Month: July 2021

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,30459-17-7

General procedure: A solution of arylpiperazine (5.5 mmol) and triethylamine (0.8 mL;5.5 mmol) in anhydrous THF (20 mL) was added dropwise to a stirredsolution of an appropriate alkyl [2-/3-(bromoacetyl)phenyl]carbamate(5.5 mmol) in anhydrous THF (30 mL), and the mixture stirred for 3 h atambient temperature. The solvents were removed under reduced pressure,and added chloroform (100 mL) and water. The organic phase waswashed with additional water, dried over anhydrous sodium sulfate andthe solvent removed under reduced pressure, to give a solid crudeproduct, which was recrystallized from acetone.

The synthetic route of 30459-17-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Campos, Ludmila E.; Garibotto, Francisco M.; Angelina, Emilio; Kos, Jiri; Toma?i?, Tihomir; Zidar, Nace; Kikelj, Danijel; Gonec; Marvanova, Pavlina; Mokry, Petr; Jampilek; Alvarez, Sergio E.; Enriz, Ricardo D.; Bioorganic Chemistry; vol. 91; (2019);,
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.21043-40-3,1-Cyclopentylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of 7 (0.1 mmol, 55 mg) in dry dichloromethane (3 ml) was added the appropriate amine (0.12 mmol, 1.2 equiv) and triethylamine (0.12 mmol) at room temperature. After stirring for overnight, the reaction mixture was purified directly by silica gel column chromatography., 21043-40-3

The synthetic route of 21043-40-3 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Jin, Yan; Liu, Jie; Huang, Wen-Ting; Chen, Shi-Wu; Hui, Ling; European Journal of Medicinal Chemistry; vol. 46; 9; (2011); p. 4056 – 4061;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78818-15-2, Benzyl 3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

b) 4-Methyl-l-(4-methyl-3′-nitro-3,4,5,6-tetrahydro-2H-[l,2′]bipyridinyl-6′-yl)- piperazin-2-one; To a solution of 6′-bromo-4-methyl-3′-niuO-3,4,5,6-tetrahydro-2H- [l,2′]bipyridinyl (as prepared in the previous step) (300 mg, 1.00 mmol) in toluene (5 mL) was added 3-oxo-piprazine-l-carboxylic acid benzyl ester (351 mg, 1.50 mmol), K3PO4 EPO (424 mg, 2.00 mmol) and CuI (38 mg, 0.20 mmol) followed by N,N’- dimethylethylenediamine (20 muL, 0.18 mmol) under Ar. The resulting mixture was heated at reflux overnight. The reaction mixture was allowed to cool to room temperature and filtered through a thin pad of Celite. The filtrate was concentrated in vacuo and the residue obtained was purified by chromatography on silica (20% EtOAc: hexane) to obtain 4-(4- methyl-3 ‘ -nitro-3 ,4,5 ,6-tetrahydro-2H- [1,2’ ]bipyridyl-6 ‘ -yl)-3 -oxo-piperazine- 1 – carboxylic acid benzyl ester (258 mg, 57%). This compound (453 mg, 1.00 mmol) was dissolved in 30% HBr/HOAc (1 mL). The resulting mixture was stirred at room temperature overnight and Et2O (20 mL) was added dropwise. The resulting mixture was stirred for another hour, the precipitated hydrobromide was collected by suction filtration, washed with Et2O (3×20 mL), dried in vacuo for 1 h and used directly in next step.The above hydrobromide (48 mg, 0.10 mmol) was added to 37% aq HCHO (ca. 0.05 mL, 0.05 mmol) followed by NaBH(OAc)3 (106 mg, 0.050 mmol). The resulting mixture was stirred at room temperature for 30 min and the product was extracted with CH2Cl2 (3×10 mL). The CH2Cl2 layers were combined, dried (Na2SO4) and concentrated in vacuo. The residue obtained was purified on silica (10-50% EtOAc:hexane) to obtain the title compound (27 mg, 81%). 1H-NMR (CDCl3; 400 MHz): delta 8.21 (d, IH, J=8.9 Hz), 7.58 (d, IH, J=8.9 Hz), 3.98 (m, 2H), 3.75 (m, 2H), 3.31 (s, 2H), 2.96 (m, 2H), 2.72 (m, 2H), 2.39 (s, 3H), 1.9-1.65 (m, 3H), 1.25 (m, 2H), 0.99 (d, 3H, J=6.42 Hz).

78818-15-2, 78818-15-2 Benzyl 3-oxopiperazine-1-carboxylate 736777, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2006/47504; (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.13889-98-0,1-Acetylpiperazine,as a common compound, the synthetic route is as follows.

Example 12[4-(3,3-Bis-{4-[3-(4-acetyl-piperazin-1-yl)-prop-1-ynyl]-phenyl}allylsulfanyl)-2-methylphenoxy]acetic acidA mixture of 1-piperazin-1-yl-ethanone (15.2 g, 0.119 mol; prepared as described in U.S. Pat. No. 2,973,362), 3-bromopropyne (17 g, 0.143 mol) and potassium carbonate anhydrous (21.5 g, 0.156 mol) in 2-butanone (150 mL) was refluxed for 6 h. A separated solid was filtered off, washed with 2-butanone (80 mL) and 2-butanone was evaporated in vacuo. The residue was purified by vacuum distillation to yield 1-(4-prop-2-ynylpiperazin-1-yl)ethanone, b.p. 115 C./7 Torr).Yield: 12.2 g (62%).M.p. 63-65 C.

13889-98-0, 13889-98-0 1-Acetylpiperazine 83795, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Novo Nordisk A/S; High Point Phamaceticals LLC; US2011/39841; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5625-67-2, Piperazin-2-one is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5625-67-2

To a stirred solution of W-1 (20.0 g, 0.200 mol) in DCM, is added Boc anhydride (43.6 g, 0.200 mol), and TEA (40.4 g, 0.400 mol). The mixture is stirred at about 25 C. for about 18 hours. The mixture is concentrated and the residue dissolved in EtOAc then extracted with water. The organic layer is concentrated and the residue is purified by silica gel chromatography to give W-2.

The synthetic route of 5625-67-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Boehringer Ingelheim International GmbH; BYLOCK, Lars Anders; US2013/236468; (2013); 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.

To a solution of czs-2,6-dimethylpiperazine (1.00 g, 8.70 mmol) in CHC13 (20 mL) was added Boc anhydride (1.90 g, 8.70 mmol) drop-wise at 0 C, and the reaction mixture was stirred at room temperature for 16 h. The reaction mixture was diluted with DCM (30 mL) and washed with H20 (30 mL). The organic layer was separated, washed with brine (10 mL), dried over anhydrous Na2S04 and concentrated in vacuo to afford tert-butyl cz5-3,5-dimethylpiperazine-l- carboxylate (1.82 g crude) as an off-white solid. This compound was used as such for the next reaction without further purification. LC/MS (ESI) m/e [M+H]+/RT (min)/%: (0321) 215.00/2.52/83.4%. 1H NMR (400 MHz, DMSO-d6) delta 1.05 (d, J = 6.1 Hz, 6H), 1.20 (d, J = 6.7 Hz, 1H), 1.46 (s, 9H), 2.32-2.40 (m, 2H), 2.72-2.82 (m, 2H), 3.80-4.02 (m, 2H)., 21655-48-1

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

Reference：
Patent; NEUROPORE THERAPIES, INC.; WRASIDLO, Wolfgang; STOCKING, Emily, M.; HALL, Adrian; MACCOSS, Malcolm; (139 pag.)WO2017/20010; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

78551-60-7,78551-60-7, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of diisopropylamine (667 mg, 6.59 mmol) in THF (5 ml) in a dryice-acetone bath was added 1.6 M butyllithium in hexanes (4.13 ml, 6.61 mmol).After 5 min the mixture was put in an ice-water bath and stirred for 20 min. Thesolution was cooled in the dry ice-acetone bath again and a solution of the product ofPreparative Example 1, Step 8 (1.74 g, 5.99 mmol) in THF (20 ml) was added. Themixture was stirred for 1 h. A solution of the above aldehyde in THF (30 ml) wasadded and the mixture was allowed to warm up to RT slowly and stirred for 16 h. Thereaction was quenched with saturated NH4CI (20 ml) and extracted with ether (3x100ml). The combined organic layer was washed with 5% citric acid, saturated NaHCO3,and brine, dried (Na2SO4), concentrated, and purified by column chromatography(gradient EtOAc/Hexanes 0-40%) to give the product (1.20 g, 35%). MS m/e 694

78551-60-7 tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate 10891590, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SCHERING CORPORATION; WO2006/14944; (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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Preparation 20 tert-butyl 4-(2-{[(6′-{2-cyano-4-[(1,2,4-thiadiazol-5-ylamino)sulfonyl]phenoxy}-1,1′:3′,1″-terphenyl-3-yl)carbonyl]amino}ethyl)piperazine-1-carboxylate To a solution of 6′-{2-cyano-4-[(1 ,2,4-thiadiazol-5-ylamino)sulfonyl]phenoxy}-1 , 1′:3′, 1″- terphenyl-3-carboxylic acid (Preparation 21 , 100 mg, 0.18 mmol) in dimethylformamide (2.0 mL) was added 1 , T-carbonylbis(1 H-imidazole) (38 mg, 0.23 mmol) and N-ethyl-N- isopropylpropan-2-amine (35 mg, 0.27 mmol). The mixture was stirred at room temperature for 30 minutes, then tert-butyl 4-(2-aminoethyl)piperazine-1 -carboxylate (41.3 mg, 0.18 mmol) was added. The resulting reaction was stirred at room temperature for 3 days. The mixture was concentrated in vacuo to provide the title compound as an orange gum (204 mg, >100percent). This material was used in the next step without further purification. LCMS Rt = 2.40 minutes MS m/z 764 [M-H]”, 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PFIZER INC.; SWAIN, Nigel Alan; BROWN, Alan Daniel; JONES, Lyn Howard; MARRON, Brian Edward; RAWSON, David James; RYCKMANS, Thomas; STORER, Robert Ian; WEST, Christopher William; WO2015/181797; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 7-benzyl-2,4-dichloro-6,8-dihydro-5H-pyrido[3,4-d] pyrimidine (3.00 g, 10.2 mmol, 1.00 eq), 1-tert-butyl-3-methyl piperazine-1,3-dicarboxylate (2.62 g, 10.7 mmol, 1.05 eq), DIEA (3.30 g, 25.5 mmol, 4.45 mL, 2.50 eq) in DMSO (50.0 mL) was degassed and purged with nitrogen 3 times. The mixture was stirred at 100° C. for 12 hours under a nitrogen atmosphere. The reaction mixture was diluted with DCM (200 mL), washed with brine (3 50 mL), dried over Na 2SO 4, filtered and concentrated under reduced pressure to dryness. The residue was purified by column chromatography (SiO 2, Petroleum ether/Ethyl acetate=10:1 to 3:1) to give 1-tert-butyl 3-methyl 4-(7-benzyl-2-chloro-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)pipera- zine-1,3-dicarboxylate (2.10 g, 3.81 mmol, 37.4% yield, 91.0% purity) as a yellow oil. ESI MS m/z 502.1 [M+H] +.

129799-08-2, As the paragraph descriping shows that 129799-08-2 is playing an increasingly important role.

Reference：
Patent; Mirati Therapeutics, Inc.; Array BioPharma Inc.; Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E.; US2019/144444; (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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

4-[5-(4-Methanesulfonyl-piperazin-1 -yl)-2-methyl-2,3-dihydro-furo[2,3-clpyridin-2-yl1- piperidine-1 -carboxylic acid tert-butyl ester4-(5-Chloro-2-methyl-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1 -carboxylic acid tert-butyl ester (100 mg) is added to a mixture of 1 -(methylsulfonyl)piperazine hydrochloride (70 mg), Pd2(dba)3 (65 mg), Xantphos (123 mg), and potassium tert- butylate (75 mg) in toluene (4 mL) under an argon atmosphere. The reaction mixture is stirred in an oil bath at 105C over night. After cooling to room temperature water is added and the mixture is extracted with ethyl acetate. The combined extracts are concentrated in vacuo and the residue is chromatographed on silica gel(cyclohexane/ethyl acetate 50:50? 0: 100) to give the title compound. LC (method 1 1 ): tR = 1 .03 min; Mass spectrum (EST): m/z = 481 [M+H]+.

161357-89-7, As the paragraph descriping shows that 161357-89-7 is playing an increasingly important role.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HIMMELSBACH, Frank; ECKHARDT, Matthias; HEINE, Niklas; LANGKOPF, Elke; NOSSE, Bernd; WO2012/80476; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics