Heterocyclic Building Blocks-piperazine

3022-15-9, Piperazine-2-carboxylic acid dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperazine-2-carboxyilc acid dihydrochloride (15.0 g, 73.9 mmol) was dissolved in H2O (240 mL) and 1,4-dioxane (360 mL), and the solution was brought to pH 10 with 6 N NaOH in H2O. Di-tert-butyldicarbonate (28.3 g, 162 mmol) was added while maintaining the pH at 10 with 6 N NaOH in H2O. After 2 h, the reaction mixture was extracted with Et2O (3 x 200 mL). The aqueous layer was brought to pH 3 with 6 N HCl and was extracted with EtOAc (4 x 300 mL). The combined EtOAc extracts were dried over Na2SO4, filtered, and concentrated under reduced pressure to give 14.45 g (59%) of the desired product as an off- white solid. The material was used without further purification. LC-MS: RT = 8.16 min; [M+Na]+ = 353.1.

3022-15-9, 3022-15-9 Piperazine-2-carboxylic acid dihydrochloride 2723757, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; CRITICAL THERAPEUTICS, INC.; WO2007/146066; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 solution of compound 3 (1 equiv) in 20 ml of ACN,NaI (1.2 equiv) was added and the mixture was refluxed for 30 min and cooled to room temperature. Subsequently,K2CO3 (1.2 equiv) and appropriate phenylpiperazine derivative(1.2 equiv) were added. Then the mixture was refluxedfor 4h. At the end of this period, the mixture was evaporatedto dryness then the product was solidified with ice-cold waterand crystallized from appropriate solvent.

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

Reference：
Article; Kilic, Burcu; Erdogan, Merve; Gulcan, Hayrettin O.; Aksakal, Fatma; Oruklu, Nihan; Bagriacik, Emin U.; Dogruer, Deniz S.; Medicinal Chemistry; vol. 15; 1; (2019); p. 59 – 76;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

[19121 Step 2: Synthesis of 1-(2.2.2-trifluoroethyl)piperazine[19131 Tert-butyl 4-(2,2,2-trifluoroethyl)piperzine- 1 -carboxylate (2.000 g, 7.455 mmol) was dissolved in methylene chloride (10 mL) / trifluoroacetic acid (5 mL) at room temperature, and the solution was stirred at the same temperature for 17 hours. The reaction mixture was concentrated under reduced pressure to remove the solvent, and the concentrate was crystallized from ethyl acetate (20 mL) at room temperature and filtered, and the resulting solid was washed with ethyl acetate and dried to afford the desired compound (0.457 g, 23.1 %) as a white solid.

692058-21-2, As the paragraph descriping shows that 692058-21-2 is playing an increasingly important role.

Reference：
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; SONG, Hyeseung; LEE, Changgon; KWAK, Dalyong; LEE, Jaeyoung; BAE, Suyeal; KIM, Yuntae; BAE, Daekwon; HA, Nina; BAE, Miseon; KIM, Jihyun; WO2015/137750; (2015); A1;,
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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.

A mixture of 5-chloro-2-nitroaniline (1.4 g, 8.1 mmol), l-(2-methoxy-iethyl)- piperazine (2.0 g, 14.0 mmol) and anhydrous potassium carbonate (1.38 g, 10.0 mmol) in N,N-dimethylacetamide (3 ml) was stirred at 120-130 C under nitrogen for 1 day. Sample NMR analysis showed complete conversion of the starting material. The resultant mixture was then cooled to room temperature, poured into cold water (15 ml) and stirred vigorously. The resulting yellow brown precipitate was collected by filtration, washed well with water then dried on the filter funnel. The resulting yellow brown solid was slurried in diethyl ether (20 mL) , filtered, washed with additional diethyl ether, dried to afford 5-[4-(2-memoxy-emyl)-piperaan-l-yl]-2-nitro-phenylamine (1.7 g, 75 %) as a yellow brown powder. NMR (400 MHz, DMSO-d6) delta 2.40-2.50, m, 6H; 3.19, s, 3H; 3.25, m, 4H; 3.41, t (J=5.9 Hz), 2H; 6.16, d (J=2.7 Hz), 1H; 6.34, dd (J=2.54, 7.23 Hz), 1H, 7.20 broad s , 2H; 7.76, d (J=9.8 Hz), 1H -, 13484-40-7

13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; PETER MACCALLUM CANCER INSTITUTE; MARTIN, Roger, Francis; WHITE, Jonathan; LOBACHEVSKY, Pavel; WINKLER, David; SKENE, Colin; MARCUCCIO, Sebastian; WO2011/123890; (2011); A1;,
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Piperazines – an overview | ScienceDirect Topics

1403898-64-5, (2R,5R)-tert-Butyl 5-(hydroxymethyl)-2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 18: (2R,5R)-4-{2-[6-(4-FI uoro-benzyl)-3,3-di methyl-2,3-di hydro-pyrrolo[3,2- b]pyridi n-I -yI]-2-oxo-ethyl}-5-hydroxymethyl-2-methyl-pi perazi ne-I -carboxylic acid tert-butyl esterFinely ground potassium iodide (7.5 g, 45.26 mmol) was added to a mixture of (2R,5R)-5-hydroxymethyl-2-methyl-piperazine-1-carboxylic acid teit-butyl ester (5.7 g, 24.89 mmol), 2-chloro- 1 -[6-(4-fluorobenzyl)-3, 3-dimethyl-2, 3-dihydro-pyrrolo[3,2-b]pyridin- 1 -yl]-ethanone hydrochloride (8.35 g, 22.63 mmol) potassium carbonate (12.5 g, 90.51 mmol) and acetonitrile (100 mL) under nitrogen. The mixture was stirred at 20 00 overnight. The mixture was partitioned between water (300 mL) and EtOAc (300 mL) and the organic phasewas dried and evaporated in vacuo to give the title compound (12.14 g). MS: [M+H] = 527.

1403898-64-5, As the paragraph descriping shows that 1403898-64-5 is playing an increasingly important role.

Reference：
Patent; ASTEX THERAPEUTICS LIMITED; CHESSARI, Gianni; JOHNSON, Christopher Norbert; PAGE, Lee William; BUCK, Ildiko Maria; DAY, James Edward Harvey; HOWARD, Steven; SAXTY, Gordon; MURRAY, Christopher William; WO2014/60770; (2014); A1;,
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Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of IV-l-c (28 mg, 0.1 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)benzenamine (22 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in 1.2 mL of /-BuOH was heated at 100 0C in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The dichloromethane was removed in vacuo and the resulting crude product was purified by reverse-phase prep-HPLC using a water (0.05% TFA)/acetonitrile (0.05% TFA) gradient to afford the title compound IV-I as TFA salt (20 mg). 1H NMR (600 MHz, CD3OD) 5 8.1 (s, IH), 7.78 (dd, J= 1.2, 7.8 Hz, IH), 7.71 (d, J= 7.2 Hz, IH), 7.57- 7.54 (m, IH), 7.28-7.23 (m, 2H), 6.76 (d, J= 2.4 Hz, IH), 6.67 (dd, J= 1.2, 8.4 Hz, IH), 3.92-3.86 (m, 5H), 3.66-3.60 (m, 2H), 3.46 (s, 3H), 3.45 (s, 3H), 3.28-3.24 (m, 2H), 3.14-3.06 (m, 2H), 2.97 (s, 3H). MS (ESI) m/z 460 (M+H)+., 122833-04-9

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

Reference：
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; DENG, Xianming; KWIATKOWSKI, Nicholas, Paul; WO2010/80712; (2010); A2;,
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Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1235865-77-6

4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide EXAMPLE 5K (3.39 g), EXAMPLE 5A (1.87 g), 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2Cl2 (40 mL) for 24 hours. The reaction was cooled and chromatographed on silica gel with 25-100% ethyl acetate/hexanes, then 10% methanol/ethyl acetate with 1% acetic acid, to give the product (1.62 g, 32%) as a white solid. 1H NMR (300 MHz, dimethylsulfoxide-d6) 11.65 (brs, 1H), 8.55 (br s, 1H), 8.04 (d, 1H), 7.89 (dd, 1H), 7.51 (m, 3H), 7.33 (d, 2H), 7.08 (m, 1H), 7.04 (d, 2H), 6.68 (dd, 1H), 6.39 (d, 1H), 6.19 (d, 1H), 3.84 (m, 1H), 3.30 (m, 4H), 3.07 (m, 4H), 2.73 (m, 2H), 2.18 (m, 6H), 1.95 (m, 2H), 1.61 (dd, 2H), 1.38 (m, 2H), 1.24 (m, 4H), 0.92 (s, 6H).

The synthetic route of 1235865-77-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ABBOTT LABORATORIES; US2010/305122; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

An amount of 120 mg (0.26 mmol) of 4-(4-chlorobutyl)-9-(2,4-dichloroanilino)-3,4-dihydro-2H-[1,4]oxazino[2,3-g]quinoline-8-carbonitrile was stirred in N,N-dimethylformamide (0.8 mL), and to this were added sodium iodide (55 mg, 0.36 mmol), tetrabutylammonium iodide (58 mg, 0.16 mmol), and 1-ethylpiperazine (0.26 mL, 2.1 mmol). The mixture was heated at 50C for three hours, after which an additional amount of 1-ethylpiperazine (0.26 mL, 2.1 mmol), was added. The mixture was heated at 60C for 3 hours, and subsequently evaporated to a yellow oil, stirred with saturated sodium bicarbonate solution, and extracted with dichloromethane. The organic layer was washed with saturated brine solution, dried over sodium sulfate, and evaporated to a yellow oil. Purification was performed by flash chromatography (10% acetone in dichloromethane, then 70:30:5 = dichloromethane: methanol: ammonium hydroxide), to give a yellow solid (74 mg, 53% yield), m.p 97-98C;1H NMR (DMSO-d6) delta 9.21 (s, 1H), 8.27 (s, 1H), 7.73 (d, 1H), 7.68 (s, 1H), 7.42 (dd, 2H), 6.70 (s, 1H), 4.27 (t, 2H), 3.49 (m, 4H), 2.31 (m, 12H), 1.62 (dd, J = 7 Hz, 2H), 1.52 (dd, J = 7 Hz, 2H), 0.97 (t, 3H); [] Analysis for C28H32Cl2N6O·0.3 CH3CO2C2H5 ·1 H2O FoundC, 60.29;H, 5.94;N, 14.76.CalcdC, 60.00;H, 6.23;N, 14.38.

As the paragraph descriping shows that 5308-25-8 is playing an increasingly important role.

Reference：
Patent; Wyeth; EP1268487; (2003); B1;,
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

Step 1 : DIPEA (879 mu, 5.17 mmol) was added to 5-bromo-2-chloropyrimidine Ex.10a (500 mg, 2.56 mmol) in acetonitrile (12 mL). Then, benzyl piperazine-1-carboxylate (500 mu, 2.56 mmol) was added to the mixture. The reaction mixture was stirred at r.t. for 60h. Water and EtOAc were added. The two phases were separated and the aqueous solution was extracted with EtOAc. The combined organic layers were dried over MgSO4, filtered and the solution was concentrated to dryness. The crude material was purified by column chromatography on silica gel eluting with Heptane/EtOAc from [100:0] to [0:100]. The product fractions were combined and concentrated to dryness to afford benzyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate Ex.10a (858 mg, 88percent) as white solid.

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

Reference：
Patent; GENFIT; DELHOMEL, Jean-Francois; PERSPICACE, Enrico; MAJD, Zouher; PARROCHE, Peggy; WALCZAK, Robert; BONNET, Pascal; FOGHA, Jade; (76 pag.)WO2018/138356; (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.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

To a stirring solution of compound 2 (1 g, 2.91 mmol) in dry THF (20 mL) were added LiHMDS (1.0 M in THF) (10.2 mL, 10.2 mmol), paraformaldehyde (69 mg, 2.32 mmol) at -78 C under nitrogen atmosphere. The reaction mixture was brought to RT and stirred for 16 h. After consumption of the starting material (by TLC), the reaction was quenched with ice water (20 mL) and extracted with EtOAc (2 x 50 mL). The combined organic layer was washed with brine solution (2 x 10 mL), dried over Na2S04 and concentrated to obtain crude compound which was purified by column chromatography by eluting 30% EtOAc/ hexanes to afford racemic EE (320 mg, 32%) as white solid. The racemic was separated by chiral HPLC purification to give 75mg each of EE-1 and EE-2. EE-1: 1H-NMR: (400 MHz, DMSO-d6): delta 7.98 (s, 1H), 3.78 (d, / = 12.8 Hz, 1H), 3.67-3.60 (m, 1H), 3.51 (d, / = 13.6 Hz, 1H), 3.41-3.30 (m, 4H), 3.07 (br s, 1H), 1.39 (s, 18H). LCMS (ESI): m/z 340.1 [M+-l]; UPLC: 99.74% EE-2: 1H-NMR: (400 MHz, DMSO-ifc): delta 7.99 (s, 1H), 3.78 (d, / = 12.8 Hz, 1H), 3.65-3.61 (m, 1H), 3.51 (d, / = 13.6 Hz, 1H), 3.40-3.30 (m, 4H), 3.07 (br s, 1H), 1.39 (s, 18H). LCMS (ESI): m/z 340.1 [M+-l]; UPLC: 99.04%, 171504-98-6

The synthetic route of 171504-98-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; APTINYX INC.; KHAN, M., Amin; (75 pag.)WO2018/26782; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics