Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.109384-27-2,1-Methylpiperazin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

A mixture of 150 mg (0.29 mmol) of 2-(morpholin-4-yl)-8-[1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl]-1,7-naphthyridin-4-yl trifluoromethanesulfonate, 150 mg (0.99 mmol) 1-methylpiperazin-2-one hydrochloride and 0.28 ml (1.99 mmol) of triethylamine in 0.43 ml of MeCN was stirred at 70C overnight under argon. After cooling the reaction mixture was diluted with ethyl acetate and washed with saturated aqueous sodium chloride solution. The organic phase was filtered using a Whatman filter and then concentrated to give the crude product thatwas used without further purification in the next step., 109384-27-2

The synthetic route of 109384-27-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; WORTMANN, Lars; LUeCKING, Ulrich; LEFRANC, Julien; BRIEM, Hans; KOPPITZ, Marcus; EIS, Knut; VON NUSSBAUM, Franz; BADER, Benjamin; WENGNER, Antje Margret; SIEMEISTER, Gerhard; BONE, Wilhelm; LIENAU, Philip; GRUDZINSKA-GOEBEL, Joanna; MOOSMAYER, Dieter; EBERSPAeCHER, Uwe; SCHICK, Hans; (509 pag.)WO2016/20320; (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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.

Step 1: tert-butyl 4-(5-bromopyridin-2-yl)-3-oxopiperazine-1-carboxylate A mixture of 2,5-dibromopyridine (1.00 g; 4.22 mmol), tert-butyl 3-oxopiperazine-1-carboxylate (562 mg; 2.80 mmol) and Cs2CO3 (1.37 g; 4.20 mmol) in toluene (20 mL) was purged with nitrogen and added Pd2(dba)3 (129 mg; 0.14 mmol) and XantPhos (97 mg; 0.17 mmol). The reaction mixture was stirred at 100 C. overnight, cooled to room temperature, diluted with EtOAc (50 mL), filtered through Celite, washed with water (50 mL), brine (50 mL), dried over anhydrous Na2SO4, filtered, concentrated, and purified by a silica gel chromatography (petroleum ether/EtOAc=10/1, v/v) to afford 955 mg (96%) of the title compound as a yellow oil. LC-MS: m/z 355.8 [M+H]+., 76003-29-7

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ITEOS THERAPEUTICS; Crosignani, Stefano; Cauwenberghs, Sandra; Driessens, Gregory; Deroose, Frederik; US2015/225367; (2015); 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.

Step E: tert-butyl (3S)-4-(2-(3-cyano-2,4-difluorophenyl)-2-hydroxyethyll-3-(hydroxymethyl)piperazine-1-carboxylate; 2,6-Difluoro-3-( oxiran-2-yl)benzonitrile (1.50 g, 8.28mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (2.40 g, 11.1 mmol) were suspended inethanol (15 mL) then heated in a microwave apparatus for 30 min at 150 C. The reactionmixture was cooled and evaporated dryness. The residue was purified by chromatographythrough a 120g Redi-sep column eluting with 5%MeOH/95% EtOAc to yield the title compoundLC-MS: M+ 1 = 398.·

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

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (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.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

To a solution of 6b (1eq.) in isopropanol the amine 11 (2.5 eq.) and N,N-diisopropylethylamine(4 eq.) were added. The reaction mixture was irradiated with microwaves for 10min at 160 C. The reaction mixture was evaporated under reduced pressure. Theyellow residue was diluted with EtOAc and washed with water. The organic phasewas washed with ammonium chloride, dried over Na2SO4 andfinally evaporated under reduced pressure. The crude mixture was purified byflash chromatography on silica gel (CH2Cl2:MeOH 98:2) togive the desired compound 9b as awhite solid (67%). 1H NMR (400 MHz, CDCl3): delta(ppm)3.31(t, J=8, 4H); 4.07 (t, J=8, 4H), 4.55(s, 2H); 4.91-4.85 (2m, 2H); 5.47 (t,J=8, 1H); 6.88 (d, J=8, 2H); 7.19-7-33 (m, 6H), 7.89 (s,1H); 8.30 (s,1H). 13CNMR (CDCl3): delta(ppm) 44.98; 48.83; 53.59; 59.22; 64.99; 116.20;128.53; 128.82; 132.82; 134.80; 136.51; 150.24; 155.27. MS: m/z 483 [M+H]+.Anal. Calcd. For C24H25Cl2N7: C,59.75; H, 5.22; N, 20.32; found: C, 59.55; H, 5.12; N, 20.21, 216144-45-5

The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Radi, Marco; Bernardo, Vincenzo; Vignaroli, Giulia; Brai, Annalaura; Biava, Mariangela; Schenone, Silvia; Botta, Maurizio; Tetrahedron Letters; vol. 54; 38; (2013); p. 5204 – 5206;,
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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

548762-66-9, 4- [2- (benzyloxy) -1,1,1,3,3,3-hexafluoropropane-2-yl] -1-bromo-2-propylbenzene (150 mg, 0.330 mmol) , And dissolved in toluene (1.1 mL) under an argon atmosphere. To the reaction solution was added 2,5-dimethylpiperazine-1-carboxylic acid (2S, 5R) -tert-butyl (47 mg, 0.220 mmol), Pd 2 (dba) 3 (8.0 mg, 8.79 mumol), (±) -BINAP (11 mg, 0.0176 mmol) and potassium tert-butoxide (89 mg, 0.923 mmol) were sequentially added thereto, followed by stirring at 60 C. for 13 hours. After the completion of the reaction was confirmed, the reaction solution was concentrated under reduced pressure, and the obtained residue was purified using silica gel column chromatography (hexane / ethyl acetate) to obtain the title compound 48.7 mg (yield 38%) as a pale yellow oil It was obtained as a thing.

548762-66-9 (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate 11745988, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; KOWA COMPANY LIMITED; KOURA, MINORU; SUMIDA, HISASHI; SHIBUYA, KIMIYUKI; (34 pag.)JP2015/48326; (2015); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5294-61-1, N-(2,6-Dimethylphenyl)-2-(piperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5294-61-1, To a solution of crude N- (4-METHOXYPHENYL)-2-OXIRAN-2-YLACETAMIDE (10) in ethanol (2. 5ML) was added triethylamine (0. 5ML), followed by N- (2, 6-dimethylphenyl) -2- piperazinylacetamide, a compound of fonnula (4) (150mg), and the mixture was heated to reflux for 18 hours. Solvent was removed from the reaction mixture under reduced pressure, and the residue purified by column chromatography on silica gel, eluting with 5% MeOH/dichloromethane, to give 4- (4-1 [N- (2, 6-dimethylphenyl) carbamoyl] methyl}- PIPERAZINYL)-3-HYDROXY-N- (4-METHOXYPHENYL) butanamide, a compound of Formula I as an off- white solid.

The synthetic route of 5294-61-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CV THERAPEUTICS, INC.; WO2004/63180; (2004); 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.106261-48-7,4-((4-Methylpiperazin-1-yl)methyl)benzoic acid,as a common compound, the synthetic route is as follows.

Comparative Example 21 : LambdaT-(5-bromo-2-cyano-4-pyrimidinyl)-Lambdar-(2,2-dimethylpropyl)- 4-[(4-methyl-1-piperazinyl)methyl]benzohydrazide trifluoroacetate.Intermediate 21 (1 g, 4.3 mmol) was dissolved in thionyl chloride (5 ml). The reaction mixture was stirred at room temperature for 17 hours. The solvent was evaporated in vacuo and the acid chloride was used without any further purification.To a stirred solution of Intermediate 19 (200 mg, 0.70 mmol) in pyridine (1 mL) and DIPEA (5 mL), potassium carbonate (193 mg, 1.40 mmol) and previously obtained acid chloride(443 mg, 1.75 mmol) were added and the resulting reaction mixture was stirred at room temperature for 17 hours. The solvent was evaporated in vacuo and the crude reaction mixture was purified by flash chromatography (silica gel, dichloromethane:methanol). The solid was repurified by HPLC (H2O:ACN) to give the title compound. 1H NMR (300 MHz, DMSO) delta ppm: 11.33 (s, 1H), 8.64 (s, 1 H), 7.91 (d, 2H), 7.49 (d, 2H), 3.72 (s, 2H), 3.37(m, 2H), 3.25-2.81 (br, 6H), 2.78 (s, 3H) 0.99 (s, 9H). [ES+ MS] m/z 500 (MH+)., 106261-48-7

The synthetic route of 106261-48-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXO GROUP LIMITED; WO2007/25774; (2007); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

171504-98-6, Methyl 1,4-Bis(Boc)-2-piperazinecarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1,4-di-tert-butyl 2-methyl piperazine-1,2,4-tricarboxylate (5.09 g, 14.7 mmol) in dry THF (49 mL) was added methylmagnesium bromide (3.0 M in THF and tol, 31.7 mL, 44.3 mmol) at 0 C. The reaction mixture was stirred at room temperature for 18 hours. After quenched with saturated aq. NH4Cl, the mixture was diluted with water and extracted with EtOAc twice. The combined organic layers were washed with brine, dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by column chromatography on SiO2 (Hex:EtOAc=5:1 to 3:1 to 2:1) to afford di-tert-butyl 2-(2-hydroxypropan-2-yl)piperazine-1,4-dicarboxylate (2.47 g, 48%) as a colorless viscous oil. 1H-NMR (CDCl3, Varian, 400 MHz): delta 1.21 (3H, s), 1.31 (3H, s), 1.46 (18H, s), 3.01-3.38 (4H, m), 3.79-4.21 (4H, m)., 171504-98-6

As the paragraph descriping shows that 171504-98-6 is playing an increasingly important role.

Reference：
Patent; HANDOK INC.; CMG Pharmaceutical Co., Ltd.; Kim, Moonsoo; Lee, Chaewoon; Lee, Gilnam; Yoon, Cheolhwan; Seo, Jeongbeob; Kim, Jay Hak; Lee, Minwoo; Jeong, Hankyul; Choi, Hyang; Jung, Myung Eun; Lee, Ki Nam; Kim, Hyun Jung; Kim, Hye Kyoung; Lee, Jae Il; Lee, MinWoo; Kim, Misoon; Choi, Soongyu; (124 pag.)US2016/168156; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5271-27-2, 1-Methyl-3-phenylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5271-27-2, General procedure: A mixture of 1a-c (1.93 g, 10 mmol), 4 (1.76 g, 10mmol) and KF (18 mmol) were heated at 120-130 °C inDMF (30 mL) for 16 – 18 h. At the end of this period, thereaction mixture was cooled to room temperature and dilutedwith water (30 mL). The separated solid was filtered, washedand dried to obtain crude 5a-i. The obtained crude productwas then purified by recrystallization using ethanol

As the paragraph descriping shows that 5271-27-2 is playing an increasingly important role.

Reference：
Article; Darsi, S.S. Praveen Kumar; Kumar, K. Shiva; Devi, B. Rama; Naidu; Dubey; Letters in Organic Chemistry; vol. 11; 8; (2014); p. 551 – 555;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

6531-38-0, 2,2′-(Piperazine-1,4-diyl)diethanamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6531-38-0, General procedure: General synthetic procedure for m1-m5, 4-15, and 27-35 A mixture of 2-methylsulfanyl-1,3-thiazolin-4-one 3a-3l (1 mmol) and the appropriate diamine (0.5 mmol) or amine (1 mmol) in ethanol was refluxed for 8 h. After cooling, the precipitate was filtered, washed with ethanol and dried. (5Z,5’Z)-2,2′-[Piperazine-1,4-diylbis(ethane-2,1-diylimino)]bis(5-(4-hydroxybenzylidene)-1,3-thiazol-4(5H)-one) (14) Yellow solid (0.33 g, 58%), mp >250C; IR (cm-1) 3190, 3008, 2826, 1715, 1680, 1600, 1581, 1504, 1450, 1346, 1271, 1248, 1204, 1176, 1137, 1008; 1H RMN (250 MHz, DMSO-d6) d: 2.48-2.53 (m, 12H, 6xCH2), 3.65-3.68 (m, 4H, 2xCH2), 6.92 (d, J =8.5, 4H, Ar-H), 7.43 (d, 4H, Ar-H), 7.52 (s, 2H, 2xC=CH), 9.82 (s, 4H, OH/NH); 13C RMN (500 MHz, DMSO-d6) d: 41.7 (x2), 52.5 (x4), 56.1 (x2), 116.1 (x4), 124.6 (x2), 124.8 (x2), 129.4 (x2), 131.4 (x4), 158.9 (x2), 173.3 (x2), 179.9 (x2). ESI-MS (m/z) calcd for C28H30N6O4S2 : 578.1, found 577.2 [M-H]-.

6531-38-0 2,2′-(Piperazine-1,4-diyl)diethanamine 81020, apiperazines compound, is more and more widely used in various fields.

Reference：
Article; Sarkis, Manal; Tran, Diem Ngan; Kolb, Stephanie; Miteva, Maria A.; Villoutreix, Bruno O.; Garbay, Christiane; Braud, Emmanuelle; Bioorganic and Medicinal Chemistry Letters; vol. 22; 24; (2012); p. 7345 – 7350;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics