Month: November 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13349-91-2,1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride,as a common compound, the synthetic route is as follows.

General procedure: To a stirred suspension of 5-chloro-2-[[5-methyl-3-(6-methyl-3-pyridyl)isoxazol-4- yl]methyl]pyridazin-3-one (building block A, 300 mg, 0.947 mmol) and (R)-3- hydroxypyrrolidine (0.14 mL, 1.73 mmol) in DMSO (0.5 mL) and acetonitrile (3 mL) was added potassium carbonate (393 mg, 2.84 mmol) Then the reaction mixture was stirred at 70 C for 18 h. After cooling to room temperature the reaction mixture was diluted with EtOAc (80 mL) was washed three times with water (10 mL) and brine (10 mL). The aqueous layers were back extracted twice with EtOAc (80 mL). The combined organic extracts were dried (Na2S04), filtered and concentrated in vacuo. Purification by flash chromatography (silica, gradient: 0% to 10% MeOH in CH2CI2) afforded the title compound (341 mg, 93 %) as an off-white foam. MS (ESI): 368.2 ([M+H]+).

13349-91-2, 13349-91-2 1-(2,2,2-Trifluoroethyl)piperazine dihydrochloride 16312067, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CECERE, Giuseppe; GROEBKE ZBINDEN, Katrin; HERNANDEZ, Maria-Clemencia; KNUST, Henner; KOBLET, Andreas; OLIVARES MORALES, Andres Miguel; PATINY-ADAM, Angelique; PINARD, Emmanuel; RUNTZ-SCHMITT, Valerie; STEINER, Sandra; (328 pag.)WO2019/238633; (2019); A1;,
Piperazine – Wikipedia
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13754-38-6, 1-Benzoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 18: N-{[1-(2-(4-benzoylpiperazine-1-yl)propane-1-yl)-pyrrolidin e-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide [Show Image] 400 mg (1.07 mmol) N-{[1-(2-hydroxypropyl)-pyrrolidin e-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide and 0.18 ml(1.29 mmol, 1.2 eq.)triethylamine described in manufacturing example 6 were dissolved to 20 ml dichloromethane and cooled to 3C under argon gas. 135 mg (1.18 mmol, 1.1 eq.) methansulfonyl chloride were slowly added to reaction solution and stirred at same temperature for 30 min. 20 ml purified water were added and then the organic layer was separated and concentrated with decompression. After 10 ml acetonitrile were added to obtained residues and dissolved them, 444 mg (3.21 mmol) potassium carbonate and 202 mg (1.06 mmol) 1-benzoylpiperazine were added. After stirring for 2 hours at room temperature, 15 ml saturated sodium chloride aqueous solution were added to the reaction solution and was extracted twice with 15 ml ethylacetate. After the organic layer was collected and dried with anhydrous magnesium sulfate, it was concentrated with decompression. 30 mg (51%) target compound as light-yellow solid were yielded by purifying obtained residues with chromatography using silicagel (mobile phase: dichloromethane/methanol=5:1 and 1:1). 1H NMR(400MHz,DMSO-d6) 1.05(3H,s), 1.55-1.65(1H,m), 2.00-2.10(1H,m), 2.15-2.25(1H,m), 2.28-2.55(9H,m), 2.70-2.85(2H,m), 3.17(1H,d) 3.54-3.65(2H,m), 3.87(2H,d), 4.10-4.20(1H,m) 7.35-7.40(2H,m), 7.40-7.47(3H,m), 7.74(1H,t), 7.92(1H,d), 8.14(1H,s) 8.18(1H,d) 8.23(1H,s), 9.01(1H,t) MS (M)+ 545.6, 13754-38-6

As the paragraph descriping shows that 13754-38-6 is playing an increasingly important role.

Reference£º
Patent; Yang Ji Chemical Co., Ltd.; EP2452939; (2012); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 4-chloro-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine 12 (1 g, 4.34 mmol) and 1,4-dioxa-8-azaspiro[4.5]decane (0.62 g, 4.34 mmol) in 2-propanol (30 mL) or 95% ethanol for other amines was refluxed for two hour. The white solid formed in the hot solution was collected after cooling and further recrystallized from ethanol yielded white crystals of compound 13a (67%), 30459-17-7

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

Reference£º
Article; Abdelazeem, Ahmed H.; Abdelatef, Shaimaa A.; El-Saadi, Mohammed T.; Omar, Hany A.; Khan, Shabana I.; McCurdy, Christopher R.; El-Moghazy, Samir M.; European Journal of Pharmaceutical Sciences; vol. 62; (2014); p. 197 – 211;,
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.142-64-3,Piperazine Dihydrochloride,as a common compound, the synthetic route is as follows.

Weigh between dimethylaminobenzoate 8.26g (0.05mol) was dissolved in 20ml of dry tetrahydrofuran was slowly added CDI8.9g (0.055mol), at room temperature for 4hAfter the reaction solution through a dropping funnel was added dropwise to a solution of constant piperazine dihydrochloride 20g (0.125mol), anhydrous piperazine 10g (0.125mol), 60ml of an aqueous solution of sodium chloride, 14g, and reacted for 5 hours at room temperature . After completion of the reaction by suction, the filtrate evaporated to remove THF, 10ml ethyl acetate again, NaOH saturated solution was adjusted to pH = 10, and the combined organic phase was extracted 3 times with ethyl acetate. The organic phase was dried over anhydrous sodium sulfate overnight, pumping filtered, spin dry ethyl acetate, the resulting white crystals is N, N- dimethyl-3- (piperazin-1-yl-carbonyl) aniline crude product 6.4g, 55% yield., 142-64-3

As the paragraph descriping shows that 142-64-3 is playing an increasingly important role.

Reference£º
Patent; Xi’an Jiaotong University; Zhang, Jie; Lu, Wen; Dong, Jinyun; Pan, Xiaoyan; He, Langchong; Zhang, Tao; Wang, Sicen; Shen, Xiuxiu; (16 pag.)CN104262238; (2016); B;,
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.171504-98-6,Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate,as a common compound, the synthetic route is as follows.

LiHMDS (9.9 mL of 1 M, 9.9 mmol) was added to a solution of 1,4-di-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (2.0 g, 5.8 mmol) in THF (30 mL) at -78 C under N2. After 45 minutes, iodomethane (615 muL, 9.9 mmol) in THF (5 mL) was added slowly. The mixture was allowed to warm slowly to ambient temperature and stirred overnight. The reaction mixture was partitioned between DCM and saturated aqueous NH4Cl solution. The organic phase was dried, filtered and concentrated in vacuo. The residue was purified by column chromatography (silica, DCM/MeOH elution) to give 1,4-di-tert-butyl 2-methyl 2-methylpiperazine-1,2,4- tricarboxylate as a colourless oil (1.5 g, 72%); MS m/z: 359 (M+H)+

171504-98-6, The synthetic route of 171504-98-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GMBH; VERTEX PHARMACEUTICALS INCORPORATED; BAYLY, Andrew; BLEICH, Matthew; CHARRIER, Jean-Damien; DODD, James; DURRANT, Steven; ENO, Meredith Suzanne; ETXEBARRIA I JARDI, Gorka; EVERITT, Simon; FRAYSSE, Damien; KELLY, Shazia; KNEGTEL, Ronald; MOCHALKIN, Igor; MORTIMORE, Michael; NORTH, Kiri; PORICHIS, Filippos; PULLIN, Robert; RUTHERFORD, Alistair; STORCK, Pierre-Henri; TWIN, Heather Clare; XIAO, Yufang; (1159 pag.)WO2019/148132; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

142-64-3, Piperazine Dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 5.1.5 1-[3-(Trifluoromethyl)benzoyl]piperazine (8a) A solution of 3-(trifluoromethyl)benzoic acid (9.5 g, 0.05 mol) and CDI (8.90 g, 0.055 mol) was stirred in 30 ml anhydrous THF at room temperature for 30 min. In a separate round bottom flask added piperazine (10.76 g, 0.125 mol) and piperazine dihydrochloride (20 g, 0.125 mol) in 60 ml of water. The reaction mixture was stirred for 5 min and added 14 g NaCl. Then add the brine solution to the round bottom flask containing acyl imidazole and stir the reaction mixture for 5 h. The mixture was filtered and the filtrate distilled by rotary evaporation to remove THF. The aqueous layer was washed with ethyl acetate (3 * 10 ml) to remove diacylated product. The pH of the aqueous layer was adjusted to about 9 using saturated solution of NaOH and washed with ethyl acetate (4 * 30 ml). The organic layer was washed with water (4 * 25 ml), dried over anhydrous Na2SO4 for overnight, concentrated by rotary evaporation and purified by flash chromatography to afford 1-[3-(trifluoromethyl) benzoyl]piperazine as colorless solid (6.5 g, 50%). The intermediate compounds 1-(3-fluorobenzoyl)piperazine (8b), 1-(3-methoxybenzoyl)piperazine (8c), 1-(4-tert-butylbenzoyl)piperazine (8d), N,N-dimethyl-3-(piperazin-1-ylcarbonyl)aniline (8e), 1-(4-bromobenzoyl) piperazine (8f) and 1-(2,4-dichlorobenzoyl) piperazine (8g) were prepared by commercially available materials 3-fluorobenzoic acid, 3-methoxybenzoic acid, 4-tert-butylbenzoic acid, 3-(dimethylamino) benzoic acid, 4-bromobenzoic acid and 2,4-dichlorobenzoic acid respectively using the similar procedure of 1-[3-(trifluoromethyl)benzoyl]piperazine (8a) described above., 142-64-3

The synthetic route of 142-64-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Dong, Jinyun; Pan, Xiaoyan; Wang, Jinfeng; Su, Ping; Zhang, Lin; Wei, Fen; Zhang, Jie; European Journal of Medicinal Chemistry; vol. 101; (2015); p. 780 – 789;,
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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

129779-30-2, To a solution of tert-butyl czs-3,5-dimethylpiperazine-l-carboxylate (1.80 g, 8.40 mmol) in DCM (20 mL) was added a 37% HCHO solution (0.34 mL, 12.0 mmol) dropwise at 0 C, followed by portion- wise addition of Na(OAc)3BH (2.31 g, 10.9 mmol). The reaction mixture was stirred at room temperature for 4 h. The reaction mixture was diluted with DCM (30 mL) and washed with NaHC03 (20 mL) solution. The organic layer was separated, washed with brine (20 mL), dried over anhydrous Na2S04 and concentrated in vacuo to afford tert-butyl czs-3,4,5- trimethylpiperazine-l-carboxylate (1.81 g crude) as a colorless liquid. This compound was used as such for the next reaction without further purification. LC/MS (ESI) m/e [M+H]+/RT (min)/%: 228.90/4.29/88.5%. 1H NMR (400 MHz, CDC13) delta 1.08 (d, J = 6.1 Hz, 6H), 1.48 (s, 9H), 2.04-2.18 (m, 2H), 2.26 (s, 3H), 2.56-2.62 (m, 2H), 3.78-3.98 (m, 2H).

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; 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

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,78818-15-2

EXAMPLE A; Preparation of Compound A of Formula 1 Process for the Preparation of Compound A-In-2:[00118] This compound was prepared by the method described by Bryant, HJ. et al, in WO 01/44250.[00119] To a stirred and cold (ice-bath cooling) suspension of benzyl 3- oxopiperazine-1-carboxylate (A-In-I) (1.00 g) and K2CO3 (11.8 g) in CH2Cl2 (40 mL) was added under N2 trimethyloxonium tetrafluoroborate (2.20 g, from Aldrich) in one portion. The cooling bath was removed and the mixture was stirred at room temperature under N2 for 19 h. This mixture was poured into water (40 mL) under ice-cooling and the organic phase was collected. The aqueous phase was extracted with CH2Cl2. The combined CH2Cl2 phases were washed with water (20 mL), then with brine, dried (Na2SO4) and concentrated. The crude residual oil was purified by silica gel column chromatography (5% MeOH/CH2Cl2) to give the title compound A- In-2 as colorless oil.

The synthetic route of 78818-15-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2009/158394; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

57260-71-6, tert-Butyl piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

57260-71-6, Example 24 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate A mixture of tert-butyl piperazine-1-carboxylate (5.0 g, 26.9 mmol), 1,2-dibromoethane (25 mL), DIPEA (3.5 g, 26.9 mmol) was stirred at 30¡ã C. under argon for 72 h. The solvent was removed under reduced pressure and the residue was purified by column chromatography on silica gel (1-2percent methanol/dichloroethane) to afford the desired product (2.8 g, 36percent yield) as a solid. ESI-MS m/z: 293.1[M+1]+.

The synthetic route of 57260-71-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ren, Pingda; Liu, Yi; Li, Liansheng; Feng, Jun; Wu, Tao; US2014/288045; (2014); 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.154590-34-8,tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of 4-(2-fluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (29.1 g, 89.4 mmol) in MeOH (150 mL) and DCM (10 mL) mixture was added Raney Ni (5.5 g) and the Parr shaker was charged with hydrogen to 50 psi for 1 h. The initial yellow solution became clear and the content was filtered, washed with MeOH and the combined filtrate evaporated to dryness. The residue was dissolved in dry dioxane (20 mL) and a 4M HC1 solution in dioxane (30 mL) was added. The solution was warmed to 45 C in a water bath and stirred vigorously overnight producing a white precipitate. After filtering and washing with cold dioxane and diethyl ether and drying in vacuo, 23.1 g (96%) of the title compound was isolated as a white solid. N1HMR (400 MHz, DMSO-4 delta (ppm): 10.5 (br. s., 1 H), 9.63 (br. s., 2H), 8.0 (br. s., 2H), 7.29 (d, J = 12.6 Hz, 1 H), 7.20 – 7.19 (m, 2H), 3.24 (d, J = 4.8 Hz, 4H), 3.19 (br. s., 4H). 19F NMR (376 MHz, DMSO-d6) delta (ppm): – 120.36 (dd, J = 13.6, 7.2 Hz, IF)., 154590-34-8

154590-34-8 tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate 16203508, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ANACOR PHARMACEUTICALS, INC.; HERNANDEZ, Vincent, S.; DING, Charles; PLATTNER, Jacob; ALLEY, Michael, Richard Kevin; ZHANG, Yong-Kang; ZHANG, Yanchen; WO2011/37731; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics