Month: September 2021

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.

Stage 1: 4-Benzyl 1 -tert-butyl 2-cyclopentyl piperazi ne-i ,2,4-tricarboxylate 4-[(Benzyloxy)carbonyl]- 1 -(tert-butoxycarbonyl)piperazi ne-2-carboxylic acid (9.96 g, 27 mmol) was dissolved in DCM (50 mL) and cooled to 0CC. Cyclopentanol (7.4 mL, 82 mmol), EDO (7.86 g, 41 mmol) and DMAP (0.33 g, 2.7 mmol) were then added and the reaction allowed to warm to RT, and stirred for 24 hrs. Water (100 mL) and DCM (50 mL) were then added and the layers separated. The aqueous layer was reextracted with DCM (2 x 50 mL) and the combined organic layers were then dried over Mg504 and concentrated in vacuo. Purification by column chromatography (40% EtOAc/heptane) afforded the title compound as a colourless oil (10.4 g, 88%). LCMS: m/z 455 [M+Na]., 149057-19-2

The synthetic route of 149057-19-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHROMA THERAPEUTICS LTD; DAVIES, Stephen John; PINTAT, Stephane; NORTH, Carl Leslie; MOFFAT, David Festus Charles; WO2014/1802; (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.129779-30-2,(3R,5S)-rel-tert-Butyl 3,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a 20 mL microwave reactor vial was added (3R,5S)-tert-butyl 3,5-dimethylpiperazine- 1 -carboxylate (250 mg, 1.1 67mmol), 1,3 -dibromo-5 -fluorobenzene(592 mg, 2.333 mmol), C52CO3 (950 mg, 2.92 mmol) and toluene (4 mL). The vessel was purged and degassed with N2, then 2,2?-bis(diphenylphosphino)- 1,1 ?-binaphthalene(109 mg, 0.175 mmol) and palladium(II) acetate (52.4 mg, 0.23 3 mmol) were added. The reaction vessel was purged and degassed again. The reaction vessel was capped and the mixture was stirred at 110 C overnight. The reaction mixture was filtered and washed with MeOH and then solvent was removed. The crude was diluted with EtOAc (20 mL),and washed with H20 (20 mL). The orange organic layer was washed with brine, dried over with MgSO4, then concentrated to give crude tert-butyl 4-(3-bromo-5-fluorophenyl) piperazine-1-carboxylate, which was then dissolved in 20% TFA in DCM. The mixture was stirred for 2 hours, concentrated, and then purified by SCX resin (CUBCX1-HL (Benzenesulfonyl, H.L. Resin, 5 g) to provide 1 -((cis)-4-(3 -bromo-5 -fluorophenyl)-3 ,5-dimethylpiperazine, which used directly for next step. LCMS (M+H) = 287.1, 289.1 (1:1 ratio).

129779-30-2, As the paragraph descriping shows that 129779-30-2 is playing an increasingly important role.

Reference：
Patent; BRISTOL-MYERS SQUIBB COMPANY; BHIDE, Rajeev S.; BATT, Douglas G.; CHERNEY, Robert J.; CORNELIUS, Lyndon A.M.; LIU, Qingjie; MARCOUX, David; NEELS, James; POSS, Michael A.; QIN, Lan-ying; RUAN, Zheming; SHI, Qing; SRIVASTAVA, Anurag S.; TINO, Joseph A.; WATTERSON, Scott Hunter; (532 pag.)WO2016/64957; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

118753-66-5, tert-Butyl 4-aminopiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a well-stirred solution of intermediate 5a (2.0 g,5.29 mmol) in ethanol (10 mL) was added 1-amino-4-methylpiperazine 9a (0.61 g, 5.29 mmol) and a drop of acetic acid,and the mixturewas stirred at 78 C for 2 h. The mixturewas cooledto room temperature and the resulting solid was collected byfiltration and purified by column chromatography to give the targetcompounds 6a-1 as a yellow solid in 75% yield. M.p: 228-230 C;

118753-66-5, 118753-66-5 tert-Butyl 4-aminopiperazine-1-carboxylate 22029174, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Wu, Yachuang; Ding, Xiudong; Yang, Yifeng; Li, Yingxiu; Qi, Yinliang; Hu, Feng; Qin, Mingze; Liu, Yajing; Sun, Lu; Zhao, Yanfang; European Journal of Medicinal Chemistry; vol. 185; (2020);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

103-76-4, N-(2-Hydroxyethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1-(2-hydroxyethyl)piperazine (651 mg, 5.00 mmol, 1.0 equiv.) in anhydrous tetrahydrofuran (15 mL) was added, at 000 under argon and dropwise, carbon disulfide (452 pL, 7.50 mmol, 1.5 equiv.). After 15 mm of stirring at 0C, sodium hydride (60% dispersion in mineral oil) (200 mg, 5.00 mmol, 1.0 equiv.) was added portionwise. After 40 mm of stirring at0C, the reaction mixture was concentrated in vacuo. The resulting crude product was washed several times with cyclohexane to eliminate mineral oil and then concentrated in vacuo et dried with a vane pump during one night to afford compound A083 (1.10 g, 4,82 mmol) as a pale yellow powder in 96 % yield which was used in the next step without further purification. 1H NMR (400 MHz, MeOD) 5 4.46 (t, J = 4.8 Hz, 4H, CH2N), 3.71 (t, J = 5.9 Hz,2H, CH2O), 2.55 (t, J = 5.1 Hz, 6H, CH2N). 130 NMR (100 MHz, MeOD) 5 60.98 (CH2N),59.80 (CH2O), 54.35 (CH2N), 51.20 (CH2N).

103-76-4, The synthetic route of 103-76-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; UNIVERSITE PARIS EST CRETEIL VAL DE MARNE; CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS); INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MOTTERLINI, Roberto; FORESTI, Roberta; MARTENS, Thierry; RIVARD, Michael; WO2015/140337; (2015); 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

Piperazine-2-one (1.0 g, 10 mmol) was suspended in 10 mL DCM and Boc2O was slowly added. After the addition was completed, it was allowed to stand overnight at room temperature.After completion of the reaction, it was washed three times with 0.1 N diluted hydrochloric acid, 20 ml each time, and washed three times with 20 ml of saturated potassium carbonate each time.Finally, the dichloromethane was dried over anhydrous sodium sulfate.The solution was removed under vacuum to give a white solid.

5625-67-2, 5625-67-2 Piperazin-2-one 231360, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Shaoxing University; Hu Chunqi; Li Xin; Shi Yaru; Du Wenting; Tong Jie; Su Wanting; Xia Weiqi; (20 pag.)CN108610332; (2018); 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.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

General procedure: General Procedure 2c (1472) 1.0 equivalent of the respective intermediate, 1.0 equivalent of 1-hydroxy-1H-benzotriazole hydrate, 2.0 equivalents of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 3.0 equivalents of triethylamine and 1.2 equivalents of the amine were stirred in tetrahydrofuran at 25 C. for 18 h. Water was added to the reaction mixture. The solid was filtered off with suction, washed with water and diethyl ether and dried.

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

Reference：
Patent; Bayer Pharma Aktiengesellschaft; BOTHE, Ulrich; SIEBENEICHER, Holger; SCHMIDT, Nicole; ROTGERI, Andrea; BOeMER, Ulf; RING, Sven; IRLBACHER, Horst; GUeNTHER, Judith; STEUBER, Holger; LANGE, Martin; SCHAeFER, Martina; (191 pag.)US2016/311833; (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.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Dissolve 2, 3-DICHLOROPYRIDINE (8. 5 g, 0. 057 moles) and (R)- (-)-2-METHYLPIPERAZINE (5. 75 g, 0. 057 moles) in DMA (125. 0 mL) under nitrogen atmosphere. Add anhydrous powdered K2C03 (23. 75 g, 0. 172 moles) to this mixture and stir at 135-140°C for 48 hours. Cool the reaction mixture to room temperature, dilute with water (400 mL), extract with EtOAc (3 x 200 mL) and wash the combined organic extract with brine (2 x 150 mL). Dry over MgS04, concentrate under vacuum to afford crude product as orange yellow liquid. Distil the crude under high vacuum to afford pyridylpiperazine derivative as yellow viscous oil.

75336-86-6, The synthetic route of 75336-86-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NEUROGEN CORPORATION; WO2005/7648; (2005); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122833-04-9, 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-Methoxy-4-(4-methylpyridazin-1-yl)phenylamine (2.21 g, 1.0 eq) was added to compound l-1 (3.7 g, 1. Oeq) n-butanol (70 ml) In the solution, the reaction was carried out at 90 C for 2-3 hours. After the reaction was completed by TLC, the mixture was cooled to room temperature, filtered, washed and dried to give a red solid (4.6 g).

122833-04-9, As the paragraph descriping shows that 122833-04-9 is playing an increasingly important role.

Reference：
Patent; Chengdu University; Zhao Lifeng; Gou Xiaojun; (47 pag.)CN109384788; (2019); 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.103-76-4,N-(2-Hydroxyethyl)piperazine,as a common compound, the synthetic route is as follows.

To a ice-cooled solution of N-(2-hydroxyethyl)-piperazine (2.51 g, 19.3 mmol) in 10 ml DCM, a solution of Boc2O (4.21 g, 19.3 mmol), solved in 20 ml DCM was added dropwise. The resulting mixture was stirred for 1 h at room temperature. The solvent was removed under reduced pressure. 20 ml water was added to the remaining oil and the aqueous phase was extracted three times with diethyl ether (3 x 20 ml). The combined organic phases were dried (Na2SO4). The solvent was removed under reduced pressure and the product was obtained as colourless oil (4.28 g, 96 % yield). (Synthesis according to Radan, G.; Gebel, J.; Rauh, D. Archiv der Pharmazie 2003, 336, 372). 1H-NMR (300MHz, CDCl3): delta 3.64 – 3.60 (m, 2H), 3.45 – 3.41 (m, 4H), 2.69 (bs, 1H), 2.56 – 2.53 (m, 2H), 2.46 – 2.43 (m, 4H), 1.45 (s, 9H). CI-MS: m/z (%): 231 (100) [MH+].

103-76-4, As the paragraph descriping shows that 103-76-4 is playing an increasingly important role.

Reference：
Article; Wagner, Eva; Wittmann, Hans-Joachim; Elz, Sigurd; Strasser, Andrea; Bioorganic and Medicinal Chemistry Letters; vol. 21; 21; (2011); p. 6274 – 6280;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The solid from the previous step was dissolved in a mixture of N,N-diisopropylethylamine (0.7 mL, 4 mmol) and DMSO (0.7 mL, 10 mmol) and (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (590 mg, 2.7 mmol) was added and the reaction mixture heated at 120 C. overnight, concentrated by rotary evaporation, dissolved in a small amount of DCM and purified by silica gel chromatography (0-40% ethyl acetate:hexanes) to produce the title intermediate (613 mg, 57% yield) as a white solid. (m/z): [M+H]+ calcd for C24H27F4N4O4 591.12 found 591.4.

The synthetic route of 548762-66-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; THERAVANCE, INC.; US2012/114600; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics