Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.38216-72-7,1-tert-Butylpiperazine,as a common compound, the synthetic route is as follows.

A. Synthesis of l-(4-(4-fert-butylpiperazin-l-yl)(phenyl)methyl)piperidin-l-yl)ethanone; [0092] 1-tert-butylpiperazine (4.48 g, 20.8 mmol), l-(4-(chloro(phenyl)methyl)piperidin-l-yl)ethanone (5.77 g, 22.9 mmol), K2CO3 (7.2 g, 52.1 mmol), and KI (22.9 mmol) were combined in dry DMF (150 mL). The reaction was refluxed overnight. Upon completion of the reaction, the DMF was removed under reduced pressure. The resulting crude was taken up in water (75 mL) and washed with EtOAc (3 x 100 mL). The organic portions were combined, dried (Na2SO4) and concentrated. The product was purified by silica gel chromatography (2.5:2.5:95 Et3N/MeOH/EtOAc, Rf 0.4) and isolated as a red oil (2.66 g, 36%).

38216-72-7, 38216-72-7 1-tert-Butylpiperazine 3530572, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; NEUROMED PHARMACEUTICALS LTD.; WO2008/31227; (2008); A1;,
Piperazine – Wikipedia
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304897-49-2, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 1 is synthesized by reacting compound l-A with l-B using the conditions indicated above. Compound l-C is then reacted with compound l-D using the reaction conditions shown to afford the product l-E. The amine protecting group is then removed using suitable acidic conditions ( e.g ., TFA or HC1 in dioxane). Purification using standard techniques (e.g., silica gel chromatography or prep-HPLC) as needed., 304897-49-2

304897-49-2 tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate 12045001, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; TOLERO PHARMACEUTICALS, INC.; SIDDIQUI-JAIN, Adam; WARNER, Steven L.; FLYNN, Paul; BEARSS, David J.; FOULKS, Jason Marc; TOMIMATSU, Nozomi; FUJIMURA, Ken; UMEHARA, Hiroki; NONOYAMA, Akihito; KIGUCHIYA, Akihito; (441 pag.)WO2019/195753; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of [l-(3,5-dichloro-benzyl)-lH-imidazol-2-ylmethyl]-(3-fluoro-benzyl)- amine (146 mg, 0.4 mmol) in TEtaF (1 mL) at -78 0C was added dropwise a solution of n- BuLi in hexane (0.19 mL, 0.44 mmol) and the mixture stirred at -78 0C for 30 min. A solution of 4-(2-Chloro-ethyl)-piperazine-l-carboxylic acid tert-butyl ester (116 mg, 0.46 EPO mmol) in THF (1 mL) was then added dropwise and the mixture allowed to warm to ambient temperature before stirring for an additional 24 h. The reaction was quenched with water (10 mL) and extracted with CH2Cl2 (2 x 40 mL). The combined CH2Cl2 extracts were dried over Na2SO4 and concentrated in vacuo. The residue was purified by column chromatography (silica gel, 20:1 CH2Cl2ZMeOH) to provide 4-{2-[[l-(3,5- dichloro-benzyl)-lH-imidazol-2-ylmethyl]-(3-fluoro-benzyl)-amino]-ethyl}-piperazine-l- carboxylic acid tert-butyl ester (102 mg, 44%) as a colorless viscous oil: ESI MS m/z 576 [C29H36Cl2FN5O2 + H]+.

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2006/107923; (2006); 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.109-01-3,1-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture [OF N-METHYLPIPERAZINE] (0. [0499MOL),] [2-BROMOETHANOL] (0. [0749MOL)] and [K2CO3] (0. [0998MOL)] in 2-butanon (90mL) was stirred for [4H] at [90¡ãC.] The cooled reaction mixture was filtered. The filtrate was evaporated. Yielding 90percent of intermediate 14. (Remark: lower yields were obtained on [A] higher scale and purification by short column chromatography was necessary)., 109-01-3

The synthetic route of 109-01-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2004/7498; (2004); A2;,
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Piperazines – an overview | ScienceDirect Topics

67455-41-8, 4-(Piperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,67455-41-8

General procedure: A mixture of compounds 5a-5i (10.0 mmol), concentrated hydrochloricacid (12.2 mmol) and melamine (20.0 mmol) in isopropylalcohol (10.0 mL) was refluxed for 8 h. Progress of reaction wasmonitored by tlc and after complete conversion of starting materialreaction mixture was cooled to rt. The reaction mixture wasquenched in saturated sodium carbonate solution (20.0 mL) andfiltered. The solid was washed with water (50.0 mL). The crudeproduct thus obtainedwas dried at 50 C under reduced pressure toget compounds 6a-6i.

The synthetic route of 67455-41-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Zhao, Hui; Hu, Xiaoxia; Cao, Kai; Zhang, Yue; Zhao, Kuantao; Tang, Chunlei; Feng, Bainian; European Journal of Medicinal Chemistry; vol. 157; (2018); p. 935 – 945;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

34770-60-0, 4-Methylpiperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 6.1.15. General procedure IV, for preparation of 14a-f A mixture of aryl bromide (1.0 mmol), 4-methylpiperazin-2-one (for compounds 15-17)/morpholin-3-one (for compounds 18-20) (2.0 mmol), N,N0-dimethylethylene diamine (0.1 mmol), K2CO3 (2.0 mmol) and CuI (0.05 mmol) in anhydrous toluene was heated to reflux with stirring for 6 h. Then the reaction mixture was cooled to room temperature, poured into water, stirred vigorously and extracted thrice with ethyl acetate, dried over anhydrous Na2SO4, concentrated under reduced pressure and purified by flash chromatography to afford compounds 14a-f in 54-68% yields. 6.1.18 1-(2-Fluoro-4-vinylphenyl)-4-methylpiperazin-2-one (14c) A mixture of 1-bromo-2-fluoro-4-vinylbenzene 3c (0.2 g, 0.99 mmol), 4-methylpiperazin-2-one (0.22 g, 1.99 mmol), N,N’-dimethylethylene diamine (0.008 g, 0.09 mmol), K2CO3 (0.27 g, 1.99 mmol) and CuI (0.009 g, 0.04 mmol) in anhydrous toluene was heated to reflux and the reaction was continued as described in general procedure IV to afford 14c (0.12 g) in 55% yield. 1H NMR (400 MHz, CDCl3): delta 7.18-7.24 (m, 3H), 6.66 (dd, J = 17.5, 10.8 Hz, 1H), 5.74 (d, J = 17.5 Hz, 1H), 5.32 (d, J = 10.8 Hz, 1H), 3.62-3.69 (m, 2H), 3.30 (s, 2H), 2.77-2.84 (m, 2H), 2.42 (s, 3H); LC-MS: 235 (M++1)., 34770-60-0

34770-60-0 4-Methylpiperazin-2-one 13704283, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Rakesh; Bruhn, David; Maddox, Marcus; Lee, Robin B.; Yang, Lei; Lee, Richard E.; Madhura, Dora B.; Trivedi, Ashit; Meibohm, Bernd; Scherman, Michael S.; Gilliland, Janet C.; Gruppo, Veronica; McNeil, Michael R.; Lenaerts, Anne J.; Bioorganic and medicinal chemistry; vol. 20; 20; (2012); p. 6063 – 6072,10;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

502649-29-8,502649-29-8, 1-Boc-3-Benzylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of Pd(OAc)2 (0.054 g, 0.2 mmol), NaOtBu (0.64 g, 6.6 mmol) in xylene (7.0 mL) in a screw-capped tube was added tBu3P (0.049 g, 0.2 mmol). After 10 minutes a solution of 5-bromo-1-(tert-butyl-dimethyl-silanyl)-1H-indole (1.30 g, 4.4 mmol) in xylene (7.0 mL) and a solution of 3-benzyl-piperazine-1-carboxylic acid tert-butyl ester (1.34 g, 4.8 mmol) in xylene (8.0 mL) were added. The mixture was heated to 80 C. for 30 minutes, then cooled to room temperature. The reaction mixture was taken up in ethyl acetate, filtered through a pad of celite, and concentrated under reduced pressure. Purification via flash chromatography (gradient: 2% to 20% EtOAc in hexane) afforded 3-Benzyl-4-[1-(tert-butyl-dimethyl-silanyl)-1H-indol-5-yl]-piperazine-1-carboxylic acid tert-butyl ester (1.65 g, 74%) as a pale yellow solid; MS (M+H)=506.

The synthetic route of 502649-29-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Carter, David Scott; Schoenfeld, Ryan Craig; Weikert, Robert James; US2008/45543; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

170911-92-9, tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

mCPBA (<77% pure) (8.8 mg, 0.039 mmol) in DCM (0.5 ml) was added to a stirred solution of 3-(8-methyl-2-(methylthio)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl acetate (11.6mg, 0.034 mmol) in toluene (1.0 mL) at RI under nitrogen. After 15 mi DIPEA (0.018 mL, 0.102 mmol) and tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (10.4 mg, 0.037 mmol) were added, successively, and the temperature was increased to 60 C. After 16 h, the reaction mixture wascooled to RI and was loaded directly onto a KP-NH column and purified by flash chromatography (0-100%, EtOAc in cyclohexane; then 10% MeOH in EtOAc) to give the title compound (9.7 mg, 54%) as a yellow solid. LCMS (MethodA) : RT = 1.25 mi m/z = 529 [M+H]. 170911-92-9, The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ALMAC DISCOVERY LIMITED; ROUNTREE, James Samuel Shane; O’DOWD, Colin Roderick; BURKAMP, Frank; BELL, Mark Peter; WO2015/19037; (2015); A1;,
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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, 1-(Bromomethyl)-4-nitro-2-(trifluoromethyl)benzene (34 g, 120 mmol) obtained in Step (1) above was stirred in a solvent of dichloromethane (300 mL). The reaction solution was added with 1-ethylpiperazine (15.97 mL, 126 mmol) and DIPEA (27.2 mL, 156 mmol), followed by stirring for about 3 hours at room temperature. The reaction mixture was diluted with dichloromethane, washed with a saturated aqueous sodium bicarbonate solution and saline. The organic layer thus obtained was dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain the title compound (21.7 g, 57%). 1H-NMR Spectrum (300 MHz, DMSO-d6): delta 8.52 (d, 1H), 8.40 (s, 1H), 8.09 (d, 1H), 3.71 (s, 2H), 2.35 (m, 10H), 1.00 (t, 3H). MS (ESI+, m/z): 318 [M+H]+

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

Reference£º
Patent; HANMI PHARM. CO., LTD.; Bae, In Hwan; Han, Sang Mi; Kwak, Eun Joo; Ahn, Young Gil; Suh, Kwee Hyun; US2015/191450; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (2-isopropylphenyl)[2-nitro-4-E-(carboxyethenyl)phenyl]sulfide (prepared according to the procedures of Example 32), the amine from Example 71A (1.0 eq), 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (1.0 eq), and diisopropylethylamine (2.0 eq) in DMF was stirred at ambient temperature for 4 hr.ethyl acetate was added, and the mixture was washed sequentially with 1N HCl, aq. NaHCO3, and brine.The resultant yellow solid was treated with 1:1 TFA/dichloromethane at ambient temperature to give the title compound as a yellow solid. 1HNMR (DMSO-d6, 300 MHz) delta 1.15 (d, J=6.6 Hz, 6H); 2.52-3.16 (br m, 4H); 3.25-3.47 (m, 1H); 3.60-3.65 (br d, 3H); 3.60, 3.66 (br s, br s, 3H); 6.61-6.67 (br m, 1H); 7.30-7.62 (m, 6H); 7.88-7.93 (br m, 1H); 8.58-8.65 (br m, 1H). MS (APCI) (M+H)+ at m/z 470.Anal calcd for C24H27N3S1O5: C, 61.39; H, 5.80; N, 8.95. Found: C, 61.51; H, 5.87; N, 8.68., 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Abbott Laboratories; US2004/116518; (2004); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics