Month: April 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

Synthesis of (4-(2-amino-9-(3-(4-ethylpiperazin-l-yl)propyl)-9H-purin-6-yl)piperazin-l- yl)(phenyl)methanone (18): Compound 17 was dissolved in acetonitrile (5 mL), potassium carbonate (1.2 g, 0.03 mmol) and phenyl(piperazine-l -yl) methanone (0.84 g, 0.03 mmol) were added. The reaction was stirred for 2 hours under N2 atmosphere condition at 100 C. Acetonitrile was evaporated under the vacuum, then water was added to the reaction mixture to get precipitate which was filter off to get precipitate (0.8 g, yield 70%) of product 18. 1H NMR (300 MHz, CDCI3) delta ppm 7.49 (s, 1H), 7.42 (d, J = 9 Hz, 4H), 4.63 (s, 2H), 4.26 (s, 3H), 4.09 (t, J = 6 Hz, 2H), 3.89 (s, 2H), 3.54 (s, 2H), 2.42 (d, J = 6 Hz, 8H), 2.28-2.40 (m, 3H), 1.85-2.03 (m, 3H), 1.08 (t, J = 6 Hz, 3H). ESI-MS m/z 478.34 (M+H)., 13754-38-6

13754-38-6 1-Benzoylpiperazine 762654, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH; TALUKDAR, Arindam; GANGULY, Dipyaman; MUKHERJEE, Ayan; PAUL, Barnali; RAHAMAN, Oindrila; KUNDU, Biswajit; ROY, Swarnali; DEBLINA, Raychaudhuri; (60 pag.)WO2019/92739; (2019); 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.196811-66-2,tert-Butyl 4-carbamothioylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of terf-butyl 4-carbamothioylpiperazine-1-carboxylate (synthesized according to Example 5, Step 1, 1.3 g, 5.3 mmol) in dioxane (10 mL,), TEA (1 mL,, 7 mmol) and 1-bromo-3,3- dimethylbutan-2-one (0.94 mL,, 6.8 mmol) were added at rt and stirred for 16 h at 90 C. The completion of the reaction was monitored by TLC. The reaction mixture was quenched with water and extracted with EtOAc. The organic layer was dried over anhydrous Na2SO4, concentrated under vacuum and the resulting crude product was taken as such for next step without further purification. Yield: 88% (1.5 g, black liquid). LCMS: (Method A) 326.2 (M+H), Rt. 3.75 min, 60.4% (Max)., 196811-66-2

The synthetic route of 196811-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASCENEURON SA; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; (243 pag.)WO2016/30443; (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.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.

Benzyl 1-piperazinecarboxylate (1.268 mL, 6.575 mmol) and tert-Butyl 2,4-dichloro-5,6-dihydropyrido[3 4-d]pyrimidine-7(8H)- carboxylate (2 g, 6.575 mmol) were dissolved in dimethyl acetamide (10 mL) and treated with N-ethyl-N-isopropylpropan-2-amine (3.445 mL, 19.73 mmol). The reaction mixture was stirred at 85 C for 2 hours. The reaction mixture was cooled to room temperature, diluted with ethyl acetate, washed with water and brine, dried over MgS04, filtered and concentrated. The concentrate was purified by chromatography (CombiFlash, 0%-50% ethyl acetate:Hexanes as the eluent to provide the product (2.69g, 83%). ES+APCI MS m/z 488.2, 490.2 [M+H]+ .

31166-44-6, The synthetic route of 31166-44-6 has been constantly updated, and we look forward to future research findings.

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

5464-12-0,5464-12-0, 1-(2-Hydroxyethyl)-4-methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

NaH (0.039g, 0.96 mmol, 60percent dispersion in oil) was taken up in a dry capped microwave vial. To this, 1-(2-hydroxyethyl)-4-methylpiperazine (0.023g, 0.16mmol) dissolved in dry tetrahydrofuran ( 1.6mL) was added dropwise. The mixture was stirred at rt for 20 min. Intermediate C ( 0.075g, 0.16mmol) was then added in one portion to this suspension and the mixture was heated to 67¡ã C in the closed seal tube for 25 min. The mixture was allowed to reach at rt and quenched with a few drops of methanol. Solvent was removed under vacuum and the resultant crude was subjected to FCC eluting with DCM- MeOH (95/5) to furnish the desired product D ( 0.081g).

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

Reference£º
Patent; ARIAD PHARMACEUTICALS, INC.; ZHU, Xiaotian; WANG, Yihan; SHAKESPEARE, William, C.; HUANG, Wei-Sheng; DALGARNO, David, C.; WO2013/169401; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

4318-42-7, 1-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4318-42-7

Tris(dibenzylideneacetone)dipalladium(0) (0.014 g, 0.02 mmol) was added to a deoxygenated suspension of 1-isopropylpiperazine (0.151 g, 1.18 mmol), methyl 4-bromobenzoate (0.215 g, 1 mmol), potassium carbonate (0.193 g, 1.4 mmol) and 2-dicyclohexylphosphino-2′-(N,N-dimethylamino)biphenyl (0.012 g, 0.03 mmol) in DME (4 mL), and sealed into a microwave tube. The reaction was heated to 130¡ã C. for 10 mins in the microwave reactor and cooled to room temperature. The reaction mixture was evaporated to dryness, redissolved in EtOAc (25 mL) and washed sequentially with water (15 mL) and saturated brine (15 mL). The organic layer was dried over MgSO4, filtered and evaporated to afford crude product. The crude product was purified by silica column chromatography, eluting with 5percent MeOH in DCM. Pure fractions were evaporated to dryness to afford methyl 4-(4-propan-2-yl-piperizin-1-yl)benzoate (0.170 g, 64.8percent) as a tan solid. 1HNMR (399.9 MHz, CDCl3) delta 1.09 (6H, d), 2.66 (4H, t), 2.73 (1H, q), 3.34 (4H, t), 3.86 (3H, s), 6.84-6.88 (2H, m), 7.89-7.93 (2H, m). MS: m/z 264 (MH+).

As the paragraph descriping shows that 4318-42-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; US2008/153812; (2008); 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.21655-48-1,cis-2,6-Dimethylpiperazine,as a common compound, the synthetic route is as follows.

Part A: 1,1 -Dimethylethyl (3R,5S)-3,5-dimethyl-1-piperazinecarboxylate. To a solution of c/s-2,6-dimethylpiperazine (1.142 g, 10 mmol) in dichloromethane (25 ml.) at 0 0C was added dropwise bis(1 ,1-dimethylethyl) dicarbonate (2.161 g, 9.9 mmol) in dichloromethane (6 ml_). The reaction mixture was allowed to warm to room temperature and stirred overnight before being diluted with dichloromethane and washed with saturated aqueous Na2CO3 solution. The aqueous layer was back extracted with dichloromethane once. The combined organic layers were washed with brine, dried (MgSO4) and evaporated to yield 1 ,1-dimethylethyl (3R,5S)-3,5-dimethyl-1- piperazinecarboxylate (2.04 g, 95%). LCMS: (M+H)+: 215.1.

21655-48-1, 21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2009/61879; (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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, 8.5 g (36.2 mmol) of crude I-a, 2.0 g of FeO(OH)/C catalyst and 100 mL of 95% ethanol were added to a 500 mL one-necked flask, and the mixture was heated under reflux, and a mixture of 25 mL of hydrazine hydrate and 20 mL of 95% ethanol was slowly added dropwise. The disappearance of the starting material by TLC (methanol: chloroform = 1:15). The filter cake was washed twice with hot ethanol (30 mL ¡Á 2). The solvent was evaporated under reduced pressure to give a white solid. Vacuum drying (I-a’) 6.7 g, The yield was 90.3%. The product was directly fed to the next reaction without further purification.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Fuxing Pharmaceutical Industrial Co., Ltd.; Lu Shuai; Jin Qiaomei; Wang Yue; Chen Yadong; Lu Tao; (54 pag.)CN104592251; (2019); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

75336-86-6, (R)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a sealed tube, 7-fluoro-2-(2-methylimidazo[1,2-b]pyridazin-6-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (Intermediate 1; 50 mg, 0.169 mmol), and (R)-2-methylpiperazine (68 mg, 0.677 mmol, 4.0 eq.) were stirred in DMSO (2 mL) at 110 C. overnight. The solvent was removed under high vacuum. The residue was taken up in CH2Cl2 and washed with an aqueous saturated solution of NaHCO3. The organic layer was separated and dried over Na2SO4 and concentrated in vacuo. The crude was purified by column chromatography (SiO2, CH2Cl2/MeOH=95/5 to 90/10) to afford the title product (48 mg, 75%) as a light yellow solid. MS m/z 376.3 [M+H+].

75336-86-6, 75336-86-6 (R)-2-Methylpiperazine 7330434, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Hoffmann-La Roche Inc.; PTC Therapeutics, Inc.; Ratni, Hasane; Green, Luke; Weetall, Maria L.; Naryshkin, Nikolai A.; (33 pag.)US2019/315773; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129779-30-2, (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0266] Step 1: (M)-tert-Butyl cis-4-(7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin- 3-yl)-2-oxo-1,2-dihydropyrido[2,3-d]pyrimidin-4-yl)-3,5-dimethylpiperazine-1- carboxylate. Phosphorous oxychloride (0.072 mL, 0.774 mmol) was added dropwise to a solution of (M)-7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3- d]pyrimidine-2,4(1H,3H)-dione (Intermediate 72A, 180 mg, 0.52 mmol) and DIPEA (0.14 mL, 0.83 mmol) in acetonitrile (2 mL). This mixture was heated to 80 oC for 3 h. The reaction mixture was cooled to 10C and DIPEA (0.27 mL) was added followed by cis-3,5-dimethyl- piperazine-1-carboxylic acid tert-butyl ester (0.122 g, 0.57 mmol). This mixture was allowed to warm to rt and stirred at rt for 18 h. The mixture was poured into ice-cold satd. NaHCO3 and stirred vigorously for 10 min. EtOAc was added and the mixture was separated. The organic extracts were dried over Na2SO4, filtered, and concentrated in vacuo. The crude material was used directly in the following step.

129779-30-2, 129779-30-2 (3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate 10822535, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; AMGEN INC.; ALLEN, John Gordon; ALLEN, Jennifer Rebecca; MINATTI, Ana Elena; XUE, Qiufen; WURZ, Ryan Paul; TEGLEY, Christopher M.; PICKRELL, Alexander J.; NGUYEN, Thomas T.; MA, Vu Van; LOPEZ, Patricia; LIU, Longbin; KOPECKY, David John; FROHN, Michael J.; CHEN, Ning; CHEN, Jian Jeffrey; SIEGMUND, Aaron C.; AMEGADZIE, Albert; TAMAYO, Nuria A.; BOOKER, Shon; GOODMAN, Clifford; WALTON, Mary; NISHIMURA, Nobuko; SHIN, Youngsook; LOW, Jonathan D.; CEE, Victor J.; REED, Anthony B.; WANG, Hui-Ling; LANMAN, Brian Alan; (738 pag.)WO2019/213516; (2019); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: The mixtures of (1,1′-thiocarbonyl) bis-1H-imidazole (5 mmol)and suitable derivative of piperazine or thiomorpholine (5 mmol)in methylene chloride (25 ml) were stirred for 24 h at room temperature.The solutions were extracted three times with distilledwater and the organic phases were dried over MgSO4 and evaporated. The obtained thioketones were refluxed for 2 h withhydrazine hydrate (5 mmol). The final thiosemicarbazides werecrystallized from dry methanol.

30459-17-7, As the paragraph descriping shows that 30459-17-7 is playing an increasingly important role.

Reference£º
Article; Mrozek-Wilczkiewicz, Anna; Malarz, Katarzyna; Rejmund, Marta; Polanski, Jaroslaw; Musiol, Robert; European Journal of Medicinal Chemistry; vol. 171; (2019); p. 180 – 194;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics