Sep 2021 News Some tips on 1-(4-Trifluoromethylphenyl)piperazine

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Carbonyldiimidazole (0.97g, 0.006mol) in 5mL of dry THF was added to a solution of intermediates 1 (1.11g, 0.006mol), 2 (1.19g, 0.006mol), 3 (1.19g, 0.006mol) or 4 (1.28g, 0.006mol) dissolved in 10mL of anhydrous THF while stirring. After the end of gaseous (carbon dioxide) evolution (c.a. 0.5h), the respective secondary amines (0.006mol) dissolved in 5mL of anhydrous THF was added dropwise. The mixture was stirred at room temperature (approx. 24h) and evaporated to dryness. The crude product was purified by column chromatography (dichloromethane/methanol, 9:0.3, v/v). The final amides were obtained as solid substances followed by concentration of organic solvents under reduced pressure, and recrystallization from 2-propanol., 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference:
Article; Kami?ski, Krzysztof; Zagaja, Miros?aw; Rapacz, Anna; ?uszczki, Jarogniew J.; Andres-Mach, Marta; Abram, Micha?; Obniska, Jolanta; Bioorganic and Medicinal Chemistry; vol. 24; 4; (2016); p. 606 – 618;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, 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.208167-83-3,tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(a) Preparation of N-[1-butyl-4-[3-{2-(4-tert-butoxycarbonyl-1-piperazinyl)ethoxy}phenyl]-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N’-(2,6-diisopropylphenyl)urea The title compound was obtained in the same manner as in Reference Example 12 from N-[4-(3-hydroxyphenyl)-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N’-(2,6-diisopropylphenyl)urea and 1-tert-butoxycarbonyl-4-(2-chloroethyl)piperazine. 1H-NMR delta (CD3OD) 8.63 (1H, dd, J=4.6Hz, 1.7Hz), 7.75 (1H, dd, J=7.9Hz, 1.7Hz), 7.47 (1H, dd, J=8.2Hz, 7.9Hz), 7.04-7.30 (5H, m), 6.93-7.04 (2H, m), 4.60-4.73 (2H, m), 4.05-4.10 (2H, m), 3.38-3.53 (4H, m), 2.92-3.10 (2H, m), 2.55-2.68 (2H, m), 2.36-2.54 (4H, m), 1.95-2.10 (2H, m), 1.70-1.90 (2H, m), 1.45-1.62 (2H, m), 1.49 (9H, s), 1.15 (12H, d, J=6.6Hz), 1.05 (3H, t, J=7.3Hz), 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; SUMITOMO PHARMACEUTICALS COMPANY, LIMITED; EP947515; (1999); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Brief introduction of 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine

5747-48-8, The synthetic route of 5747-48-8 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.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

Example 10 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol OR 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of 11-piperazinyldibenzo[b,f][1,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25-30 C., and, to which, was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 moles)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110-112 C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check absence of compound of formula IV) and was cooled to 25 C. to 30 C. To which, was added 150 cc DM water. Then the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extracts and the organic layer were combined, and the pH was adjusted to 2-3 using 1N HCl solution in DM (demineralized) water, the reaction mixture was then stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30 C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The extracts and the organic layer were combined, and washed with DM (demineralized) water 300 cc twice. The organic layer was distilled-off under vacuum below 70 C. to afford 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol Purity of 2-(2-(4-dibenzo[b,f]-[1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol was 99.0 (area % by HPLC).

5747-48-8, The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Kansal, Vinod Kumar; Ahmad, Suhail; Lal, Kanhaiya; Patil, Bhatu Tumba; US2008/241949; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News New learning discoveries about (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

300543-56-0, (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,300543-56-0

Example 3; Preparation of oxalate salt of Compound (III); A solution of compound (III, obtained above) in IPA (508 ml) was heated to 40-45C. To this, oxalic acid (78.13 g) was added. The reaction mixture was allowed to reflux to 80-85C for 30 min and then cooled at 20-30C and stirred for 5h. The solid thus obtained was filtered and washed with IPA (124 ml). The title compound was then dried under vacuum at 50-55 C for 12h. The title compound (1 15.0 g) was obtained with 71.65% yield.

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

Reference:
Patent; JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; DUBEY, Shailendra, Kumar; MANGLA, Amit; MASAND, Mukesh; VIR, Dharam; WO2012/101475; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

22 Sep 2021 News New learning discoveries about 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline

122833-04-9, As the paragraph descriping shows that 122833-04-9 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

4.1.4.12 (S)-1-(2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(trifluoromethoxy)benzyl)piperidine-3-carboxamide (2d) Compound 5d (257?mg, 0.56?mmol) was reacted with 2-methoxy-4-(4-methylpiperazin-1-yl)aniline (137?mg, 0.62?mmol) according to the general procedure B to give compound 2d (177?mg, yield: 53%).

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference:
Article; Liu, Siming; Jiang, Ying; Yan, Ruohong; Li, Zhonghuang; Wan, Shanhe; Zhang, Tingting; Wu, Xiaoyun; Hou, Ju; Zhu, Zhengguang; Tian, Yuanxin; Zhang, Jiajie; European Journal of Medicinal Chemistry; vol. 179; (2019); p. 358 – 375;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Simple exploration of tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate

192130-34-0, The synthetic route of 192130-34-0 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a mixture of 2-HEXYLMERCAPTO-6- (3, 4, 5-trimethoxyphenyl)-pyrimidin-4-carboxylic acid (Example 1A, 150 mg, 0.37 MMOL), HATU (210 mg, 1.5 equiv. ) and HOAT (85 mg, 1.5 equiv. ) in DMF (1.5 ML), DIISOPROPYLETHYLAMINE (200, UL) is added at 4°C, and the reaction mixture stirred for 30 minutes at 4°C, followed by addition of 1- (2-AMINOETHYL)-4-TERT-BUTOXYCARBONYL- piperazine (127 mg, 1.5 equiv. ) in DMF (0.5 ml) at 4°C. The reaction mixture is stirred for 4 hours at room temperature, extracted with ethyl acetate and 0.5 N aqueous HCI solution, the organic layer washed with saturated aqueous NaHCO3 solution and brine, dried (MgSO4), the solvents evaporated and the residue chromatographed on SiO2 with ethanol/ethyl acetate (1: 6), to yield the title compound as an oil. MS: 618.2 [M+H] + ; H-NMR (300 MHz, DMSO-d6) : 8.72 (br. t, J=9, NH); 8.19 (s, 1 arom. H); 7.54 (s, 2 arom. H); 3.91 (s, 2 MEO) ; 3.76 (s, MeO) ; 3.5-3. 4 (m, 2H); 3.35-3. 25 (m, 4H); 2.6-2. 45 (m, 2H); 2.4-2. 35 (m, 4H); 1.8-1. 7 (m, 2H); 1.55-1. 4 (m, 2H); 1.40 (s, tBu); 1.35-1. 25 (m, 4H); 0.9-0. 8 (m, 3H).

192130-34-0, The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; APONETICS AG; WO2004/87679; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Analyzing the synthesis route of tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate

154590-35-9, The synthetic route of 154590-35-9 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.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

Sep 2021 News Brief introduction of 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

5747-48-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

A 1 liter round bottom flask equipped with stirring rod, thermo pocket, water condenser was charged with solution of l l-piperazinyldibenzo[b,f] [l,4]thiazepine in toluene 350 cc [63.0 g (0.22 moles)] and the mixture was stirred for 15 min 25- 30C, and was added sodium carbonate [41.0 gm (0.39 moles)], tetra butyl ammonium bromide [16.0 gm (0.05 mole)] and 2-(2-chloroethoxy)ethanol [32.0 gm (0.257 moles)] at room temperature. The reaction mixture was heated to reflux at 110- 112C. The reaction mixture was maintained at reflux for 10-12 hrs. The reaction mixture was analyzed by HPLC (to check for absence of compound of Formula IV) and was cooled to 25C to 30C. To which, was added 150 cc DM water, then the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 50 cc toluene. The extract and the organic layer were combined, to which was added 250 cc water and was acidified with acetic acid to obtain a pH of 2-3. The reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer washed with 100 cc toluene twice. To the aqueous layer was added 250 cc toluene, and the pH was adjusted to 8-10 using sodium carbonate, the reaction mixture was stirred for 30 min at 25-30C. The layers were separated and the aqueous layer extracted with 125 cc toluene. The extract and the organic layer were combined, to which was washed with DM (dimineralized) water 300 cc twice. The organic layer was distilled off under vacuum below 70C to afford 2-(2-(4-dibenzo[b,f]-[l,4] thiazepine-l l-yl-l-piperazinyl)ethoxy) ethanol. Purity of 2-(2-(4-dibenzo[b,fj-[l,4] thiazepine-l l-yl-l-piperazinyl)ethoxy) ethanol was 99.0% (area % by HPLC).

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2008/121415; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Sep 2021 News Downstream synthetic route of tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate

192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

0.14 g (0.61 mmol) of 1, 0.12 g (0.74 mmol) of 2 and 0.2 ml of 4-methylmorpholine are dissolved in 6 ml of DMF. 0.14 g (0.73 mmol) of N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide.x.HCl (DAPECI) and 0.1 g (0.74 mmol) of 1-hydroxybenzotriazole (HOBt) are then added. The mixture is stirred at RT for 18 h. The solvent is removed in a rotary evaporator, diluted with water (100 ml) and extracted 2.x. with EA. The organic phase is dried over magnesium sulfate, filtered off and evaporated to dryness, giving 0.21 g (92.3percent) of 3 as brown crystals.

192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; Staehle, Wolfgang; Schiemann, Kai; Schultz, Melanie; US2012/15959; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

22 Sep 2021 News Simple exploration of tert-Butyl 4-aminopiperazine-1-carboxylate

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

118753-66-5, To Compound 33 prepared as in Intermediate Example 1 (8.29 g, 41.2 mmol) and pyridine (6.0 mL, 74.2 mmol) in MeCN (120 mL) was added dropwise ethyl chloroformate (5.9 mL, 61.9 mmol). The resulting mixture was stirred at room temperature for 3 h, then partitioned between EtOAc and saturated aqueous NaHCO3, dried with Na2SO4, and concentrated in vacuo to yield a residue, which was used in the next step without further purification. MS 274 (M+1)+

118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference:
Patent; MACIELAG, Mark J.; Tennakoon, Manomi; US2009/275594; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics