Heterocyclic Building Blocks-piperazine

196811-66-2, tert-Butyl 4-carbamothioylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-chloro-l-(4,5-dihydro-5-phenyl-3-isoxazolyl)ethanone (i.e. the product of Step C) (0.450 g, 2.018 mmol) and 1,1-dimethylethyl 4-(amino-thioxomethyl)-l- piperazinecarboxylate (i.e. the product of Step A) (0.5 g, 2.04 mmol) in ethanol (10 mL) was added triethylamine (0.204 g, 2.013 mmol), and the reaction mixture was stirred at room temperature for 12 h. The reaction mixture was concentrated under reduced pressure, and the residue was partitioned between ethyl acetate (30 mL) and water (30 mL). The organic layer was separated and washed with brine (25 mL), dried (Na2S04), and concentrated under reduced pressure. The crude residue was purified by column chromatography using 20% ethyl acetate in petroleum ether as eluant to give 700 mg of the title compound as a white solid..H NMR (CDCI3) delta 1.48 (s, 9H), 3.30 (m, 1H), 3.54 (m, 8H), 3.74 (m, 1H), 5.71 (m, 1H), 6.91 (s, 1H), 7.40-7.29 (m, 5H).

196811-66-2, The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; E. I. du Pont de Nemours and Company; DUNG, Mei H.; PASTERIS, Robert, James; WO2011/72207; (2011); 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.

To a solution of N-1-Boc-2-piperazinecarboxylic acid methyl ester (CAS Reg. No: [129799-15-1]) (1 g) in DMF (5 mL) was added 3-chlorobenzenesulfonyl chloride (0.95 g) and triethylamine (1.71 mL). The reaction mixture was stirred at RT overnight. Water was added and the mixture was extracted with ethyl acetate (x2). The combined organic layers were washed with water (×2) and brine, were dried (Na2SO4), filtered and evaporated. Purification by chromatography (SiO2, n-heptane/ethyl acetate 3:1) yielded 4-(3-chloro-benzenesulfonyl)-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester as white foam (1.66 g), MS: 436.3 ([M+NH4, 1Cl]+)., 129799-15-1

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

Reference：
Patent; Dehmlow, Henrietta; Kuhn, Bernd; Sander, Ulrike Obst; Roever, Stephan; Schulz-Gasch, Tanja; Wright, Matthew; Wyler, Rene; US2009/48264; (2009); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 3-bromobiphenyl (0.70 g, 3.00 mmol) in toluene (10 mL) was added t-butyl 2-methylpiperazine-l-carboxylate (0.720 g, 3.60 mmol), potassium t- butoxide (0.504 g, 4.50 mmol), tris(dibenzylideneacetone)dipalladium(0) (0.090 g, 98.3 mmol) and tri-t-butylphosphine (0.018 g, 89.0 mmol). The mixture was heated at 90 C for 5 hours. At this time the reaction was cooled, diluted with water and extracted with ethyl acetate. The combined extracts were washed with brine, dried (Na2S04) and concentrated. The residue was purified by flash chromatography over silica using a hexane/ethyl acetate eluant to afford t-butyl 4-([l, -biphenyl]-3-j/j-2-methylpiperazine- 1-carboxylate (0.750 g, 71%) as a brown oil. The t-butoxycarbonyl protecting group was removed from this compound using General Procedure G to afford l-([l,l’-biphenyl]-3- yl)-3-methylpiperazine. This intermediate was, in turn, was reacted with Intermediate 5 using General Procedure A to generate the title compound. 1H NMR (500 MHz, CDCI3) delta 7.60-7.34 (m, 6H), 7.12-7.11 (m, 2H), 6.92-6.90 (m, 1H), 4.40-4.39 (d, J= 6.5 Hz, 1H), 4.19-4.14 (m, 1H), 3.87-3.33 (m, 4H), 3.09-2.88 (m, 8H), 2.46-2.43 (m, 1H), 1.99-1.55 (m, 9H), 1.38 (t, J = 7.0 Hz, 3H) ppm. 13C NMR (125 MHz, CDC13) delta 156.7, 156.7, 151.9, 142.5, 141.6, 129.5, 128.7, 127.3, 127.2, 119.1, 115.4, 115.4, 115.3, 115.3, 59.0, 54.3, 54.3, 53.2, 53.3, 49.1, 49.1, 47.9, 47.8, 47.7, 47.7, 46.1, 46.0, 39.8, 39.5, 39.1, 39.0, 36.7, 36.4, 25.9, 25.8, 25.4, 24.3, 24.3, 24.1, 24.0, 15.8, 15.7 ppm. Purity: >99% (214 & 254 nm) LCMS; retention time: 1.29 min; (M+H+) 433.3

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GENZYME CORPORATION; BOURQUE, Elyse; CABRERA-SALAZAR, Mario, A.; CELATKA, Cassandra; CHENG, Seng, H.; HIRTH, Bradford; GOOD, Andrew; JANCSICS, Katherine; MARSHALL, John; METZ, Markus; SCHEULE, Ronald, K.; SKERLJ, Renato; XIANG, Yibin; ZHAO, Zhong; LEONARD, John; NATOLI, Thomas; MAKINO, Elina; HUSSON, Herve; BESKROVNAYA, Oxana; WO2014/43068; (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.57260-70-5,tert-Butyl 4-benzylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound lOA was treated with 30 mL EA solution of HCl (1 M) and stirred at rt for18.5 hrs. The mixture was concentrated in vacuo to give about 135 mg of 1-benzylpiperazine(Compound lOB) as a white solid which was used directly in the next step. MS: calc’d 177(M+Ht, measured 177 (M+Ht.

57260-70-5, The synthetic route of 57260-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; WANG, Lisha; YUN, Hongying; ZHANG, Weixing; ZHU, Wei; ZHANG, Zhiwei; (69 pag.)WO2017/202704; (2017); A1;,
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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: The mixture of intermediate 2 (267 mg, 1.0 mmol), co-responding amines and Zn(ClO4)2. 6H2O (7.4 mg, 2.0 mol %) in dichloromethane (5 mL) was stirred at room temperature under argon. After completion of the reaction, the mixture was diluted with water and extracted with dichloromethane(3×30 mL). The combined dichloromethane was dried over anhydrous sodium sulfate and solvent was removed under reduced pressure to give target compounds 6a-n (Table 2) which were purified by column chromatography eluting with chloroform : methanol., 30459-17-7

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

Reference：
Article; Van Chinh, Luu; Anh, Le Duc; Nga, Nguyen Thi; Ly, Nguyen Thi Hai; Ha, Vu Thi; Toan, Tran Quoc; Cuong, Nguyen Manh; Vu, Tran Khac; Letters in Organic Chemistry; vol. 14; 8; (2017); p. 603 – 611;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.,54699-92-2

Example 11; Synthesis of Active Esters Of N-Methyl Piperazine Acetic Acid Via Oxalyl Chloride (Scheme B, FIG. 4B); To a suspension of N-methyl piperazine acetic acid (N-MPAA) (79 mg, 0.5 mmol) in DCM (25 mL) was added a solution of oxalyl chloride (4 mL, 0.8 mmol, 2.0 M solution in DCM) over 10 minute at room temperature. After another 30 minutes of reaction, solvent and excess reagent were removed under reduced pressure to give a white solid (23). A solution of NHS (57 mg, 0.5 mmol) in DCM (25 mL) was added to the solid followed by ss-TBD (390 mg, 1 mmol, 2.6 mmol/g). The resulting solution was sonicated for 5 minute when all solid dissolved. The ss-TBD resin was removed by filtration and solvent was evaporated to yield a white foam (97% yield). Product was characterized by ES-MS as before.

The synthetic route of 54699-92-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Applera Corporation.; US2005/148773; (2005); A1;,
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Piperazines – an overview | ScienceDirect Topics

183742-34-9, 4-Boc-1-Fmoc-2-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-(l-(((9Eta-fluoren-9-yl)methoxy)carbonyl)-4-(ter?- butoxycarbonyl)piperazin-2-yl)acetic acid (5 g, 10.72 mmol) in dichloromethane (100 mL) with Lambda/,Lambda/-dimethylformamide (2 drops) was added oxalyl dichloride (3.4 g, 26.8 mmol). The reaction mixture was stirred at room temperature for 1 hour, then concentrated. Tetrahydrofuran (100 mL) was added to the concentrate followed by the slow addition of a solution containing 2-bromo-6-fluoroanaline (3 g, 16 mmol) and diisopropylethylamine (9 mL) in tetrahydrofuran (20 mL). The solution was stirred at room temperature for 2 hours before the addition of piperazine (2.77 g, 32.2 mmol) after which the solution was stirred for 15 hours. The reaction mixture was concentrated onto silica gel and purified via flash chromatography (0-100 % ethyl acetate/hexane, then 0-10 % methanol/dichloromethane) to afford the title compound. 1H NMR (300 MHz, DMSO-J6) delta ppm 7.47 – 7.65 (m, 1 H) 7.21 – 7.46 (m, 2 H) 3.55 – 4.05 (m, 2 H) 2.67 – 3.14 (m, 3 H) 2.49 – 2.67 (m, 2 H) 2.26 – 2.46 (m, 2 H) 1.39 (s, 9 H); MS (APCI+) m/z 418.2 (M+H)+.

183742-34-9, As the paragraph descriping shows that 183742-34-9 is playing an increasingly important role.

Reference：
Patent; ABBOTT LABORATORIES; ABBOTT GMBH &; CO. KG; WANG, Ying; BREWER, Jason, T.; AKRITOPOULOU-ZANZE, Irini; DJURIC, Stevan, W.; POHLKI, Frauke; BRAJE, Wilfried; RELO, Ana-Lucia; WO2010/124042; (2010); A2;,
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934-98-5, 2-(4-Methylpiperazin-1-yl)ethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The chloropteridine from above was dissolved in n-butanol (50 mL) and N-methyl- N’-(2-aminoethyl)piperazine (2.0 gm, 1.4 X 10″2 moles) was added. This mixture was heated at 110°C. for 30 minutes. TLC (silica, 25percent methanol in methylene chloride) showed a single, blue fluorescent, product at Rf = 0.093. The n-butanol was removed under reduced pressure and the residual material was extracted by stirring in diethyl ether (50 mL). This mixture was filtered and the solid filtercake was washed with diethyl ether (100 mL). The combined filtrates were extracted with water (50 mL). These aqueous extracts were treated with potassium carbonate to precipitate the product as an oil. The product was extracted into methylene chloride (100 mL). After drying over magnesium sulfate the methylene chloride solution was filtered and evaporated under reduced pressure. The remaining solid (1.28 gm) was dissolved in methanol (40 mL) and the solution was heated to reflux. Concentrated hydrochloric acid (982mu) was added and the solution was cooled on ice. The hydrochloride salt of Example 57 crystallized and was isolated by filtration. After being washed with methanol followed by diethyl ether, the solid was dried to give the product as its hydrochloride salt in a yield of 950 mg. LC/MS: M+l = 448.45, 934-98-5

934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; JANUS BIOTHERAPEUTICS, INC.; LIPFORD, Grayson, B.; ZEPP, Charles, M.; WO2012/167046; (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.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.

A mixture of compound 3 (306 mg, 1 mmol), tert-butyl 2-amino-4-(thiophen-2-yl)phenylcarbamate (260 mg, 0.9 mmol) and 1 -(3-dimethylaminopropyl)-3-ethylcar- bodiimide hydrochloride (573 mg, 3 mmol) in pyridine (15 mE) was stirred at room temperature for overnight. The mixture was poured into water (100 mE), filtered to obtain compound 4 (442 mg, 85%) as a yellow solid., 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; Regenacy Pharmaceuticals, LLC; van Duzer, John H.; Mazitschek, Ralph; (123 pag.)US2018/141923; (2018); 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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Into a 100-mL round-bottom flask, purged and maintained with an inert atmosphere of nitrogen, was added tert-butyl (4-bromophenethyl)carbamate (4,00 g, 13.3 mmol) and anhydrous toluene (50 mL). To the resulting solution was added benzyl piperazine-1- carboxylate (3.53 g, 16.0 mmol), Pd(OAc)2 (300 mg, 1.34 mmol), XPhos (1.28 g, 2.69 mmol), and CsiCO, (13.1 g, 40.0 mmol). The reaction mixture was stirred overnight at 105 °C in an oil bath and then cooled to RT and quenched by the addition of H20 (200 mL). The resulting mixture was extracted with ethyl acetate (2 x 50 mL). The combined organic layers were washed with brine (1 x 200 mL), dried over anhydrous sodium sulfate, filtered, and concentrated in vacuo. The crude product was purified by FCC eluting with ethyl acetate/petroleum ether (PE/EA=3 : 1) to afford benzyl 4-(4-(2-((fert-butoxycarbonyl)amino)ethyl)phenyl)piperazine-l- carboxylate as a yellow solid (5 g, 85percent), LCMS (ESI, m/z) 440 [M+H]+

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; FORMA THERAPEUTICS, INC.; GUERIN, David Joseph; BAIR, Kenneth W.; CARAVELLA, Justin A.; IOANNIDIS, Stephanos; LANCIA, JR., David R.; LI, Hongbin; MISCHKE, Steven; NG, Pui Yee; RICHARD, David; SCHILLER, Shawn E.R.; SHELEKHIN, Tatiana; WANG, Zhongguo; (113 pag.)WO2017/139779; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics