Heterocyclic Building Blocks-piperazine

5308-25-8, 1-Ethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 4 Preparation of 1-ethyl-4-(6-nitropyridin-3-yl)piperazine A mixture of 5-bromo-2-nitropyridine (1.02 g, 5.02 mmol) and 1-ethylpiperazine (1.71 g, 15.0 mmol) in N-methyl-2-pyrrolidinone (5 mL) was stirred at 120 C. for 3 h. After this time, the reaction was cooled to room temperature, poured into water (100 mL) and extracted with methylene chloride (2*100 mL). The combined organic layers were dried over sodium sulfate, filtered and the filtrate concentrated under reduced pressure. The resulting residue was purified by chromatography (silica, gradient, 1:49 methanol/methylene chloride to 1:9 methanol/methylene chloride) to afford 1-ethyl-4-(6-nitropyridin-3-yl)piperazine as a yellow solid: 1H NMR (400 MHz, DMSO-d6.) d 8.25 (d, J=2.8 Hz, 1H), 8.14 (d, J=9.2 Hz, 1H), 7.48 (dd, J=9.2, 2.8 Hz, 1H), 3.50-3.46 (m, 4H), 2.50-2.38 (m, 4H, merged with DMSO peak), 2.37 (q, J=7.2 Hz, 2H), 1.02 (t, J=7.2 Hz, 3H)., 5308-25-8

The synthetic route of 5308-25-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Gilead Connecticut, Inc.; Blomgren, Peter A.; Currie, Kevin S.; Kropf, Jeffrey E.; Lee, Seung H.; Mitchell, Scott A.; Schmitt, Aaron C.; Xu, Jianjun; Zhao, Zhongdong; US2014/148430; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

4-[2-(4-tert-butoxycarbonylpiperazin-1-yl)thiazol-4-ylmethoxy]benzoic Acid A solution of tert-butyl 4-thiocarbamoylpiperazine-1-carboxylate (650 mg, 2.65 mmol) and 1,3-dichloroacetone (672 mg, 5.3 mmol) in 1,2-dichloroethane was treated with sodium bicarbonate (22 mg, 2.65 mmol). The reaction mixture was stirred at 70 C. for 18 hours and then diluted with chloroform. The dilution was washed with water and brine, dried over sodium sulfate and concentrated. Product was purified from the residue on a silica gel column, using ethyl acetate/hexanes (317) as eluent, to provide tert-butyl 4-(4-chloromethylthiazol-2-yl)piperazine-1-carboxylate (830 mg, 100% yield). H-NMR (dmso-d6): 6.92 (1H, s), 4.57 (2H, s), 3.40 (8H, m), 1.42 (9H, s)., 196811-66-2

196811-66-2 tert-Butyl 4-carbamothioylpiperazine-1-carboxylate 12093220, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; AXYS PHARMACEUTICALS, INC.; US2002/86996; (2002); A1;,
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262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To N, N-dimethylformamide (1000 ml) were added methyl 2-oxindole-6-carboxylate (100.0 g), benzoic acid methyl ester (78.3 g) and potassium carbonate (180.7 g) were added and stirred at room temperature for 3 hours. N- (4-aminophenyl) -N-methyl-2- (134.5g). After stirring at room temperature for 4 hours, the reaction mixture was poured into water (3000ml), stirred for 30 minutes, filtered and recrystallized from methylene chloride / methanol (10: 4 by volume) and dried to give 257.8g of crystals Compound. (89.7% yield).

262368-30-9, The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Beijing Kanglisheng Pharmaceutical Development Co., Ltd.; Cheng Gang; (12 pag.)CN104844499; (2017); B;,
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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: To a solution of carboxylic acid (50 mmol) in DMF (0.25 mL) in a 48 position Mettler Toledo XT reaction block was added PyBOP (50 mmol, 0.2 mL of 0.3 M solution in DMF) and TEA (75 mmol, 0.05 mL of 1.5 M solution in DMF) followed by the appropriate amine build blocks (55 mmol, 0.55 ml of 1 M solution in DMF). The reactions were stirred at rt 24 h and concentrated by GeneVac HT-4 to remove all reaction mixture including excess amine and DMF. The crude mixtures were dissolved in EtOAc (1 mL) and filtered through silica-packed short-column and washed with EtOAc (3 mL). The collected organic solution was concentrated in GeneVac HT-4 and dissolved in DMSO (1 mL). DMSO solution was subjected to HTAC for pre-purification analysis, purification, and final QC., 30459-17-7

As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference：
Article; Hwang, Jong Yeon; Attia, Ramy R.; Carrillo, Angela K.; Connelly, Michele C.; Guy, R. Kiplin; Bioorganic and Medicinal Chemistry Letters; vol. 23; 6; (2013); p. 1891 – 1895;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109-07-9,2-Methylpiperazine,as a common compound, the synthetic route is as follows.

1-(t-Butoxycarbonyl)-3-methylpiperazine To a cold (-5° C.) solution of 2-methylpiperazine (5.00 g, 0.05 mole) in 200 mL of CH2 Cl2 under Ar was added a solution of di-t-butyl dicarbonate (10.9 g, 0.05 mole) in 100 mL of CH2 Cl2 over 1 h. The resulting mixture was stirred at -5° C. for 1 h and then at r.t. for 2 h. The solution was then washed (H2 O), dried (Na2 SO4) and evaporated to give an oil which was chromatographed (SiO2 /ethyl acetate then ethyl acetate-MeOH-NH4 OH 10:1:0.1) to give the product (4.30 g, 43percent) as an oil. This material was used without further purification: 1 H nmr (200 MHz, CDCl3) delta 4.15-3.75 (br s, 2H), 3.0-2.6 (m, 4H), 2.47-2.35 (m, 1H), 1.48 (s, 9H), 1.08 (d, J=6.7 Hz, 3H).

109-07-9, The synthetic route of 109-07-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; US5434154; (1995); A;,
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Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A NaOEt solution, prepared from sodium hydride (60% dispersion in mineral oil) (0.990 g, 26 mmol) and 100 mL EtOH, diethyl carbonate (9.00 mL, 74 mmol) and (S)-4-N-BOC-2-hydroxymethyl-piperazine (2.17 g, 10 mmol) was heated at 80 C. The reaction was cooled to RT and filtered. The filtrate was concentrated to dryness to give an off-white amorphous solid.

314741-40-7, 314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Amgen Inc.; US2006/199817; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (0.25g, 0.53mmol), 1-Boc-2- piperazine carboxylate(157mg, 0.64mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide Hydrochloride (153mg, 0.80mmol)and N- hydroxy-7-aza-benzotriazole (181mg, 1.33mmol) was dissolved in dichloromethane (20mL) Theconditions at 0 C to this solution was added dropwise N, N- diisopropylethylamine (0.37mL, 2.13mmol), 5Hstirred at room temperature, the solvent was removed, Concentrate was separated by column chromatography(eluent: Petroleumether / EtOAc (v / v) = 3/1), to give 260mg colorless viscous substance, yield: 70.

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.

Example 18; iV”-(2-Ammophenyl)-4-(3-chloro-5-{[4-(2-methoxyethyl)piperazin-l-yl]niethyl}pyridin-2- yl)benzamide; A solution of tert-bvyl (2-{[4-(3-chloro-5-formylpyridin-2- yl)benzoyl]amino}phenyl)carbamate (Method 1; 181 mg, 0.40 mmol) in dichloromethane (4 ml) was added to l-(2-methoxyethyl)piperazine (102 mg, 0.70 mmol). The reaction mixture was stirred for 5 minutes before addition of titanium (IV) isopropoxide (240 mul, 0.8 mmol). The reaction was allowed to stir at ambient temperature for 2 hours then sodium borohydride (61 mg, 1.60 mmol), added followed by methanol (0.4 ml). The reaction mixture was stirred for 2 hours then a further portion of sodium borohydride (61 mg, 1.60 mmol) added the reaction mixture was left to stir overnight (20 hours). Saturated aqueous sodium hydrogencarbonate solution (5 ml) was added, followed by water (5 ml) and dichloromethane (5 ml). The mixture was stirred for 30 minutes and the organic phase separated by filtration through an 1ST phase separating cartridge, and the aqueous extracted again with dichloromethane. The combined organic extracts were evaporated to dryness and the residue purified by flash chromatography on silica eluting with ethyl acetate followed by a rising gradient of methanol in ethyl acetate (0-20% v/v) to afford the protected product. This was taken up in dichloromethane (3 ml) and treated with trifiuoroacetic acid (1 ml) then at ambient temperature for 22 hrs. The reaction mixture was diluted with dichloromethane and poured onto an SCX-2 cartridge (5g). The cartridge was washed with dichloromethane (25 ml) and methanol (50 ml) before eluting products with a 2M solution of ammonia in methanol (50 ml). The ammoniacal fraction was evaporated to dryness and the resultant residue triturated with diethyl ether/isohexane to afford the title compound (78 mg, 41%); MMR Spectrum: (CDCl3) delta 2.61 (m, 10H), 3.35 (s, 3H), 3.53 (t, 2H), 3.58 (s, 2H), 3.88 (s, 2H), 6.87 (m, 2H), 7.11 (m, IH), 7.38 (d, IH), 7.84 (d, 2H), 7.88 (s, 2H), 8.00 (d, 2H), 8.53 (s, IH); Mass Spectrum: M+H+ (35Cl) 480.

13484-40-7, The synthetic route of 13484-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/75160; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of bromide 61 (180 mg, 0.5 mmol), Cu20 (8 mg, 0.1 eq.) and 1 -Z-piperazine (0.5 mL, 2.5 mmol) in water (1 .0 mL) was stirred in a seal tube at 100 °C for 18 h. The reaction was cooled and the residue was extracted with EtOAc (3 x 25 mL). The combined organic layers were dried on MgS04, filtered and concentrated in vacuo. The crude reaction mixture was purified by flash column chromatography on silica gel [DCM/MeOH (2percent MeOH)] to give 89 as colourless solid (220 mg, 89percent), which was used in the next step without further purification. (0603) 1H NMR (500 MHz, CDCU, deltaEta): 7.37-7.30 (m, 5H, Ar), 5.74 (d, J = 2.5 Hz, 1 H, C3-H), 5.64 (s, 1 H, C5-H), 5.16 (s, 2H, CH2-Ph), 4.39-4.06 (m, 3H, C7-H, C1 1 -H, C12-H), 3.77 (dd, J = 15.0, 6.0 Hz, 1 H, C7-H), 3.60 (m, 4H, C13-H), 3.27 (m, 4H, C14-H), 3.01 (m, 2H, C1 1 -H C12-H), 2.87 (s, 1 H, C10-H), 2.35 (s, 1 H, C8-H), 1 .97 (d, J = 12.5 Hz, 1 H, C9-H), 1 .89 (d, J = 12.5 Hz, 1 H, C9-H), 1 .40-1 .18 (s, 9H, Boc); 13C NMR (125 MHz, CDCI3, 5C): 164.3 (CO), 156.4 (CO), 155.1 (CO), 154.6 (C4), 148.3 (C6), 136.4 (Ar), 128.5 (2C, Ar), 128.1 (Ar), 127.9 (2C, Ar), 96.4 (C3), 95.0 (C5), 80.1 (q Boc), 67.7 (CH2-Ph), 50.6, 50.5 (C1 1 , C12), 47.9 (C7), 46.1 (2C, C13), 43.1 (2C, C14), 35.4 (C10), 28.1 (3C, Boc), 27.7 (C8), 26.5 (C9); HRMS (ESI+): calculated for C28H37N4O5: 509.2758, found [M+H]+: 509.2733.

31166-44-6, 31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; THE UNIVERSITY OF BRISTOL; GALLAGHER, Timothy Charles; REGO CAMPELLO, Hugo; (154 pag.)WO2018/33742; (2018); A2;,
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Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DECP (5.9 ml; 0.0395 mol) was added to a stirring solution of l-(l,l-dimethylethyl)-4- (4-carboxyphenyl)-l-piperazinecarboxylic acid ester (10 g; 0.0326 mol) and 4- methoxybenzylamine (4.7 ml; 0.036 mol) in Et3N (9.2 ml; 0.0655 mol) and CH2Cl2 (250 ml). The reaction mixture was stirred at room temperature for 18 hours. Saturated NaHCO3 solution (150 ml) was added and the mixture was stirred for 30 minutes. Then H2O (100 ml) was added and the mixture was stirred for 30 minutes. The layers were separated and CH2Cl2-layer was dried with MgSO4, evaporated, co-evaporated with toluene and dried at 50 0C in vacuum for 3 hours. Yield : 15.21 g of intermediate 53 (107 %)., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; JANSSEN PHARMACEUTICA N.V.; WO2008/148868; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics