Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

Amixture of A2. C-2) (0.0002 mol) and 4-[(4-methyl-1-piperazinyl)methyl]-benzenamine (0.0004 mol) in DMSO (2 ml) was stirred for 3 hours at 80C and then the reaction mixture was stirred overnight at room temperature. The solvent was evaporated (Genevac) and the obtained residue was purified by high-performance liquid chromatograp hy. The product fractions were collected, then the solvent was evaporated and co-evaporated with CH3OH. Yield: 0.0119 g of final compound 80., 70261-82-4

The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2005/12304; (2005); A2;,
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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

1- (Methylsulfonyl) piperazine hydrochloride (1.07 mmol) was added to acetonitrile (5 ml) and potassium carbonate (1.16 mmol) was added followed by 3-phenylpropyl isocyanate (1.07 mmol). The reaction mixture was stirred at room temperature for 8 hours. After the reaction was completed, water was added and extracted with ethyl acetate. The organic layer was concentrated and purified by column chromatography to give the title compound., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; The Industry & Academic Cooperation in Chungnam National University (IAC); Jung, Sang-Hun; Woo, Sun-Hee; Kim, Sang- Kyum; Jeon, Eun-Seok; Lee, Yu-Jung; Meunikam, Manoj; Jalani, Hiteshkumar; Sharma, Niti; (205 pag.)KR2016/108281; (2016); A;,
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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

To n-butanol (2 mL) was added compound 4A-3 (30 mg, 0.135 mmol) and compound 5A-1 (47 mg, 0.135 mmol), and then p-toluenesulfonic acid (23.3 mg, 0.135mmol) was added under stirring. The mixture was heated to 100C and stirred for 5 hours. After TLC indicated the reaction was completed, the reaction mixture was concentrated under reduced pressure to give a crude product, which was further purified and isolated by column chromatography to obtain an off-white solid product, compound I-13 (56 mg, yield 77.8%). 1H NMR (400 MHz, cd3od) delta 8.49 (d, J=8.4 Hz, 1H), 8.07 (s, 1H), 7.86 (dd, J=8.0, 1.3 Hz, 1H), 7.67 (d, J=8.7 Hz, 1H), 7.60 (dd, J=11.5, 4.3 Hz, 1H), 7.30 (t, J=7.6 Hz, 1H), 6.67 (s, 1H), 6.49 (dd, J=8.7, 2.1 Hz, 1H), 3.84 (s, 3H), 3.29-3.20 (m, 4H), 2.97-

122833-04-9, 122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Humanwell Healthcare (Group) Co., Ltd.; WANG, Xuehai; XU, Yong; SHENG, Xijun; ZHANG, Xiaolin; XIA, Hangui; YANG, Zhongwen; YUE, Yang; HUANG, Lu; XIAO, Qiang; (80 pag.)EP3372594; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step C: tert-butyl (3S)-3-(hydroxymethyl)-4-{2-hydroxy-2-[(3R)-3-methyl-1-oxo-3,4-dihydro-1H-isochromen-6-yl]ethyl}piperazine-1-carboxylate:A solution of (3R)-3-methyl-6-( oxiran-2-yl)-3,4-dihydro-IH-isochromen-1-one (325 mg, 1.59 mmol) and tert-butyl (3S)-3-(hydroxymethyl)piperazine-1-carboxylate (345 mg, 1.59 mmol dissolved in EtOH (7mL) was heated in a sealed tube to 155C for 3 hours in the microwave. The reaction was cooled andconcentrated to give crude product which was purified via MPLC ( 40-100% EtOAc/Hexane) togive the title compound as a mixture of diastereomers.

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.639068-43-2,tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,639068-43-2

A solution of compounds of general structure 1 (1 equiv), Boc protected amine (1-3 equiv) and DIPEA (3 equiv) in DMSO were reacted at 100-110 ¡ãC. The reaction mixture was cooled to room temperature and quenched by addition of water and crude residue extracted with EtOAc. Combined organic layers were washed with brine, dried over Na2S04, filtered and concentrated under reduced pressure to provide crude compound of general strucutre 2, which was used in the following step without further purification. To a solution of compounds of general structure 2 in CH2C12 was added HCl/dioxane (4 N) or TFA. The reaction was stirred at room temperature for 2 hrs and mixture was concentrated under reduced pressure. The residue was purified by reverse phase preparative HPLC to afford final compounds of general structure 3.

As the paragraph descriping shows that 639068-43-2 is playing an increasingly important role.

Reference£º
Patent; KADMON CORPORATION, LLC; SKUCAS, Eduardas; LIU, Kevin, G.; KIM, Ji-In; POYUROVSKY, Masha, V.; MO, Rigen; (345 pag.)WO2019/45824; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Example 61 (4-Fluoro-phenyl)-f 3- [3- (4-fluoro-phenyl)- [1, 2,4] oxadiazol-5-yl]-4-methyl-piperazin- l-yl}-methanone; 61 (A) Piperazine-1,3-dicarboxylic acid-1-tert-butyl ester To a solution of 2-piperazine-carboxylic acid dihydrochloride (1.0 g, 4.92 mmol) in 20 mL of water/dioxane 1 : 1, NaOH 6N was added to adjust the pH to 11. A solution of BOC-ONS (1.34 g, 5.41 mmol) in dioxane (5 mL) was then added dropwise, while maintaining the pH=l 1 during the addition and the resulting solution was stirred overnight at room temperature. Another 0.134 g of BOC-ONW were added and the reaction mixture was stirred for 2h. The solvent was evaporated under reduced pressure and the residue was diluted with diethyl ether/water (60 mL). The phases were separated and the pH of the aqueous layer was adjusted to 7 by slow addition of HC1 1N. Evaporation of water under reduced pressure afforded the title compound as a white solid which was dried in a vacuum oven at 50C and used without further purification for the next step. LCMS (Tr): 3.3 min (Method B); MS (ES+) gave m/z: 231. 0.

3022-15-9, As the paragraph descriping shows that 3022-15-9 is playing an increasingly important role.

Reference£º
Patent; ADDEX PHARMACEUTICALS SA; WO2005/44797; (2005); A1;,
Piperazine – Wikipedia
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 5 6- [3-(4-MethanesuIfonyl-piperazin-l-vImethyl)-phenyn -2- morpholin-4-vI-[4,5’lbipyrimidinyl-2>-ylamine (38)Intermediate Cl (lOOmg, 0.33mmol) and Intermediate G (1.2 equiv., 80mg) were taken up in 1,2-dichloroethane (5ml). To this was added sodium triacetoxyborohydride (2.4equiv., 170mg) and trimethyl orthoformate (0.1ml) and the reacton mixture was stirred at room temperature overnight. Purification by DCM/aqueous NaHCO3 extraction, SCX-2 cartridge and flash chromatography gave 4- {4-chloro-6-[3-(4-methanesulfonyI-piperazin- 1 -ylmethyl)-phenyl]-pyrimidin-2-yl} – morpholine as a white solid (95mg). 4- {4-Chloro-6- [3 -(4-methanesulfonyl-piperazin- 1 -y lmethyl)-phenyl] -pyrimidin-2-yl } – morpholine (90mg, 0.20mmol) and 2-aminopyrimidine-5-boronic acid pinacol ester (1.8 equiv., 80mg) were taken up in acetonitrile (3ml). To this were added sodium carbonate (3 equiv., 64mg) as a solution in water (ImI) and PdCl2(PPh3)2 (0.05 equiv.). The reaction mixture was heated in microwave at 14O0C for 30 min. Purification using SCX- 2 cartridge, flash chromatography and trituration with hot DCM gave the title compound as a white solid (105mg).NMR (CDC13): 2.61-2.64 (4H, m), 2.81 (3H, s), 3.27-3.30 (4H, m), 3.67 (2H, s), 3.84- 3.87 (4H, m), 4.00-4.03 (4H, m), 5.32 (2H, br), 7.28 (IH, s), 7.47-7.49 (2H, m), 7.99 (IH, s), 8.01-8.04 (IH, m), 9.04 (2H, s) MS (ESI+): MH+ 511.17 (100%)., 161357-89-7

161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; WO2009/66084; (2009); 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.960283-58-3,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

Description 103; 1 ,1 -Dimethylethyl (2S)-4-[(2-chloro-4-nitrophenyl)methyl]-2-methyl-1 – piperazinecarboxylate (D103); A mixture of crude 1-(bromomethyl)-2-chloro-4-nitrobenzene (D102) (0.391 g), 1 ,1- dimethylethyl (2S)-2-methyl-1-piperazinecarboxylate hydrochloride (0.407 g, 1.72 mmol) and Hunig’s base (0.625 ml_, 3.59mmol) in dry DMF (3 mL) was stirred at room temperature for 10 minutes. The reaction mixture was concentrated to give an orange oil which was dissolved in DCM and washed with water (x2) and brine, then dried and concentrated to give an orange oil. Purification by column chromatography eluting with 0-30% EtOAc/pentane gave the title compound as a yellow oil (0.199 g). deltaH (CDCI3, 400MHz) 8.24 (1 H1 d), 8.12 (1 H, dd), 7.77 (1 H, d), 4.24 (1 H, br.s), 3.85 (1 H, d), 3.63 (2H, s), 3.14 (1 H, td), 2.76 (1 H, m), 2.59 (1H, m), 2.33 (1H, dd), 2.18 (1 H, m), 1.47 (9H1 s), 1.28 (3H1 d). MS (ES): MH+ 370/372,

960283-58-3, 960283-58-3 (S)-tert-Butyl 2-methylpiperazine-1-carboxylate hydrochloride 45072182, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2008/729; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

485841-52-9, (S)-1,2-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[Step 4] tert-Butyl 8-[(3S)-3,4-dimethylpiperazin-1-yl]-7,10-dimethyl-5-oxo-1,5-dihydro-2H-chromeno[3,4-c]pyridine-3(4H)-carboxylate A suspension of tert-butyl 7,10-dimethyl-5-oxo-8-{[(trifluoromethyl) sulfonyl]oxy}-1,5-dihydro-2H-chromeno[3,4-c]pyridine-3(4H)-carboxylate (1.063 g), cesium carbonate (2.2 g), chloro-(2-dicyclohexylphosphino-2′,6′-diisopropoxy-1,1′-biphenyl)[2-(2-aminoethyl)phenyl] palladium (II)-methyl-t-butyl ether adduct (91 mg), 2-dicyclohexylphosphino-2′,6′-diisopropoxybiphenyl (52 mg), and (2S)-1,2-dimethylpiperazine (510 mg) in toluene (30 ml) was stirred while heating in a nitrogen atmosphere at 110 C. for 2.5 hours. The reaction solution was diluted with chloroform and a small volume of methanol and an insoluble solid was filtered off and the mother liquid was concentrated. The residue was purified by silica gel column chromatography (4-8% methanol/chloroform) to obtain the title compound (710 mg) as a solid. 1H-NMR (CDCl3) delta: 1.13 (3H, d, J=6.1 Hz), 1.50 (9H, s), 2.29-2.40 (1H, m), 2.33 (3H, s), 2.37 (3H, s), 2.46-2.62 (2H, m), 2.66 (3H, s), 2.87-2.98 (2H, m), 2.99-3.14 (4H, m), 3.58-3.65 (2H, m), 4.40 (2H, s), 6.70 (1H, s). MS (ESI/APCI) m/z: 442 [M+H]+

485841-52-9, As the paragraph descriping shows that 485841-52-9 is playing an increasingly important role.

Reference£º
Patent; Daiichi Sankyo Company, Limited; Ota, Masahiro; Inoue, Hidekazu; Kawai, Junya; Ohki, Hitoshi; Toki, Tadashi; (25 pag.)US2019/284198; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

115761-79-0, 1-(2,4-Difluorophenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 48 (26 mg, 0.1 mmol) in DMF (1 mL) was added 2,4- difluorophenylpiperazine (20 mg, 0.1 mmol). The reaction mixture was stirred for 1.5 hours. To the crude mixture was added 2-thiopheneethylamine (14 pL, 0.12 mmol), DIEA (38 pL, 0.22 mmol) and HATU (42 mg, 0.11 mmol). The reaction was stirred overnight at room temperature. The reaction mixture was poured into water and extracted with EtOAc. The combined organic layers were washed with 0.1 N NaOH, 0.1 N HCI, and brine; dried over sodium sulfate and concentrated in vacuo to yield 49 as an oil (49 mg, 94%). HPLC- MS tR = 2.10 min (UV254 nm); mass calculated for formula C24H27F2N3O6S 523.2, observed LCMS m/z 524.4 (M+H) ; purity > 95% (ELSD).

115761-79-0, As the paragraph descriping shows that 115761-79-0 is playing an increasingly important role.

Reference£º
Patent; SCHERING CORPORATION; WO2005/121130; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics