Month: June 2021

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.,192130-34-0

64-1) 1-[2-(4-Fluorobenzoylamino)ethyl]-4-(t-butoxycarbonyl)piperazine The 1-(2-aminoethyl)-4-(t-butoxycarbonyl)piperazine (1.33 g) obtained in Example 58 and 4-fluorobenzoyl chloride (1.1 g) were dissolved in tetrahydrofuran (20 ml), then triethylamine (1.6 ml) was added thereto, and the mixture was stirred overnight at room temperature. The organic layer was partitioned by adding aqueous saturated sodium bicarbonate and ethyl acetate, and the organic layer was washed with water, dried, and evaporated. The residue was purified by Cromatorex NH silica gel column chromatography (hexane/ethyl acetate system), whereby the title compound (1.42 g, 70 percent) was obtained as a colorless oil.

192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Eisai Co., Ltd.; EP1099692; (2001); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound 2Sa (3.0 g, 18.8 mmol), compound 2Sb (3.0 g, 13.8 mmol, 100% ee) and potassium hydroxide (2.4 g, 42.8 mmol) were added sequentially to 30 mL DMSO while stirring. The reaction mixture was heated to 30C. for 3 hours and then warmed to 60C. for 5 hours. After completion of the reaction, the system was cooled to room temperature, 300 mL of water was added, precipitation formed, and stirring was continued at room temperature overnight. Solid was collected via filtering, and and was added to 25 mL of a mixed solvent consisting of 5:1 petroleum ether:ethyl acetate, and stirred at room temperature for half an hour. The solid was collected via filtering, and was dried to give compound 2Sc (3.0 g, yield 64%) as a yellow solid. MS 336.2 [M+H]+.

314741-40-7, As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference：
Patent; Hangzhou Innogate Pharma Co., Ltd.; ZHANG, Hancheng; LIU, Shifeng; (40 pag.)US2019/100531; (2019); 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, To a solution of thiocarbonyldiimidazole (2.1 g, 11.8 mmol) in tetrahydrofuran (30 mL) at room temperature, was added 1,1 -dimethylethyl 1-piperazinecarboxylate (2.0 g, 10.7 mmol). The reaction mixture was stirred at room temperature for 2 h and then heated to 55 C for additional 2 h. The reaction mixture was cooled to room temperature and concentrated under reduced pressure until approximately 20 mL of tetrahydrofuran remained. The residue was then treated with a 2 M solution of ammonia in methanol (10 mL) and stirred at room temperature for 24 h. The reaction mixture was concentrated under reduced pressure, and the residue was triturated with diethyl ether (25 mL) to give a white precipitate. The precipitate was filtered and dried to give 1.5 g of the title compound as a white solid..H NMR (CDCI3) delta 1.39 (s, 9H), 3.32 (m, 4H), 3.73 (m, 4H), 7.49 (br s, 2H).

As the paragraph descriping shows that 57260-71-6 is playing an increasingly important role.

Reference：
Patent; E. I. du Pont de Nemours and Company; DUNG, Mei H.; PASTERIS, Robert, James; WO2011/72207; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21043-40-3, 1-Cyclopentylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1-cyclopentyl Piperazine(507 mg, 0.003 mmol) was added to a stirred solution of 6 (1 g, 0.0029 mmol) in dry 1,4-Dioxaneand DIPEA (0.7 mL,0.005 mmol). The solution was stirred for 4 h at room temperature. After adding water a precipitate was formed which was filtered to give compound 7 (1.1g, 86% yield) as white solid (m.p-156-159 C).1H NMR (300 MHz, CDCl3) ^ 1.39 – 1.50 (m, 2H), 1.58 (dd, J=7.72, 4.71 Hz, 2H), 1.68 – 1.75 (m, 2H), 1.88 (br. s, 2H), 2.51 – 2.60 (m, 1H), 2.64 – 2.70 (m, 4H), 3.66 – 3.71 (m, 1H), 3.76 – 3.82 (m, 4H), 3.96 (s, 3H), 5.25 (s, 2H), 7.06 (s, 1H), 7.18 (s, 1H), 7.31 – 7.41 (m, 3H), 7.42 – 7.48 (m, 2H).ESI [M+H]+:453.40., 21043-40-3

21043-40-3 1-Cyclopentylpiperazine 806421, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH; TALUKDAR, Arindam; GANGULY, Dipyaman; PAUL, Barnali; MUKHERJEE, Ayan; ROY, Shounak; ROY, Swarnali; GHOSH, Amrit Raj; BHATTACHARYA, Roopkatha; RAHAMAN, Oindrila; KUNDU, Biswajit; (89 pag.)WO2017/163264; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1001180-21-7, (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 4: (Reaction run in a 20-mL plastic bottle): To a solution of (R)-tert-butyl 4-(5- methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-l-carboxylate (0.250 g, 0.752 mmol) in 5 mL DCM was added DAST (0.795 mL, 6.02 mmol). The reaction mixture was capped and stirred at room temperature for 45 hours, after which it poured into ice saturated NaHCO3. The mixture was extracted with 2 x 40 mL DCM, and the combined extracts were dried (Na2SO4), filtered, and concentrated in vacuo. The crude was purified on silica gel (Biotage 40S) eluting with 6:1 to 3:1 hexanes:EtOAc to give (R)-tert-butyl 4-(7,7-difluoro-5-methyl-6,7-dihydro- SH-cyclopenta^pyrimidin^-ytypiperazine-l-carboxylate (0.092 g, 34.5% yield) as a yellow oil. MS (APCI+) m/z 355 [M+H]+.

1001180-21-7, 1001180-21-7 (R)-tert-Butyl 4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-1-carboxylate 59580350, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; MITCHELL, Ian S.; BLAKE, James F.; XU, Rui; KALLAN, Nicholas C.; XIAO, Dengming; SPENCER, Keith Lee; BENCSIK, Josef R.; LIANG, Jun; SAFINA, Brian; LI, Jun; CHABOT, Christine; WO2008/6032; (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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1-fluoro-4-nitrobenzene (1.460 g, 10.4 mmol) and potassium carbonate (4.29 g, 31.0 mmol) were suspended inanhydrous DMF (10 mL) . (S)-tert-butyl 3- (hydroxymethyl)piperazine-1-carboxylate (2.35 g, 10.9 mmol) was added and the mixture was heated at 90 C for 21 h. After cooling the mixture was partitioned between brine/water (100 mL) and ethyl acetate (25 mL) . Theaqueous layer was separated and further extracted with ethyl acetate (3 x 25 mL) . The combined ethyl acetate fractions were washed with brine/water (1:1, 4 x 25 mL), dried (anhydrous sodium sulfate), filtered and reduced in vacuo. The resulting residue was purified by silica gelchromatography (gradient 25-100% ethyl acetate incyclohexane) to afford the title compound (0.99 g, 28.4%) . ?H NMR (400 MHz, CDC13) : 3 8.12 (d, 2H), 6.83 (d, 2H),4.20-4.46 (m, 1H), 4.02-4.14 (m, 2H), 3.48-3.76 (m, 3H),3.08-3.30 (m, 3H), 2.86 (br s, 1H), 1.50 (s, 9H) . LCMS(Method C) : = 1.38 mi m/z = 338 [M+H]., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of intermediate 6 (200 mg, 0.53 mmol ) and 1-(methylsulfonyl)piperazine hydrochloride (87 mg, 0.53 mmol) in dry toluene (5 ml_), sodium tert butoxide (150 mg, 1.6 mmol) was added at RT and the resulting solution was flushed with nitrogen for 10 min. BINAP (66 mg, 0.1 mmol), Pd (dba (98 mg, 0.1 mmol) were added and the reaction mixture was flushed again with nitrogen for 10 min. It was then stirred at 100 C overnight. After completion of the reaction, the reaction mixture was diluted with EtOAc (20 mL) and filtered through celite pad. The filtrate was concentrated under vacuum and resulting crude product was purified by flash chromatography (Eluent: 47% EtOAC in pet ether) to afford the title compound. Yield: 5% (1 1 .3 mg, off-white solid). 1H NMR (400 MHz, DMSO-cfe): d 7.09 (d, J = 8.4 Hz, 2H), 6.92-6.90 (m, 3H), 6.85 (d, J = 2.0 Hz, 1 H), 6.82-6.80 (m, 1 H), 4.22 (s, 4H), 3.61 (d, J = 12.8 Hz, 1 H), 3.23-3.20 (m, 10H), 2.92 (s, 3H), 2.1 1 -2.06 (m, 2H), 1.72-1.68 (m, 2H), 1.56-1.48 (m, 1 H). LCMS: (Method A) 458.1 (M +H), Rt.1.570 min, 99.4% (Max). HPLC: (Method A) Rt. 3.038 min, 99.5% (Max), 99.4% (220 nm).

161357-89-7, 161357-89-7 1-(Methylsulfonyl)piperazine hydrochloride 16265612, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; WISHART, Grant; KULKARNI, Santosh S.; RAKESH, Paul; (338 pag.)WO2020/39027; (2020); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of the 3-(bromoacetyl)-6-methoxy-2- methylbenzonitrile (2.25 g, 8.40 mmol) in THF was added tert-butyl (35)-3- (hydroxymethyl)piperazine-l -carboxylate (2.18 g, 10.8 mmol) and Hunig’s Base (2.93 mL, 16.8 mmol). The reaction was allowed to stir at RT for 16 hours. TLC showed good reaction at that point. The crude reaction was adsorbed onto silica gel, and purified by silica gel flash chromatography to afford the title compound., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (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.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.

59878-57-8, To the reaction flask was added compound 6 (prepared in Example 3-2, 256.5g,0.86mol), CDI (139.45g, 0.86mol), 1.6LTHF, after stirring for 0.5h Compound 7 (138.8g,0.90mol) at room temperature The reaction 3h, after completion of the reaction, water was added to quench the reaction, of THF was distilled off under reduced pressure, theresidue was dissolved in ethyl acetate was added, the organic phase was separated,washed with water three times, the organic phase was dried over anhydrous Na 2SO 4Dried,filtered and concentrated to give Ola Trapani (356.3g, 0.82mol), yield 95%, HPLC purity 99.8%.

59878-57-8 1-(Cyclopropylcarbonyl)piperazine 2064235, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shandong Luoxin Pharmaceutical Group Heng Xin Pharmaceutical Co. Ltd.; Li, Hua; Wang, Chunyan; Liu, Shuxin; (8 pag.)CN105820126; (2016); 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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

General procedure: To a solution of 3-iodo-4-methylbenzoyl chloride obtained above in dry DCM (10mL) at 0C was added Et3N (0.28mL, 2.0mmol) and 4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) aniline (328mg, 1.2mmol). The mixture was stirred at room temperature for 5h, and then the solvent was removed under reduced pressure. The residue was purified by using column chromatography to afford the corresponding product 6-1 (439mg, 2 steps yield: 85%)., 694499-26-8

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Liu, Yang; Peng, Xia; Guan, Xiaocong; Lu, Dong; Xi, Yong; Jin, Shiyu; Chen, Hui; Zeng, Limin; Ai, Jing; Geng, Meiyu; Hu, Youhong; European Journal of Medicinal Chemistry; vol. 126; (2017); p. 122 – 132;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics