Tag: M.W:300-400

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

To the reaction flask was added compound 40 (17.57 g, 63.39 mmol)Soluble in methanol,Add 1.7 g of Pd / C,Catalytic hydrogenation at room temperature,TLC tracking, to be completely complete,Diatomaceous earth filtration,The solvent was removed by distillation under reduced pressure,To obtain a crude solid,And then beaten with ether to get pink powder,Drying to give 12.31 g of compound 7-11,Yield: 73.8%., 182618-86-6

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Zhengda Tianqing Pharmaceutical Group Co., Ltd.; Zhang Yinsheng; Gao Yong; Ren Jing; Wang Qinglin; Wang Zhao; (67 pag.)CN106905245; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

N-Indan-5-yl-4-piperazin-1-yl-benzamide To a mixture of 4-(4-carboxy-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (918 mg, 3 mmol) and 5-aminoindan (399 mg, 3 mmol) in methylene chloride (30 mL) was added EDCI (580 mg, 3 mmol) and DMAP (20 mg, 0.16 mmol). The mixture was stirred at room temperature overnight and then extracted with methylene chloride (50 mL) and aqueous hydrochloric acid (1N, 20 mL). The organic layer was washed with water, then sodium hydroxide solution and finally with water and brine. The solution was dried over sodium sulfate and filtered. Solvents were evaporated and the residue was crystallized from ethyl acetate (40 mL) to give 4-[4-(indan-5-ylcarbamoyl)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. This intermediate was dissolved in methylene chloride (5 mL) and trifluroacetic acid (3 mL). The mixture was stirred at room temperature for 1 hr and solvents were evaporated. The residue was extracted with methylene chloride and 1 N sodium hydroxide solution. The organic layer was washed with brine and dried over sodium sulfate. The product, N-indan-5-yl-4-piperazin-1-yl-benzamide was obtained after solvent evaporation (450mg, Yield: 47%). LCMS calc for C20H23N3O (m/e) 321.42, obsd 322.5 (M+H)., 162046-66-4

162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Madrigal Pharmaceuticals, Inc.; BOLIN, David, R.; CHEUNG, Adrian, Wai-hing; HAMILTON, Matthew, Michael; MARCOPULOUS, Nicholas; McDERMOTT, Lee, Apostle; QIAN, Yimin; EP2350311; (2013); B1;,
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.182618-86-6,1-Boc-4-(4-Nitrophenyl)piperazine,as a common compound, the synthetic route is as follows.

To the reaction flask was added compound 40 (17.57 g, 63.39 mmol)Soluble in methanol,Add 1.7 g of Pd / C,Catalytic hydrogenation at room temperature,TLC tracking, to be completely complete,Diatomaceous earth filtration,The solvent was removed by distillation under reduced pressure,To obtain a crude solid,And then beaten with ether to get pink powder,Drying to give 12.31 g of compound 7-11,Yield: 73.8%., 182618-86-6

The synthetic route of 182618-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Zhengda Tianqing Pharmaceutical Group Co., Ltd.; Zhang Yinsheng; Gao Yong; Ren Jing; Wang Qinglin; Wang Zhao; (67 pag.)CN106905245; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

509073-62-5, tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,509073-62-5

To a degassed solution of tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate (2c, 4.1 g, 12.3 mmol, 1 equiv.) in anhydrous MeOH (40 mL) was added Pd/C (10% wt., dry; 600 mg).The reaction was sealed, fifted with a H2 balloon and then stirred for 3 h at room temperature. The reaction mixture was filtered through Celite and then concentrated to obtain the product 2d as a white foam (3.7 g, 12 mmol, 98% yield).

The synthetic route of 509073-62-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; DOBROVOLSKY, Dennis; HUANG, Hai-Tsang; (152 pag.)WO2018/98275; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

479353-63-4,479353-63-4, 1-Boc-4-(4-Carboxybenzyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of compound 5 (1.0 g, 2.81 mmol), compound 7a (0.98 g, 4.19 mmol), HATU (1.28 g, 3.37mmol) in DMF (20 mL) was cooled to 0C and DIPEA (1.95 mL, 11.24 mmol) was added. The reaction mixture was allowed to warm to room temperature and stirred for 15 min. Saturated aqueous sodium bicarbonate (20 mL) was added and the resulting mixture was extracted with ethyl acetate (50 mL><2). The combined extracts were dried over anhydrous sodium sulfate and concentrated. The residue was purified by flash column chromatography on silica gel (petroleum ether/ethyl acetate = 3 : 1 to 1 : 1) to afford compound 8a (1.29 g, 80% yield) as a yellow solid. As the paragraph descriping shows that 479353-63-4 is playing an increasingly important role. Reference：
Patent; INHIBIKASE THERAPEUTICS, INC.; WERNER, Milton, H.; KELLY, Terence, A.; (89 pag.)WO2018/81251; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The 10 mmol of acid (6-8, 11a,b or 14) was dissolved in anhydrous acetonitryle (25 ml). The solution was cooled to -5 C, and triethylamine (1.4 ml, 10 mmol), and then HBTU (3.79 g, 10 mmol) or HATU (3.8 g, 10 mmol), were added. The mixture was stirred for 1 h at -5 C and then 10 mmol of amine 5 was added. The reaction mixture was allowed to stand overnight at room temperature. The residual amount of the activated ether (Bt- or At-ether of starting acid) was destroyed by addition of few drops of N,N-dimethylpropane-1,3-diamine, and the solvent was evaporated in vacuo to dryness. The residue was dissolved in 100 ml of chloroform. The solution was washed with water (40 mL), aqueous solution of 1 M HCl (40 ml) and 5% aqueous solution of NaHCO3 (40 ml). The organic layer was dried over Na2SO4, filtered off, and the solvent was evaporated in vacuo to dryness. The resulting residue was triturated with warm hexane (20 ml), and the precipitate was collected by filtration and dried., 162046-66-4

The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Krysko, Andrei A.; Samoylenko, Georgiy V.; Polishchuk, Pavel G.; Fonari, Marina S.; Kravtsov, Victor Ch.; Andronati, Sergei A.; Kabanova, Tatyana A.; Lipkowski, Janusz; Khristova, Tetiana M.; Kuz’Min, Victor E.; Kabanov, Vladimir M.; Krysko, Olga L.; Varnek, Alexandre A.; Bioorganic and Medicinal Chemistry; vol. 21; 15; (2013); p. 4646 – 4661;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-34-8, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At room temperature, 3.5 g (10 mmol) of intermediate Ib was dissolved in 35 mL of 90% EtOH and heated to 70 C. 0.44 g (1.5 mmol) of FeCl · 6H2O and 0.038 g (3 mmol) of activated charcoal were added and stirred for 10 min. A solution of 6.73 g (100 mmol) of 80% hydrazine hydrate was added dropwise and heated to 90 C for 2 h. Reaction is completed, the hot filter, the solvent evaporated to dry the crude product, and then add 50mL of crude water, the platform stirring 0.5h, filter, filter cake with a small amount of water rinse, dry pale yellow solid 2.5g, yield 78.6 %, 154590-34-8

The synthetic route of 154590-34-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shenyang Red Flag Pharmaceutical Co., Ltd.; Li Juan; Yang Bo; Li Xingyuan; Zhang Tiejie; Sun Jukui; (19 pag.)CN107033095; (2017); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

350684-49-0, tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of tert-butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate (2d, 1.7 g, 5.7 mmol, 1 equiv.), 3,5-dibromo-1-methylpyrazin-2(1H)-one (2e, 1.8 g, 6.8 mmol, 1.2 equiv.)and N,N-diisopropylethylamine (1.48 mL, 8.5 mmol, 1.5 equiv.) in N,N-dimethylacetamide (5 mL) was stirred in a sealed vial at 105 C for 30 h. The reaction was cooled to room temperature and EtOAc (20 mL) was then added. The solid precipitate was filtered and dried on high vacuum overnight to provide tert-butyl 4-(4-((6-bromo-4-methyl-3-oxo-3 ,4- dihydropyrazin-2-yl)amino)benzoyl)piperazine- 1 -carboxylate 2f. The product was carriedonto the next step without further purification., 350684-49-0

350684-49-0 tert-Butyl 4-(4-aminobenzoyl)piperazine-1-carboxylate 2763355, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; DOBROVOLSKY, Dennis; HUANG, Hai-Tsang; (152 pag.)WO2018/98275; (2018); 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.149057-19-2,4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid,as a common compound, the synthetic route is as follows.

CS2CO3 (0.5 eq) was added to a stirred solution of 4-((benzyloxy)carbonyl)-l-(tert- butoxycarbonyl)piperazine-2-carboxylic acid (1.0 eq) in EtOH (0.54 M) . Stirring was continued at 20 C for 2 h then solvent was evaporated and cesium 4-((benzyloxy)carbonyl)-l-(tert-butoxycarbonyl)-l,4-diazepane-5-carboxylate was dried at high vacuum pump for 1 h, then it was dissolved with DMF (0.54 M) and 2-bromo-l-(naphthalen-2-yl)ethan-l-one (1.0 eq) was added. The mixture was stirred at 20 C for 1 h, then DMF was removed under reduced pressure co- evaporating with toluene. The residue was diluted with EtOAc and filtered off. Filtrate was evaporated to give 4-benzyl 1 -(tert-butyl) 2-(2-(naphthalen-2-yl)-2-oxoethyl) piperazine-1,2,4-tricarboxylate. The latter was dissolved with toluene (0.13 M) and NH4OAc (20 eq) was added. The mixture was stirred at reflux using a Dean Stark apparatus for 30 min. Toluene was removed under reduced pressure, the residue was diluted with EtOAc, washed with sat. aq. NaHC03, brine, dried and concentrated to give an orange oily residue. This material was purified by flash chromatography (petroleum ether/EtOAc from 95:5 to 20:80) to give the title compound (86%) as an orange solid. MS (ES+) m/z 513 (M+H)+.

149057-19-2, As the paragraph descriping shows that 149057-19-2 is playing an increasingly important role.

Reference：
Patent; IRBM SCIENCE PARK S.P.A.; C.N.C.C.S. S.C.A.R.L. COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING; BIANCOFIORE, Ilaria; CIAMMAICHELLA, Alina; FERRIGNO, Federica; HARPER, Steven; MALANCONA, Savina; ONTORIA ONTORIA, Jesus Maria; PAONESSA, Giacomo; PONZI, Simona; SUMMA, Vincenzo; (143 pag.)WO2018/115275; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

162046-66-4, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The 10 mmol of acid (6-8, 11a,b or 14) was dissolved in anhydrous acetonitryle (25 ml). The solution was cooled to -5 C, and triethylamine (1.4 ml, 10 mmol), and then HBTU (3.79 g, 10 mmol) or HATU (3.8 g, 10 mmol), were added. The mixture was stirred for 1 h at -5 C and then 10 mmol of amine 5 was added. The reaction mixture was allowed to stand overnight at room temperature. The residual amount of the activated ether (Bt- or At-ether of starting acid) was destroyed by addition of few drops of N,N-dimethylpropane-1,3-diamine, and the solvent was evaporated in vacuo to dryness. The residue was dissolved in 100 ml of chloroform. The solution was washed with water (40 mL), aqueous solution of 1 M HCl (40 ml) and 5% aqueous solution of NaHCO3 (40 ml). The organic layer was dried over Na2SO4, filtered off, and the solvent was evaporated in vacuo to dryness. The resulting residue was triturated with warm hexane (20 ml), and the precipitate was collected by filtration and dried., 162046-66-4

The synthetic route of 162046-66-4 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Krysko, Andrei A.; Samoylenko, Georgiy V.; Polishchuk, Pavel G.; Fonari, Marina S.; Kravtsov, Victor Ch.; Andronati, Sergei A.; Kabanova, Tatyana A.; Lipkowski, Janusz; Khristova, Tetiana M.; Kuz’Min, Victor E.; Kabanov, Vladimir M.; Krysko, Olga L.; Varnek, Alexandre A.; Bioorganic and Medicinal Chemistry; vol. 21; 15; (2013); p. 4646 – 4661;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics