopropylethylamine (3.28 g, 25.4 mmol) was added and after 2min the cooling bath was removed. The mixture was stirred for 30 min and dilutedwith water (50 ml). CH2CI2 (40 ml) was added and the aqueous layer was extractedwith CH2CI2 (40 ml). The combined organic layer was washed with brine, dried(MgSC>4), and concentrated to give the aldehyde, which was not further purified.To a solution of diisopropylamine (896 mg, 8.85 mmol) in THF (5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (5.5 ml, 8.8 mmol). After 5min the mixture was put in an ice-water bath and stirred for 20 min. The solution wascooled in the dry ice-acetone bath again and a solution of the product of Step 5 (2.14g, 7.37 mmol) in THF (8 ml) was added. The mixture was stirred for 1 h. A solutionof the above aldehyde in THF (10 ml) was added and the mixture was stirred for 1.5h. The reaction was quenched with water and partitioned between ether (4×50 ml)and water (50 ml). The combined organic layer was washed with brine (50 ml), dried(MgSO4), concentrated, and purified by column chromatography (gradientEtOAc/Hexanes 0-20%) to give the product (2.67 g, 52%). MS m/e 698 (M+H)+

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; WO2006/14762; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,78551-60-7

To a solution of oxalyl chloride (1.08 g, 8.30 mmol) in CH2CI2 (7 ml) in a dryice-acetone bath was added DMSO (1.14 g, 14.6 mmol). After 5 min, a solution ofthe product of Step 3 (3.01 g, 7.34 mmol) in CH2CI2 (7 ml) was added and the mixturewas stirred for 1 h. Diisopropylethylamine (3.28 g, 25.4 mmol) was added and after 2min the cooling bath was removed. The mixture was stirred for 30 min and dilutedwith water (50 ml). CH2CI2 (40 ml) was added and the aqueous layer was extractedwith CH2CI2 (40 ml). The combined organic layer was washed with brine, dried(MgSC>4), and concentrated to give the aldehyde, which was not further purified.To a solution of diisopropylamine (896 mg, 8.85 mmol) in THF (5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (5.5 ml, 8.8 mmol). After 5min the mixture was put in an ice-water bath and stirred for 20 min. The solution wascooled in the dry ice-acetone bath again and a solution of the product of Step 5 (2.14g, 7.37 mmol) in THF (8 ml) was added. The mixture was stirred for 1 h. A solutionof the above aldehyde in THF (10 ml) was added and the mixture was stirred for 1.5h. The reaction was quenched with water and partitioned between ether (4×50 ml)and water (50 ml). The combined organic layer was washed with brine (50 ml), dried(MgSO4), concentrated, and purified by column chromatography (gradientEtOAc/Hexanes 0-20%) to give the product (2.67 g, 52%). MS m/e 698 (M+H)+

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SCHERING CORPORATION; WO2006/14762; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78551-60-7, To a solution of the product of Step 8 (261 mg, 0.900 mmol) in anhydrous THF(5 ml) in a dry ice-acetone bath was added 2M LDA (0.45 ml) and the mixture wasstirred for 1 h. A solution of the above aldehyde in THF (5 ml) was added and themixture was stirred in the dry ice-acetone bath for 2 h. The reaction was quenchedwith saturated NH4CI (4 ml), diluted with CH2CI2 (50 ml), and washed with water (30ml). The organic layer was extracted with saturated NH4CI and brine, dried (MgSO4),concentrated, and purified by PTLC (5% MeOH/CH2CI2) to give the product (100 mg,48%). MS m/e 699 (M+H)+

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SCHERING CORPORATION; WO2006/14944; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78551-60-7,tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

78551-60-7, To a solution of oxalyl chloride (762 mg, 6.00 mmol) in CH2CI2 (10 ml) in a dryice-acetone bath was added DMSO (938 mg, 12.0 mmol). After 5 min, a solution ofthe product of Step 4 (2.03 g, 5.01 mmol) in CH2CI2 (20 ml) was added and themixture was stirred for 1 h. Triethylamine (2.42 g, 23.9 mmol) was added and after 2min the cooling bath was removed. The mixture was stirred for 30 min and dilutedwith water (50 ml). CH2CI2 (100 ml) was added and the aqueous layer was extractedwith CH2CI2 (2×100 ml). The combined organic layer was washed with brine, dried(MgSO4), and concentrated to give the aldehyde, which was not further purified.To a solution of diisopropylamine (667 mg, 6.59 mmol) in THF (5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (4.13 ml, 6.61 mmol).After 5 min the mixture was put in an ice-water bath and stirred for 20 min. Thesolution was cooled in the dry ice-acetone bath again and a solution of the product of Preparative Example 1, Step 5 (1.74 g, 5.99 mmol) in THF (20 ml) was added. Themixture was stirred for 1 h. A solution of the above aldehyde in THF (30 ml) wasadded and the mixture was allowed to warm up to RT slowly and stirred for 16 h. Thereaction was quenched with saturated NH4CI (20 ml) and extracted with ether (3x100ml). The combined organic layer was washed with 5% citric acid, saturated NaHCO3,and brine, dried (Na2SO4), concentrated, and purified by column chromatography(gradient EtOAc/Hexanes 0-40%) to give the product (1.20 g, 35%). MS m/e 694

The synthetic route of 78551-60-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SCHERING CORPORATION; WO2006/14762; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics