Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.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,as a common compound, the synthetic route is as follows.

Compound 22 (0.10 g, 0.18 mmol), Compound 16 (0.055 g, 0.18 mmol), 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC, 0.052 g, 0.27 mmol)And 4-dimethylaminopyridine (DMAP, 0.044 mg,0.36 mmol) was added to a solution of dichloromethane (20 ml) and stirred at room temperature for 10 h. The reaction was quenched with water (10 mL). Dry over anhydrous sodium sulfate, remove the solvent, The concentrate was subjected to column separation (eluent: ethyl acetate/methanol (v/v) = 30:1), Obtained 50 mg of a yellow solid, The yield was 33%., 1235865-77-6

As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference£º
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Liu Zhiqiang; (35 pag.)CN108658983; (2018); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.

5271-27-2, General procedure: A mixture of 3 (2.91 g, 10 mmol), 4 (1.76 g, 10 mmol)and KF (18 mmol) were heated at 120-130 ¡ãC in DMF (30mL) for 16 – 18 h. At the end of this period, the reactionmixture was cooled to room temperature and diluted withwater (30 mL). The separated solid was filtered, washed anddried to obtain crude 6a-i. The obtained crude product wasthen purified by recrystallization using ethanol.

5271-27-2 1-Methyl-3-phenylpiperazine 2760009, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Darsi, S.S. Praveen Kumar; Kumar, K. Shiva; Devi, B. Rama; Naidu; Dubey; Letters in Organic Chemistry; vol. 11; 8; (2014); p. 551 – 555;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

A solution of 1 mol of N-hydroxyethylpiperazine and 40% (by mass) of aqueous potassium vinylsulfonate (containing 1.05 mol of ethylene Potassium sulfonate) was added to a 1000 mL four-necked flask equipped with a reflux tube and the addition reaction was carried out with sufficient stirring. The reaction was carried out at 50 C Should be heated for a period of 1.5 hours and then gradually heated to reflux and continue to react for 2.0 hours; then, the resulting solution containing 4-hydroxyethylpiperazine Reaction of potassium ethanesulfonate. The yield of potassium 4-hydroxyethylpiperazine ethanesulfonate was calculated by high performance liquid chromatography (HPLC) 95.1%.A reaction mother liquor containing 0.5 mol HEPES-K at a mass concentration of 35 wt% was placed in a 500 mL beaker,Under stirring,25.0 g of concentrated sulfuric acid (98 wt%) was slowly added dropwise at room temperature,Then stir,At 40 C,Acidification for 1 hour.Into the low temperature thermostat,Cooling to -20 ,Cooling crystallization for 0.5 hours,Removal of potassium sulfate by filtration.The filtrate was placed in a beaker,Constantly stirring,4.0 g of Ca (OH) 2 was slowly added,Reaction for 1 hour,Remove the remaining sulfate.Adding 5 g of activated carbon decolorization and filtering by filtration to obtain the filtrate,By rotary evaporation to anhydrous,To obtain a solid primary purified product.The solids were washed twice with 500 ml of methanol,500ml ethanol once,And then vacuum drying,Get high purity HEPES.

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shandong University of Technology; Cui Hongyou; Wang Jiangang; Zhu Liwei; Liu Ransheng; Yang Yong; Wang Yang; (8 pag.)CN104803949; (2017); B;,
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31166-44-6, 1-Cbz-Piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0512] Benzyl piperazine-1-carboxylate 23 (27 .3 mL,142.2 mmol) was dissolved in dry THF (313.1 mL) andoxetan-3-one (12.29 g, 10.93 mL, 170.6 mmol) was added.The resulting solution was cooled in an ice-bath. NaBH(Oac )3 (59.99 g, 284.4 mmol) was added portionwise over 30mins, about a quarter was added. Mixture removed from icebath, allowed to warm to room temperature then continuedadding the NaBH(Oac )3 portionwise over 30 mins. On completeaddition, an exotherm from 22¡ã C. slowly to 32¡ã C. wasobserved, whereby the mixture was subsequently cooled onan ice bath until an internal of 22¡ã C. was reached. The icebath was removed and the reaction mixture’s internal tempwas steady at 22¡ã C. The mixture was stirred at room temperatureovernight. [0513] The resulting white suspension was quenched byaddition of 2M sodium carbonate solution (approx 150 mL)(pH=8) and concentrated under reduced pressure to removeTHF. Product was then extracted with EtOAc (3×250 mL).Organics were combined, dried over MgS04 , filtered andconcentrated under reduced pressure to leave product 24 as awhite solid (32.7 g 83percent yield). 1H NMR (500 MHz, DMSOd6)o 7.39-7.30 (m, 5H), 5.07 (s, 2H), 4.52 (t, 2H), 4.42 (t,2H), 3.43-3.39 (m, 5H) and 2.22 (t, 4H). MS (ES+) 276.8., 31166-44-6

As the paragraph descriping shows that 31166-44-6 is playing an increasingly important role.

Reference£º
Patent; Charrier, Jean-Damien; Davis, Christopher John; Fraysse, Damien; Etxebarria I Jardi, Gorka; Pegg, Simon; Pierard, Francoise; Pinder, Joanne; Studley, John; Zwicker, Carl; Sanghvi, Tapan; Waldo, Michael; Medek, Ales; Shaw, David Matthew; Panesar, Maninder; Zhang, Yuegang; Alem, Naziha; US2015/158872; (2015); A1;,
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5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5464-12-0, Sodium hydride (60percent, 0.87 g, 21.80 mmol) was added to diglyme (10 mL). A solution of 2-(4-methyl-piperazin-1-yl)-ethanol (3.14 g, 21.80 mmol) in diglyme (10 mL) was added slowly. The reaction mixture was heated at 40 00 for 1 hour, 4-chloro-pyridin-2- ylamine (1.40 g, 10.9 mmol) was added and the reaction mixture was heated at 80 0 o for 1 hour, then at 15700 for 16 hours. The reaction mixture was cooled, diluted with water (20 mL), and then THF (20 mL) and NaCI were added. The organic phase was separated and the aqueous phase was extracted with THF. The combined organic phase was dried, and then the solvent was evaporated. Diethyl ether was added to the residue. The resulting solid was filtered, washed with ether, and dried to afford white solid (1.86 g, 72percent), (M+H)=237.

The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTEX THERAPEUTICS LIMITED; SAXTY, Gordon; MURRAY, Christopher William; BERDINI, Valerio; PAGE, Lee William; ROOMANS, Susan; TAMANINI, Emiliano; BUCK, Ildiko Maria; DAY, James Edward Harvey; CARR, Maria Grazia; LEE, Lydia Yuen Wah; WO2015/4481; (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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Example 13A tert-butyl (2S)-2-methyl-4-[(6-{[5-(trifluoromethyl)pyridin-2-yl]oxy}quinolin-2-yl)carbonyl]piperazine-1-carboxylate The product from Example 1D (200 mg, 0.59 mmol) was subjected to the conditions described in Example 11, substituting (S)-tert-butyl 2-methylpiperazine-1-carboxylate for 4-(piperidin-4-yl)morpholine to give the titled compound (232 mg, 75%)., 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AbbVie Inc.; Bogdan, Andrew; Cowart, Marlon D.; DeGoey, David A.; Jinkerson, Tammie K.; Koenig, John R.; Kort, Michael E.; Liu, Bo; Matulenko, Mark A.; Nelson, Derek W.; Patel, Meena V.; Peltier, Hillary; Scanio, Marc J.; Wakefield, Brian D.; US2015/218102; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A vial was charged with (S)-tert-butyl 3-(hydroxymethyl)piperazine-l-carboxylate (321.4 mg, 1.441 mmol) and (S)-2-(methoxymethyl)oxirane (162.4 mg, 1.788 mmol) in ethanol (2.5 mL). The mixture was heated at 120 C for 30 min using microwave. The mixture was cooled to room temperature, concentrated to remove all of solvent. The residue was purified with flash column chromatography on silica gel using 1-10% methanol in dichloromethane to afford the final product as colorless oil (379.3 mg) in 86% yield. 1H NMR (500 MHz, Chloroform-;/) delta 3.88 (m, l H), 3.82 (m, 1H), 3.66 (dd, J = 13, 3 Hz, 1H), 3.64 (br, 1 H), 3.50 – 3.47(m, 2H), 3.41 (dd, J= 9.7, 3.8 Hz, 1H), 3.37 (s, 3H), 3.30 (dd, J = 9.7, 6.2 Hz, 1H), 3.25 (br, lH), 2.90 (br, 1 H), 2.80 (t, J = 11.5 Hz, 2H), 2.46 (br, 1H), 2.35 (m, 2H), 1.43 (s, 9H). MS for C|4H28N205: 305.2 (MH+)., 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£º
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); A2;,
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414910-15-9, tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,414910-15-9

TFA (965 muL) was added to a solution of intermediate 11 (210 mg) in anhydrous DCM (1 mL). The solution was stirred at r.t. for 2 hours, then it was concentrated in vacuo. The residue was diluted in a saturated potassium carbonate solution (10 mL) and extracted with AcOEt (2¡Á20 mL). The combined organic extracts were dried and concentrated in vacuo to give the title compound (110 mg) as an oil. [0244] T.I.c.: AcOEt, Rf=0.14. [0245] IR (CDCl3, cm-1): 1626 (CO). [0246] NMR (CDCl3): delta (ppm) 3.7 (bs, 1H); 3.63 (bd, 4H); 2.88 (bd, 4H); 1.72 (m, 1H); 0.99 (m, 2H); 0.75 (m, 2H). [0247] MS (ES/+): m/z=155 [M+H]+.

414910-15-9 tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate 968936, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Alvaro, Giuseppe; Di Fabio, Romano; Maragni, Paolo; Tampieri, Marsia; Tranquillini, Maria Elvira; US2004/14770; (2004); A1;,
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120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2-(5-chloro-2,4-dimethoxyphenyl)-7-(4-(2-chloropyrimidin-4- yl)piperazin-l-yl)imidazo[ l,2-a|pyridine 311 (200 mg, 0.41 mmol) and tert-butyl 2- methylpiperazine-1-carboxylate (164 mg, 0.824 mmol) was heated at 125 C in a microwave reactor for 3 h. The reaction mixture was diluted with water; the precipitate was collected by filtration, washed with water and dried. The crude compound was purified by combi-flash companion (silica gel, NH4OH/CH3OH CH2CI2) to provide tert-butyl 4-(4-{4-[2-(5-chloro-2,4-dimethoxyphenyl)imidazo[1,2-a]pyridin-7-yl]piperazin-1-yl}pyrimidin-2-yl)-2-methylpiperazine-1-carboxylate 312j (125 mg, 47%) as an off-white solid. lH NMR (300 MHz, DMSO-d6): delta 8.36 (d, ./ = 7.5 Hz, i l l). 8.17 (s, 1H), 8.03 (s, 1H), 7.92 (d, J = 6 Hz, I H), 6.87-6.84 (m, 2H), 6.71 (s, 1H), 6.18 (d, J = 6 Hz, IH), 4,51 (dd, J = 13.2, 20.7 Hz, 2H), 4.18 (bs, IH), 4.01 (s, 3H), 3.93 (s, 3H), 3 ,78-3.68 (m, 4H), 3.33-3.12 (m, 4H), 3.07-2.99 (m, 2H), 2.90-2.81 (m, IH), 1.42 (s, 9H), 1.05 (d, ./ 6.6 I zeta. 3H); HPLC (Method 1) 96.1% (AUC), fR – 13.0 min.; ESI+APCI MS rn/z 649 M + l |, 120737-78-2

120737-78-2 tert-Butyl 2-methylpiperazine-1-carboxylate 15087784, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ONCOTHERAPY SCIENCE, INC.; MATSUO, Yo; HISADA, Shoji; NAKAMURA, Yusuke; CHAKRABARTI, Anjan; RAWAT, Manish; RAI, Sanjay; SATYANARAYANA, Arvapalli, Venkata; DUAN, Zhiyong; TALUKDAR, Arindam; RAVULA, Srinivas; DECORNEZ, Helene; (491 pag.)WO2017/58503; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.25057-77-6,1,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Example 126D8-(4-((3,4-Dimethylpiperazin-l-yl)methyl)phenyl)-9-(4-fluorophenyl)-8,9-dihydro-2H-pyrido[4,3,2-<5fe]phthalazin-3(7H)-one[00772] A mixture of 4-(9-(4-fluorophenyl)-3-oxo-3,7,8,9-tetrahydro-2H-pyrido[4,3,2-25057-77-6

25057-77-6 1,2-Dimethylpiperazine 198037, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; CHU, Daniel; WO2011/130661; (2011); A1;,
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Piperazines – an overview | ScienceDirect Topics