Heterocyclic Building Blocks-piperazine

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.

Step 1: CbzCl (17 g, 0.1 mol) was added into a solution of compound 219-1 (30 g, 0.3 mol) and DIPEA (40 g, 0.3 mol) in DCM (200 mL) at 0C, then the mixture was stirred at room temperature for 3h and the solvent was removed, the crude product was purified by column chromatography to deliver compound 2 (11 g, yield 47%) as yellow oil. MS ESI calcd for C13H18N2O2 [M+H]+ 235, found 235., 109-07-9

109-07-9 2-Methylpiperazine 66057, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; WU, Hao; LIN, Jun; LI, Yunhui; WEI, Changqing; CHEN, Shuhui; LONG, Chaofeng; CHEN, Xiaoxin; LIU, Zhuowei; CHEN, Lijuan; (212 pag.)EP3124482; (2017); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.,59878-57-8

General procedure: A solution of 1,1?-carbonyldiimidazole (CDI) in THF (3 ml, 3.7 mmol) was added to indole-2-carboxylic acid (3.1 mmol) in THF (5 ml) at room temperature and stirred for 1 hunder N2. Then, the reaction mixture was cooled to 0d fC andN-substituted piperazine derivatives (3.7 mmol) in THF (3ml) were added and stirred for further 17-18 h at roomtemperature. Basic workup (CHCl3, sat. NaHCO3) wasapplied, evaporated under vacuo and recrystallization fromethyl acetate:n-hexane provided the desired compounds (1,4-15, Scheme 1).

As the paragraph descriping shows that 59878-57-8 is playing an increasingly important role.

Reference£º
Article; Altuntas, Tunca Gul; Yilmaz, Niluefer; Coban, Tuelay; Oelgen, Suereyya; Letters in drug design and discovery; vol. 14; 4; (2017); p. 380 – 386;,
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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

31166-44-6, EXAMPLE 2trans-(5-Carbamoyl-adamantan-2-yl)-amide of 4-{5-[4-(2,2-difluoro-cyclopropylmethyl)-piperazin-1-yl]-pyridin-2-yl}-3,4-dihydro-2H-quinoxaline-1-carboxylic acid (compound No. 4) 2.1: tert-Butyl ester of 4-[5-(4-benzyloxycarbonyl-piperazin-1-yl)-pyridin-2-yl]-3,4-dihydro-2H-quinoxaline-1-carboxylic acid10.12 g of tert-butyl ester of 4-(5-bromo-pyridin-2-yl)-3,4-dihydro-2H-quinoxaline-1-carboxylic acid (intermediate 1.1) and 5.7 g of 4-carboxybenzyl piperazine are mixed in 118 ml of toluene, then 0.95 g of tris(dibenzylideneacetone)dipalladium (0), 1.7 g of 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl and 3.5 g of sodium tert-butylate are added. The reaction mixture is heated at 110¡ã C. for 3 h. Then ethyl acetate is added and the mixture is washed once with water and once with a saturated aqueous solution of sodium chloride. The organic phase is dried over magnesium sulfate and concentrated under reduced pressure. The raw product obtained is chromatographed on silica gel, eluting with a gradient of a mixture of heptane/ethyl acetate (90/10 to 0/100). 10.16 g of tert-butyl ester of 4-[5-(4-benzyloxycarbonyl-piperazin-1-yl)-pyridin-2-yl]-3,4-dihydro-2H-quinoxaline-1-carboxylic acid is obtained.M+H+=530.5

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

Reference£º
Patent; SANOFI; US2012/135958; (2012); A1;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59702-07-7,1-Methylpiperazin-2-one,as a common compound, the synthetic route is as follows.

To a solution of methyl 2-[1-(3-ethylphenyl)cyclopentyl]ethanimidate hydrochloride (2.0 g) and 1-methylpiperazin-2-one (1.62 g) in THE (150 ml) was added at 22¡ãC diisopropylethyl amine (1.83 g) and after 5 mm acetic acid (426 mg) and stirring was continued at 22¡ãC for 16 h. The mixture can be further processed as described below or the intermediate 4-[2-[1-(3- ethylphenyl)cyclopentyl]ethanimidoyl]-1 -methyl-piperazin-2-one hydrochloride can be isolated by dilution with ethyl ether followed by filtration and drying of the residue.The mixture containing the intermediate was cooled down to -30¡ãC, a solution of lithium hexamethyldisilazide in THF (1M, 50 ml) was added followed by diethyl oxalate (4.15 g) and stirring was continued at -30¡ãC. In case of incomplete conversion a further portion of lithium hexamethyldisilazide and diethyl oxalate has to be added. The mixture was warmed to 22¡ãC, partitioned between aqueous hydrochloric acid (1 N) and dichloromethane, the organic layerwas dried, evaporated, the residue triturated with diethyl ether, filtered and the residue dried to give example 1 (1.40 g) as a white powder. Alternatively, the crude material can purified by preparative HPLC (RP-18, MeCN/H20 containing 0.23percent of HCOOH).MS (ESI, mlz): 382.3 [(M+H)]

59702-07-7, As the paragraph descriping shows that 59702-07-7 is playing an increasingly important role.

Reference£º
Patent; SAVIRA PHARMACEUTICALS GMBH; EUROPEAN MOLECULAR BIOLOGY LABORATORY; LERNER, Christian; KREIS, Lukas; WEIKERT, Robert James; NEIDHART, Werner; HILPERT, Hans; (97 pag.)WO2017/158147; (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.154590-34-8,tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

STEP A: 4-(2-fluoro-4-methylamino-phenyl)-piperazine-1-carboxylic acid tert- butyl ester. 4-(2-Fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (10 mmol) was dissolved into EtOH/EtOAc (50/50 ml_). SnCI22H2O (10 g) was then added. The resulting mixture was heated at 1000C for 16 h. After being cooled down, ice-H2O (100 mL) was added followed by addition of NaHCO3 until pH = 9. The resulting mixture was extracted by EtOAc (3 x 200 mL). The organic layer was collected, dried (Na2SO4), filtered, and concentrated to yield the crude title compound., 154590-34-8

As the paragraph descriping shows that 154590-34-8 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2009/79597; (2009); 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

A solution of methyl (Z)-3-((4-acetamidophenyl)chloromethylene)-2-oxoindoline-5-carboxylate (10 mg, 0.03 mmol), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (8.1 mg, 0.03 mmol) and TEA (0.01 mL, 0.06 mmol) in EtOH (0.1 mL) was stirred under refluxed for overnight. The reaction solvent was evaporated under reduced pressure, and the residue was purified by column chromatography with dichloromethane/ethanol (50/1, v/v) to obtain the final compound 102 as a yellow solid (14 mg, 88% yield): 1H NMR (400 MHz, DMSO-d6) _ 11.89 (s, 1H), 11.12 (s, 1H), 10.26 (s, 1H), 7.77 (d, J = 8.6 Hz, 2H), 7.58 (dd, J = 8.2, 1.7 Hz, 1H), 7.41 (d, J = 8.6 Hz, 2H), 7.15 (d, J = 8.2 Hz, 2H), 6.93 (d, J = 8.2 Hz, 1H), 6.90 (d, J = 5.0 Hz, 2H), 6.69 (s, 1H), 3.64 (s, 3H), 3.06 (bs, 2H), 2.67 (bs, 2H), 2.18 (bs, 4H), 2.11 (s, 3H), 2.10 (bs, 2H); HRMS (ESI-TOF) m/z calcd for C33H36N6O5 [M + H+] 596.2747 found 597.2818.

262368-30-9, As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference£º
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; DALBY, Kevin N.; EDUPUGANTI, Ramakrishna; TALIAFERRO, Juliana; LEE, Juhyeon; (0 pag.)WO2018/160967; (2018); A1;,
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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

10222] Step 4. To a suspension of 2-methoxy-4-(4-meth- ylpiperazin- 1 -yl)aniline (Green Chempharm; 3.45 g, 15.57 mmol) and N-(3-(5-methyl-2-(methylsulfinyl)-7-oxopyrido [2,3-d]pyrimidin-8(7H)-yl)phenyl)acrylamide (Sb) (4.59 g, 12.46 mmol) in anhydrous tert-butanol (40 mE) and dioxane (5 mE) at RT was added DIEA (4.33 mE, 24.92 mmol). The mixture was heated at 1000 C. for 40 h. The reaction mixture was concentrated under reduced pressure (rotary evaporator) to remove the volatiles and the resulting crude residue was suspended in Et20 and filtered. The greenish-brown amorphous solid was washed with Et20 (3×50 mE) and this removed most of the remaining aniline starting material. The crude material was dry-packed on silica gel and purified on a silica gel column (1-20% MeOH in DCM) affording N-(3- (2-((2-methoxy-4-(4-methylpiperazin-1 -yl)phenyl)amino)5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl)phenyl)acrylamide (5) (2.03 g, 3.86 mmol, 31% yield) as a yellow amorphous solid. m/z (ESI, +ve ion) 526.2 (M+H). ?H NMR (400 MHz, DMSO-d5) oe ppm 10.33 (1H, s), 8.80 (1H, s), 8.09 (1H, s), 7.88 (1H, d, J=8.2 Hz), 7.56 (1H, J=1 .9Hz), 7.50 (1H, t, 1=8.1 Hz), 7.27 (1H, d, J=8.8 Hz), 6.97 (1H, dt, J=6.9, 1.0 Hz), 6.52 (1H, d, J=2.5 Hz), 6.37-6.48 (1H, m), 6.29-6.35 (1H, m), 6.19-6.29 (1H, m), 6.01 (1H, bt s.), 5.71-5.80 (1H, m), 3.78 (3H, s), 3.02 (4H, bt s.), 2.46 (3H, s), 2.43 (4H, t, J=4.9 Hz), 2.22 (3H, s)., 122833-04-9

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

Reference£º
Patent; TASKER, Andrew; WURZ, Ryan; PETTUS, Liping H.; HERBERICH, Bradley J.; US2014/249131; (2014); A1;,
Piperazine – Wikipedia
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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.

(0122) To a mixture of Compound 3J (59.8 mg, 0.105 mmol), Compound 11B (33 mg, 0.105 mmol) and N,N-dimethylpyridin-4-amine (38.4 mg, 0.314 mmol) in dichloromethane (5 ml) was added 1-ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (24.07 mg, 0.13 mmol). The reaction mixture was stirred at room temperature overnight and concentrated. The residue was purified by reverse phase HPLC on a C18 column using a gradient of 40-60% acetonitrile/0.1% trifluoroacetic acid in water to give the title compound as the trifluoroacetate salt. The trifluoroacetic acid salt was dissolved in dichloromethane (6 ml) and washed with 50% aqueous NaHCO3. The organic layer was dried over anhydrous Na2SO4 and concentrated to give the title compound. 1H NMR (500 MHz, dimethylsulfoxide-d6) delta 11.68 (s, 1 H), 11.40 (s, br, 1 H), 8.53-8.58 (m, 2 H), 8.04 (d, 1 H), 7.80 (dd, 1 H), 7.47-7.54 (m, 3 H), 7.34 (d, 2 H), 7.02-7.09 (m, 3 H), 6.67 (dd, 1 H), 6.39 (dd, 1 H), 6.19 (d, 1 H), 3.79 (dd, 1 H), 3.69-3.73 (m, 1 H), 3.22-3.37 (m, 3 H), 3.16-3.21 (m, 1 H), 3.07 (s, 4 H), 2.74 (s, 2 H), 2.09-2.24 (m, 6 H), 1.95 (s, 2 H), 1.86-1.93 (m, 1 H), 1.79-1.85 (m, 1 H), 1.58-1.64 (m, 1 H), 1.42-1.51 (m, 1 H), 1.38 (t, 2 H), 1.25-1.34 (m, 1 H), 0.92 (s, 6 H).

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

Reference£º
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
Piperazine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

A solution of 5-fluoro-2-nitroanisole (200 g, 1 eq) and piperazine (302 g, 3 eq) in DMF was stirred for 30 minutes and heated for 12 hours. Acetic anhydride (358 g, 3 eq) was slowly added to the reaction solution, and the reaction solution was stirred at room temperature for 12 hours. Water was added to the reaction solution for dilution, and the solid was filtered and washed twice with water. After drying at 50 C, the product was obtained as a yellow solid (284 g, 87%)., 13889-98-0

As the paragraph descriping shows that 13889-98-0 is playing an increasingly important role.

Reference£º
Patent; Anqing Yuanqi Pharmaceutical Technology Co., Ltd.; Jin Wei; Liu Jinlun; Wang Jianbing; (6 pag.)CN110294721; (2019); A;,
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Piperazines – an overview | ScienceDirect Topics

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15 1 -mesyl-4-(5-methoxycarbonyl-2-pyridyl)piperazine 1-Mesylpiperazine hydrochloride (4.24 g) was added to a solution of methyl 6-chloronicotinate (1.7 g) and N,N-diisopropylethylamine (6.3 ml) in dimethylacetamide (20 ml) and the mixture was heated at 120 C. for 2 hours.. The mixture was allowed to cool to ambient temperature and poured onto crushed ice/water (50 ml) to precipitate a tan solid.. The solid was collected by filtration and dried at 80 C. for 18 hours in a vacuum oven, to give 1-mesyl-4-(5-methoxycarbonyl-2-pyridyl)piperazine (2.05 g), mp 205-207 C. NMR (d6-DMSO): 2.90 (s, 3H), 3.20 (m, 4H), 3.78 (m, 3H), 3.80 (s, 3H), 6.92 (d, 1H), 8.00 (dd, 1H), 8.67 (d, 1H), m/z 300 (M+1)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AstraZeneca AB; US6734184; (2004); B1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics