Sep 2021 News Brief introduction of Butyl piperazine-1-carboxylate

The synthetic route of 50606-32-1 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.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

50606-32-1, 2-{[Methyl(5,6,7,8-tetrahydro-8-quinolinyl)amino]methyl}-1H-benzimidazole-4-carboxylic acid (190 mg, 0.56 mmol), bis(2-oxo-3-oxazolidinyl)phosphinic chloride(220 mg, 0.85 mmol), /V-butoxycarbonylpiperizine (104 mg, 0.56 mmol), and N,N-diisopropylethylamine (110 mg, 0.85 mmol) were dissolved in acetonitrile (5mL) andA/,/V-dimethylformamide (2ml_) and the reaction was stirred for 16 h at 35 C. Thereaction mixture was concentrated and purified using reverse phase HPLC (0% to70% acetonitrile/water/0.1% trifluoroacetic acid gradient) to provide the protectedamine (56 mg). The amine was dissolved in dichloromethane (3mL) andtrifluoroacetic acid (2mL) and stirred for 3 h. The reaction was concentrated,dissolved in water and lyophilized to provide the product (68 mg, 30%) as an off-white trifluoroacetate salt: 1H-NMR (DMSO-cf6) 8 8.62 (d, 1H), 7.94 (d, 1H), 7.72 (d,1H), 7.58-7.54 (m, 1H), 7.41-7.35 (m, 2H), 4.74-4.70 (m, 1H), 4.60 (d, 1H), 4.48 (d,1H), 4.38 (s, 2H), 3.25 (br s, 4H), 3.13 (br s, 4H), 2.88-2.80 (m, 2H), 2.65 (s, 3H),2.36-2.30 (m, 1H), 2.08-1.96 (m, 2H), 1.82-1.72 (m, 1H). MS m/z405 (M+1).

The synthetic route of 50606-32-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2006/23400; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of Butyl piperazine-1-carboxylate

The synthetic route of 50606-32-1 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.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

50606-32-1, 2-{[Methyl(5,6,7,8-tetrahydro-8-quinolinyl)amino]methyl}-1H-benzimidazole-4-carboxylic acid (190 mg, 0.56 mmol), bis(2-oxo-3-oxazolidinyl)phosphinic chloride(220 mg, 0.85 mmol), /V-butoxycarbonylpiperizine (104 mg, 0.56 mmol), and N,N-diisopropylethylamine (110 mg, 0.85 mmol) were dissolved in acetonitrile (5mL) andA/,/V-dimethylformamide (2ml_) and the reaction was stirred for 16 h at 35 C. Thereaction mixture was concentrated and purified using reverse phase HPLC (0% to70% acetonitrile/water/0.1% trifluoroacetic acid gradient) to provide the protectedamine (56 mg). The amine was dissolved in dichloromethane (3mL) andtrifluoroacetic acid (2mL) and stirred for 3 h. The reaction was concentrated,dissolved in water and lyophilized to provide the product (68 mg, 30%) as an off-white trifluoroacetate salt: 1H-NMR (DMSO-cf6) 8 8.62 (d, 1H), 7.94 (d, 1H), 7.72 (d,1H), 7.58-7.54 (m, 1H), 7.41-7.35 (m, 2H), 4.74-4.70 (m, 1H), 4.60 (d, 1H), 4.48 (d,1H), 4.38 (s, 2H), 3.25 (br s, 4H), 3.13 (br s, 4H), 2.88-2.80 (m, 2H), 2.65 (s, 3H),2.36-2.30 (m, 1H), 2.08-1.96 (m, 2H), 1.82-1.72 (m, 1H). MS m/z405 (M+1).

The synthetic route of 50606-32-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2006/23400; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Some tips on Butyl piperazine-1-carboxylate

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

50606-32-1,50606-32-1, Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl ester: To a solution of intermediate 50.2 (7.37 g) in DCM (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDC-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with DCM, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with DCM. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1:0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/116328; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6 Sep 2021 News Some tips on Butyl piperazine-1-carboxylate

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

50606-32-1,50606-32-1, Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl ester: To a solution of intermediate 50.2 (7.37 g) in DCM (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDC-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with DCM, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with DCM. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1:0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/116328; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of Butyl piperazine-1-carboxylate

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

50606-32-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

8.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl esterTo a solution of intermediate 8.2 (7.37 g) in CH2Cl2 (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDCI-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with CH2Cl2, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with CH2Cl2. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1 :0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00.

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; LEHMANN, David; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/122504; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of Butyl piperazine-1-carboxylate

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

50606-32-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

8.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl esterTo a solution of intermediate 8.2 (7.37 g) in CH2Cl2 (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDCI-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with CH2Cl2, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with CH2Cl2. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1 :0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00.

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; LEHMANN, David; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/122504; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Downstream synthetic route of Butyl piperazine-1-carboxylate

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

50606-32-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

8.3. 4-[(R)-2-tert-Butoxycarbonylamino-3-(diethoxy-phosphoryl)-propionyl]-piperazine-l- carboxylic acid butyl esterTo a solution of intermediate 8.2 (7.37 g) in CH2Cl2 (95 mL), THF (24 mL) and DIPEA (16.3 mL) were added HOBT (3.83 g) and EDCI-HCl (4.78 g), and the reaction mixture was stirred at RT for 10 min. Subsequently, piperazine- 1 -carboxylic acid butyl ester (5.31 g) was added and the mixture stirred at RT for 2.5 h. The reaction mixture was diluted with CH2Cl2, the org. phase washed with sat. aq. NaHCO3 and the aq. phase re-extracted with CH2Cl2. The combined org. phases were washed with brine, dried over Na2SO^ and concentrated to dryness. Purification by CC (EtOAc/MeOH 1 :0 to 9: 1) gave 7.66 g of the desired product. LC-MS: tR = 0.94 min; [M+H]+: 494.00.

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CAROFF, Eva; HILPERT, Kurt; HUBLER, Francis; LEHMANN, David; MEYER, Emmanuel; RENNEBERG, Dorte; WO2010/122504; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on Butyl piperazine-1-carboxylate

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

50606-32-1,50606-32-1, Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-methyl-2-{[methyl(5,6,7,8-tetrahydro-8-quinolinyl)amino]methyl}-1/-/-benzimidazole-7-carboxylic acid (105 mg, 0.3 mmol), bis(2-oxo-3-oxazolidinyl)phosphinic chloride(109 mg, 0.43 mmol), A/-butoxycarbonylpiperizine (80, 0.43 mmol), and N,N-diisopropylethylamine (56 mg, 0.43 mmol) were dissolved in acetonitrile (5 ml_) andA/,A/-dimethylformamide (2 ml_) and the reaction was stirred for 16 h at roomtemperature. The reaction mixture was concentrated and purified using reversephase HPLC (0% to 70% acetonitrile/water/0.1% trifluoroacetic acid gradient) toprovide the protected amine. The amine was dissolved in dichloromethane (2 mL)and trifluoroacetic acid (2 mL) and stirred for 3 h. The reaction was concentrated anddried to provide the product (30.0 mg, 13%) as a sticky yellow solid. 1H-NMR(DMSO-de) 5 9.01 (brs, 1H), 8.51 (d, 1H), 7.78-7.69 (m, 2H), 7.40-7.27 (m, 3H),5.01-4.90 (m, 1H), 4.81-4.71 (m, 1H), 4.59-4.52 (m, 1H), 4.00-3.84 (m, 2H), 3.62 (s,3H), 3.54-3.40 (m, 2H), 3.29-2.97 (m, 4H), 2.88-2.82 (m, 5H), 2.53-2.49 (m, 1H),2.16-2.06 (m, 2H), 1.82-1.69 (m, 1H). MS m/z419 (M+1).

50606-32-1 Butyl piperazine-1-carboxylate 21963126, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2006/23400; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about Butyl piperazine-1-carboxylate

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

50606-32-1, Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,50606-32-1

2-{[Methyl(5,6,7,8-tetrahydro-8-quinolinyl)amino]methyl}-1H-benzimidazole-4-carbaldehyde (100 mg, 0.30 mmol), /V-butoxycarbonylpiperizine (115 mg, 0.60mmol), acetic acid (28 mg, 0.47 mmol) and sodium triacetoxyborohydride (100 mg,0.47 mmol) were dissolved in 1,2-dichloroethane (10 ml_) and stirred for 16 h at roomtemperature. The reaction concentrated and purified using reverse phase HPLC (0%to 70% acetonitrile/water/0.1% trifluoroacetic acid gradient) to provide the protectedamine. The carbamate was dissolved in dichloromethane (2 ml_) and trifluoroaceticacid (2 ml) and stirred for 3 h at room temperature. The reaction was concentrated,dissolved in water and lyophilized to provide the product (68 mg, 30%) as an off-white solid: 1H-NMR (DMSO-d6) 5 8.62 (d, 1H), 7.94 (d, 1H), 7.72 (d, 1H), 7.58-7.54(m, 1H), 7.41-7.35 (m, 2H), 4.74-4.70 (m, 1H), 4.60 (d, 1H), 4.48 (d, 1H), 4.38 (s,2H), 3.25 (br s, 4H), 3.13 (br s, 4H), 2.88-2.80 (m, 2H), 2.65 (s, 3H), 2.36-2.30 (m,1 H), 2.08-1.96 (m, 2H), 1.82-1.72 (m, 1 H). MS m/z 391 (M+1).

As the paragraph descriping shows that 50606-32-1 is playing an increasingly important role.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2006/23400; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Brief introduction of Butyl piperazine-1-carboxylate

The synthetic route of 50606-32-1 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.50606-32-1,Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

50606-32-1, 2-{[Methyl(5,6,7,8-tetrahydro-8-quinolinyl)amino]methyl}-1H-benzimidazole-4-carboxylic acid (190 mg, 0.56 mmol), bis(2-oxo-3-oxazolidinyl)phosphinic chloride(220 mg, 0.85 mmol), /V-butoxycarbonylpiperizine (104 mg, 0.56 mmol), and N,N-diisopropylethylamine (110 mg, 0.85 mmol) were dissolved in acetonitrile (5mL) andA/,/V-dimethylformamide (2ml_) and the reaction was stirred for 16 h at 35 C. Thereaction mixture was concentrated and purified using reverse phase HPLC (0% to70% acetonitrile/water/0.1% trifluoroacetic acid gradient) to provide the protectedamine (56 mg). The amine was dissolved in dichloromethane (3mL) andtrifluoroacetic acid (2mL) and stirred for 3 h. The reaction was concentrated,dissolved in water and lyophilized to provide the product (68 mg, 30%) as an off-white trifluoroacetate salt: 1H-NMR (DMSO-cf6) 8 8.62 (d, 1H), 7.94 (d, 1H), 7.72 (d,1H), 7.58-7.54 (m, 1H), 7.41-7.35 (m, 2H), 4.74-4.70 (m, 1H), 4.60 (d, 1H), 4.48 (d,1H), 4.38 (s, 2H), 3.25 (br s, 4H), 3.13 (br s, 4H), 2.88-2.80 (m, 2H), 2.65 (s, 3H),2.36-2.30 (m, 1H), 2.08-1.96 (m, 2H), 1.82-1.72 (m, 1H). MS m/z405 (M+1).

The synthetic route of 50606-32-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SMITHKLINE BEECHAM CORPORATION; WO2006/23400; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics