Heterocyclic Building Blocks-piperazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Step 1: 2-chloro-5-nitropyridine (5 g, 32 mmol) and K2CO3 (8.8 g, 64 mmol) were dissolved in acetonitrile (40 mL), compound 245-1 (4.3 g, 38.4 mmol) was added. The reaction mixture was stirred at 80¡ãC for 1h, then the reaction mixture was filtrated, concentrated to deliver compound 245-3 (4.5 g) as yellow solid. MS ESI calcd for C11H16N4O2 [M+H]+ 237, found 237., 21655-48-1

As the paragraph descriping shows that 21655-48-1 is playing an increasingly important role.

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
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.16154-62-4,1-(2-Chloro-4-nitrophenyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

To a solution of SG4-029 (2.00 g, 7.82 mmol) in MeOH (32 mL, deoxygenated with Argon gas) was added PtC (18 mg, 0.0782 mmol). A balloon of hydrogen gas was attached to the flask via a septum cap. The mixture was stirred at room temperature for 5 h. The reaction mixture was filtered over Celite and the filtrate concentrated under reduced pressure to provide the title compound as a light yellow solid (1.741 g, 98%). NMR (400 MHz, DMSO-ifc) delta: 6.85 (d, J = 8.5 Hz, 1H), 6.59 (d, / = 2.6 Hz, 1H), 6.45 (dd, / = 8.5, 2.6 Hz, 1H), 5.01 (s, 2H, disappeared on D20 shake), 2.81- 2.72 (m, 4H), 2.40 (brs, 4H), 2.18 (s, 3H). HPLC-MS (ESI+): m/z 228.2 [35%, (M37C1+H)+], 226.2 [100%, (M35C1+H)+]., 16154-62-4

The synthetic route of 16154-62-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas J.; LAWRENCE, Harshani R.; (293 pag.)WO2017/66428; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74852-62-3, 4-(4-(4-Methoxyphenyl)piperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

c) A solution of 400 g of 4-[4-(4-methoxyphenyl)-1-piperazinyl]benzenamine (prepared as described in example I of U.S. Pat. No. 4,267,179) in 1000 ml of tetrahydrothiophene 1,1-dioxide was stirred for 1 hour at 100 C. A solution of 382.8 g intermediate (2) in 200 ml of tetrahydrothiophene 1,1-dioxide, which was prepared by warming to 60 C., was added dropwise over 4 hours at 100 C. The mixture was stirred overnight at 100 C. and for 3 hours at 160 C. After cooling to 50 C., the precipitate was filtered off, washed with acetone and dried in vacuo at 60 C. under nitrogen, yielding 290 g (56%) of 2,4-dihydro-4-[4-[4-(4-methoxyphenyl)-1-piperazinyl]phenyl]-5-methyl-3H-1,2,4-triazol-3-one (interm. 3)., 74852-62-3

The synthetic route of 74852-62-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Janssen Pharmaceutica N.V.; US5254553; (1993); A;,
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.84477-72-5,2,2-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

84477-72-5, 2,2-dimethylpiperazine (1 1 .5 kg, 101 mol) was dissolved in ethanol (48.5 L) and the solution was cooled to approximately 9C. Di-tert-butyl dicarbonate (21 .9 kg, 100 mol) was dissolved in ethanol (41 .7 L). The solution of di-tertbutyl dicarbonate was added to the solution of dimethylpiperazine over a period of 2 h 30 min, keeping the temperature of the reaction below 15C. Ethanol (12.4 L) was added and the solution was stirred overnight at a temperature between 12-25C. The reaction was warmed to reflux and 75 L were distilled off. Ethanol (76 L) was added to the reaction and the solution was heated to 52C and transferred to a suspension of D,L-tartaric acid (7.5 kg, 50.0 mol) in ethanol (25.2 L), and warmed to 51 C. Ethanol (25.3 L ) was added and the reaction was kept at 20C overnight. The precipitate was filtered off and washed with ethanol (28.1 L). The solid was dried in a vacuum oven at 50C overnight to yield compound (XVIII) (27.1 kg, 93%) with 99% purity according to GC analysis.

As the paragraph descriping shows that 84477-72-5 is playing an increasingly important role.

Reference£º
Patent; H. LUNDBECK A/S; JACOBSEN, Mikkel Fog; BRANDES, Sebastian; WO2014/96151; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

16154-62-4, 1-(2-Chloro-4-nitrophenyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Chloro-4-(4-methylpiperazin-l-yl)aniline (SG4-030): To a solution of SG4-029 (2.00 g, 7.82 mmol) in MeOH (32 niL, deoxygenated with Argon gas) was added PtC (18 mg, 0.0782 mmol). A balloon of hydrogen gas was attached to the flask via a septum cap. The mixture was stirred at room temperature for 5 h. The reaction mixture was filtered over Celite and the filtrate concentrated under reduced pressure to provide the title compound as a light yellow solid (1.741 g, 98%). NMR (400 MHz, DMSO-) delta: 6.85 (d, J= 8.5 Hz, 1H), 6.59 (d, J= 2.6 Hz, 1H), 6.45 (dd, J= 8.5, 2.6 Hz, 1H), 5.01 (s, 2H, disappeared on D2O shake), 2.81- 2.72 (m, 4H), 2.40 (brs, 4H), 2.18 (s, 3H). HPLC-MS (ESI+): m/z 228.2 [35%, (M37C1+H)+], 226.2 [100%, (M35C1+H)+].

16154-62-4, As the paragraph descriping shows that 16154-62-4 is playing an increasingly important role.

Reference£º
Patent; H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas, J.; LAWRENCE, Harshani, R.; (257 pag.)WO2016/22460; (2016); 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.288851-44-5,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)-4-oxobutanoic acid,as a common compound, the synthetic route is as follows.

To a solution of Boc-piperazine (P/N: Lancaster L13363, 500 mg, 2.68 mmol) in DCM(30 ml) was added succinic anhydride (269 mg, 2.68 mmol). The reaction was stirred for 2 hours at ambient temperature. TLC analysis showed formation of succinylated Boc-piperazine (Rf= 0.50; 9:1:0.01 DCM-MeOH-AcOH, TLC developed by heating with 3% (w/v) solution of ninhydrin in EtOH). To this solution was added TFA (30 mL) and the mixture was then stirred for 1 h at ambient temperature. The volatile components of the mixture were removed under reduced pressure and the resulting oil dissolved in THF (30 mL) with minimum amount of water and adjustment of the pH to 9 by the addition of DIPEA. A solution of Fmoc-OSu (907 mg, 2.69 mmol) in THF (10 mL) was added and stirred for 1 h at ambient temperature. TLC analysis showed formation of a product (Rf = 0.55; 9:1:0.01 DCM-MeOH-AcOH, UV 254 nm, TLC developed by heating with 3% (w/v) solution of ninhydrin in EtOH). The volatile components of the mixture were then removed under reduced pressure and the resulting oil was dissolved in minimum volume of saturated NaHCO3. The aqueous solution was then extracted with Et2O (100 mL x 2), acidified (pH ~1) with HCI (1 M) and re-extracted with EtOAc (150 mL x 2). The combined EtOAc layers were dried over Na2SO4 and concentrated to give the product as colorless oil., 288851-44-5

The synthetic route of 288851-44-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; APPLERA CORPORATION; WO2007/87534; (2007); 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.219509-79-2,1-tert-Butyl 4-methyl piperazine-1,4-dicarboxylate,as a common compound, the synthetic route is as follows.

The compound 1-tert-butoxycarbonyl-2,4-piperazine carboxylate (0.18g, 0.61mmol) in dichloromethane(6mL) was added HCl in ethyl acetate solution (4M, 3mL), stirred at rt for 1h, the solvent was removed to give awhite solid 146mg: 1,3-piperazine compound Two carboxylate hydrochloride, yield: 99%., 219509-79-2

219509-79-2 1-tert-Butyl 4-methyl piperazine-1,4-dicarboxylate 11118267, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5753-26-4,5753-26-4, 1-(2-Chloroethyl)-4-methylpiperazine dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) A mixture of 8.5 g of 9-acridanone, 180 ml of dimethylformamide and 3.3 g of sodium hydride is stirred for 0.5 hour, treated portionwise with 10.3 g of 2-[1-(4-methyl)-piperazinyl]ethyl chloride dihydrochloride, stirred at 80 for 3 days and evaporated. The residue is treated with water and extracted with methylene chloride. The extract is washed with water, dried over sodium sulfate and evaporated, whereupon the residue is recrystallized firstly from ether and then from ethyl acetate. There is obtained 10-[2-(4-methyl-1-piperazinyl)ethyl]-9-acridanone of melting point 156-157.

As the paragraph descriping shows that 5753-26-4 is playing an increasingly important role.

Reference£º
Patent; Hoffman-La Roche Inc.; US4711889; (1987); A;,
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.879896-50-1,2-(4-Methylpiperazin-1-ylmethyl)benzylamine,as a common compound, the synthetic route is as follows.,879896-50-1

Example 111 lambda/-Methoxy-4-methyl-3-[3-[[[2-[(4-methyl-1-piperazinyl)methyl]phenyl]methyl]amino]- 2-oxo-1(2H)-pyrazinyl]-benzamideTo a stirred solution of 3-(3,5-dibromo-2-oxo-2H-pyrazin-1-yl)-4-methyl-benzoic acid, methyl ester (Example 1 b, 0.1 g) in tetrahydrofuran (2 ml.) in a microwave vial was added triethylamine (250 mul_) and 2-[(4-methyl-1-piperazinyl)methyl]-benzenemethanamine (90 mg). The reaction was stirred overnight before the addition of O-methylhydroxylamine hydrochloride (83 mg) and cyclopentylmagnesium bromide (2M in diethyl ether, 2 ml.) dropwise. After stirring for 60 minutes, ethanol (2 ml.) was added followed by the addition of ammonium formate (0.4 g) and 10% palladium on carbon (40 mg). The reaction mixture was heated within a microwave for 30 minutes at 100C before being cooled to room temperature, filtered and washed with ethanol. The filtrate was concentrated in vacuo. Purification by preparative HPLC (Gemini column, 0.1 % trifluroacetic acid: acetonitrile eluent) afforded the title compound (13 mg). MS: APCI(+ve) 477 (M+H+).1H NMR delta(DMSO-d6, 400MHz) 7.77 (1 H, d), 7.67 (1 H, s), 7.51 (1 H, d), 7.41 (1 H, d), 7.33 – 7.27 (3H, m), 6.90 (1 H, d), 6.75 (1 H, d), 4.72 (1 H, d), 4.62 (1 H, d), 3.80 – 3.69 (2H, m), 3.69 (3H, s), 3.44 – 3.25 (4H, m), 2.70 (3H, s), 2.50 – 2.35 (2H, m), 2.12 (3H, s).

The synthetic route of 879896-50-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/1132; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1589082-06-3, (S)-tert-Butyl 3-(cyanomethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A reaction mixture of fert-butyl (3,51-3- (cyanomethyl)piperazine-l-carboxylate (850 mg, 3.77 mmol) and HCl/dioxane (4 M, 20 mL) was stirred at 15 C for 1 hour. Upon completion, the solvent was removed under vacuum to give 2-[(25)-piperazin-2-yl]acetonitrile (740 mg, 3.74 mmol, 99.0% yield, 2HC1) as a white solid. NMR (400MHz, METHANOLS) delta = 4.04 – 3.90 (m, 1H), 3.81 – 3.70 (m, 2H), 3.69 – 3.61 (m, 2H), 3.53 – 3.36 (m, 2H), 3.13 (d, J=6.4 Hz, 2H)., 1589082-06-3

As the paragraph descriping shows that 1589082-06-3 is playing an increasingly important role.

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics