Category: 154590-35-9

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step 1: Cool in ice a solution of glycidol (0.63 g, 8.5 mmol) in ether (30 ml). Add DIPEA (1.6 ml, 8.5 mmol) and phosgene (1.85M in toluene, 5.8 ml, 10.8 mmol). Stir 2 h, filter, and concentrate. Dissolve in ether (50 ml) and add the product of Preparation 13, Step 3 (2.50 g, 7.7 mmol) and DIPEA (1.6 ml, 8.5 mmol). Stir 2 h, wash with sat. NaHCO3, dry (MgSO4), and concentrate to obtain the carbamate as a yellow solid

154590-35-9, The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Schering Corporation; US2004/220194; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3-4-3 Preparation of 2-[3-fluoro-4-(BOC-piperazino)]phenylamino-6-chloro-3-nitropyridine To 100ml of methanol were added 2.75g (14.2mmol) of 2,6-dichloronitropyridine and 2.38ml (17.0mmol) of triethylamine and 4.2g (14.2mmol) of [3-fluoro-4-(BOC-piperazino)]aniline obtained in Preparation Example 3-4-2 was then added thereto, followed by reaction at room temperature (20 to 30C) for about 24 hours. After the reaction was complete, the reactant was filtered, washed with 20ml of methanol and then dried under vacuum at about 40C to afford 4.47g (yield: 70%) of the desired compound. Mass (M+): 452.0 1H-NMR (DMSO-d6): 1.42(s, 9H), 2.96(t, 4H), 3.48(m, 4H), 7.01(d, 1H), 7.07(t, 1H), 7.34(d, 1H), 7.53(d, 1H), 8.53(d, 1H), 10.08(s, 1H)., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Dong Wha Pharm. Co., Ltd.; EP2394993; (2011); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To the product of Step 3 (1.00 g, 3.3 mmol) and DIPEA (0.88 ml, 5.1 mmol) in CH2Cl2 (15 ml) add trifluoroacetic anhydride (0.57 ml, 4.1 mmol). Stir 2 h and add a second portion each of DIPEA and anhydride. Stir 1 h and wash with satd. NaHCO3, then water. Dry (MgSO4) and concentrate to obtain the amide as a yellow solid., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To the product of Step 3 (1.00 g, 3.3 mmol) and DIPEA (0.88 ml, 5.1 mmol) in CH2Cl2 (15 ml) add trifluoroacetic anhydride (0.57 ml, 4.1 mmol). Stir 2 h and add a second portion each of DIPEA and anhydride. Stir 1 h and wash with satd. NaHCO3, then water. Dry (MgSO4) and concentrate to obtain the amide as a yellow solid., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154590-35-9

Combine the product of Preparation 17, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid.

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154590-35-9

Combine the product of Preparation 17, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid.

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154590-35-9

Combine the product of Preparation 17, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid.

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,154590-35-9

Combine the product of Preparation 17, Step 3 (2.2 g, 6.7 mmol) and 2-chloroethyl isocyanate (0.64 ml, 7.4 mmol) in DMF (30 ml). Heat at 60 C. 18 h, allow to cool and partition with CH2Cl2 and water. Dry (MgSO4) and concentrate to obtain the crude urea as a yellow solid.

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-35-9, tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenvH-piperazine-1-carboxylic acid tert-butyl ester. 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester(4.54 g, 15.4 mmol) and DIPEA (2.95 ml_, 16.9 mmol) were dissolved in DCM (90.0 ml.) and cooled to 00C. 2-Ethyl-butyryl chloride (2.28 ml_, 16.2 mmol) was added slowly. The resulting mixture was then stirred at 00C for 1 h and at room temperature for 4 h. The resulting mixture was then washed with water, 1 N NaOH solution and water. The organic phase was dried (Na2SO4), filtered and concentrated to yield a residue. Chromatography of the residue (SiO2, 0-8 % acetone/DCM) yielded the title compound.MS (ESI) mass calculated for C21H32FN3O3, 393.50, m/z measured, 394.6 [M+H]+ 1H NMR (CDCI3): 7.50 (dd, J = 13.9, 2.4, 1 H), 7.22 (s, 1 H), 7.15-7.07 (m,1 H), 6.88 (t, J = 9.0, 1 H), 3.63-3.52 (m, 4H), 3.00-2.92 (m, 4H), 2.06-1.93 (m, 1 H), 1.75-1.65 (m, 2H), 1.59-1.52 (m, 2H), 1.48 (s, 9H), 1.00-0.88 (m, 6H)., 154590-35-9

As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); 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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step A. 4-{2-Fluoro-4-[(R-tetrahvdro-furan-3-carbonyl)-amino1-phenyl)- piperazine-1-carboxylic acid tert-butyl ester. A mixture of 4-(4-Amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (0.7 g, 2.4 mmol), (R)-tetrahydro-furan-3-carboxylic acid (0.33 g, 2.9 mmol) and HATU (1.1 g, 2.9 mmol) was dissolved into DMF (15.0 ml.) and stirred for 1 h at room temperature. The resulting mixture was diluted with ethyl acetate (200 mL) and washed with 1 N NaOH (30 mL) and then with water (2x 200 mL), dried (Na2SO4), filtered and concentrated to dryness to yield a residue. Chromatography of the residue (SiO2, 0-5 % acetone/DCM) yielded the title compound. MS (ESI) mass calculated for C20H28FN3O4, 393.46, m/z measured, 394.6 [M+H]+1H NMR (CDCI3): 7.50-7.40 (m, 2H), 7.1 1-7.06 (m, 1 H), 6.86 (t, J = 9.0, 1 H), 4.09-3.98 (m, 2H), 3.97-3.90 (m, 1 H), 3.88-3.80 (m, 1 H), 3.62-3.54 (m, 4H), 3.08-2.92 (m, 5H), 2.30-2.20 (m, 2H), 1.48 (s, 9H).

154590-35-9, As the paragraph descriping shows that 154590-35-9 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics