Month: March 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.373608-48-1,tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1-Benzyl-5-(methylcarbamoyl)-6-oxo- 1,6-dihyd ropyrid ine-3-carboxylic acid (205 mg, 0.716 mmol), HATU (412 mg, 1.084 mmol), DIPEA (0.38 mL, 2.176 mmol), tert-butyl 4-(3- aminopropyl)piperazine-1-carboxylate (344 mg, 1.414 mmol) and DMF (4 mL) were stirred at rt under N2 for 1 h. The solution was concentrated to give 1.18 g of a red oil which was purified bychromatography on 5i02 (Biotage SNAP 25 g cartridge, eluting with O-5O% (2O% (2M ammonia in MeOH) in DCM)/DCM). The appropriate fractions were concentrated to give tert-butyl 4-(3-(1- benzyl-5-(methylcarbamoyl)-6-oxo-1,6-d ihydropyridine-3-carboxamido)propyl)piperazine- 1-carboxylate (497 mg) as a pink solid.LCMS (2 mm Formic): Rt=0.66 mi [MH] = 512., 373608-48-1

373608-48-1 tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate 17750945, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; ATKINSON, Stephen John; DEMONT, Emmanuel Hubert; HARRISON, Lee Andrew; HAYHOW, Thomas George Christopher; HOUSE, David; LINDON, Matthew J; PRESTON, Alexander G; SEAL, Jonathan Thomas; WALL, Ian David; WATSON, Robert J; WOOLVEN, James Michael; (141 pag.)WO2017/50714; (2017); 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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

3-(2-Thienyl) propanoic acid (50 mg, 0.32 mmol), HOBt (47 mg, 0.35 mmol), TBTU (1 13 mg, 0.35 mmol), anhydrous triethylamine (71 ??, 0.51 mmol) and dry DMF (2 ml) were placed in an oven-dried Schlenk tube under a nitrogen atmosphere. The resulting solution was stirred at room temperature for 15 minutes. A second Schlenk tube was prepared containing 1-(4-trifluoromethyl phenyl) piperazine (81 mg, 0.35 mmol and dry DMF (1 ml) under a nitrogen atmosphere. The resulting solution was stirred until complete dissolution of the piperazine had occurred. The piperazine solution was then transferred, via a cannula, to the first Schlenk tube containing the carboxylic acid. The resulting solution was stirred for 24 hrs, under nitrogen, and monitored by TLC. After 24 hrs, the DMF was removed under reduced pressure and the resulting oil was acidified using a 0.1 M hydrochloric acid solution. The aqueous mixture was extracted with dichloromethane (20 ml, followed by 4 x 10 ml) and the organic layer washed with a saturated sodium bicarbonate solution (3 x 20 ml) and brine (3 x 20 ml). The organic layer was dried over magnesium sulphate and evaporated under reduced pressure. The residue was purified using flash chromatography (3:2, EtOAc:n-hexane) to obtain the desired product in an 44 % yield. H NMR (300 MHz, CDCI3) ? 7.48 , (d, 2H), 7.1 1 (dd, 1 H), 6.88-6.93 (m, 2H), 6.84-6.85 (m, 2H), 3.76 (t, 2H), 3.57 (t, 2H), 3.17-3.26 (m, 6H), 2.69 (t, 2H). MS (+ESI) calcd for C18 H19 F3 N2 O m/z: [M + H]+ , 368.1 164; found 369.1243 [Diff(ppm) = -1.25].

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

Reference£º
Patent; NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH; STEPHENS, John; FINDLAY, John; KINSELLA, Gemma; MARTIN, Darren; DEVINE, Robert; VELASCO-TORRIJOS, Trinidad; WO2013/60860; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

132710-90-8, 1-Boc-4-(3-hydroxypropyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Procedure A2a: 0.61 ml (3.07 mmol) of diisopropyl diazene-1,2-dicarboxylate is added drop by dr op at 0 C. under argon to 0.5 g (2.05 mmol) of tert-butyl 4-(3-hydroxypropyl)piperazine-1-carboxylate, 0.3 g (2.46 mmol) of 4-hydroxybenzaldehyde and 1 g (3.07 mmol) of supported triphenylphosphine (3 mmol/g of resin) diluted in 14.5 ml of anhydrous tetrahydrofuran. The reaction mixture is stirred at room temperature for 20 hours, and then the solid is filtered and rinsed with dichloromethane. The filtrate is concentrated and diluted in sodium hydroxide solution (1 M), the product is extracted several times with ethyl acetate, and then the organic phases are combined, dried on magnesium sulfate and concentrated. The residue is purified by silica gel chromatography (eluent: 4:6 cyclohexane/ethyl acetate to 100% ethyl acetate) to yield 0.58 g of tert-butyl 4-(3-(4-formylphenoxy)propyl)piperazine-1-carboxylate in the form of a colorless oil. LCMS (ESI, m/z): (M+1) 348.9 1H NMR: deltaH pm 400 MHz, DMSO: 9.87 (1H, s, CHO), 7.86 (2H, d, CHarom), 7.12 (2H, d, CHarom), 4.13 (2H, t, CH2), 3.28-3.31 (4H, m, 2CH2), 2.44 (2H, t, CH2), 2.31-2.34 (4H, m, 2CH2), 1.91 (2H, q, CH2), 1.40 (9H, s, 3CH3).

132710-90-8, The synthetic route of 132710-90-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PIERRE FABRE MEDICAMENT; Rabot, Remi; Bedjeguelal, Karim; Kaloun, El Bachir; Schmitt, Philippe; Rahier, Nicolas; Mayer, Patrice; Fournier, Emmanuel; US2014/31362; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

414910-15-9, tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

S2: 20L four-neck flask with mechanical stirring and thermometer, nitrogen protection,Add tert-butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate (2.40 kg, 9.44 mol),Sodium borohydride (0.71 kg, 18.88 mol), THF 5.06 Kg, cooled to 10 C,Boron trifluoride etherate (2.02 kg, 14.16 mol) was slowly added dropwise, and the temperature was controlled from 0 C to 10 C.After the dropwise addition is completed, the reaction is carried out at 10 C to 25 C for 4 h.The reaction solution was slowly poured into ice water of 5 kg of ice and 5 kg of water, and extracted with methyl tert-butyl ether (4 kg * 2).The methyl tert-butyl ether phase was combined and washed once with 5 kg of saturated sodium chloride solution.Concentration and removal of methyl tert-butyl ether gave a pale-yellow solid, N-Boc-4-(cyclopropylmethyl)piperazine, 2.13 kg, yield 94%.The nuclear magnetic warp alignment is consistent with the standard map.

414910-15-9, 414910-15-9 tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate 968936, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Suzhou Laikeshide Pharmaceutical Co., Ltd.; Liu Tongchang; Yu Jurong; (6 pag.)CN108341792; (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.120737-59-9,tert-Butyl 3-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

[Referential Example 21] 3,4-Dimethylpiperazine-1-carboxylic acid tert-butyl ester 10percent Palladium-carbon (0.59 g), 35percent aqueous formalin (9.7 mL), and 1M HCl-ethanol (31.3 mL) were added to a solution of 3-methylpiperazine-1-carboxylic acid tert-butyl ester (5.70 g) obtained in Referential Example 20 in methanol (100 mL) at room temperature, and the mixture was stirred for 15 hours in a hydrogen atmosphere. The reaction mixture was purged with nitrogen, and insoluble matter was removed through filtration. The solvent of the filtrate was removed under reduced pressure, and chloroform-methanol (9percent) was added to the residue. The mixture was alkalified with aqueous sodium hydroxide and then partitioned. The aqueous layer was extracted with chloroform – methanol (9percent), and the organic layers were combined, washed with saturated brine, and dried over sodium sulfate anhydrate. After a filtration step, the solvent was removed under reduced pressure, and the residue was purified through silica gel column chromatography (chloroform – methanol), to thereby give the title compound as an oil (3.10 g, 51percent). 1H-NMR (400MHz, CDCl3) delta: 1.04 (3H, d, J=6. 3Hz), 1.46(9H,s), 1.95-2.20(2H,m), 2.28(3H,s), 2.50-2.78(2H,br), 2. 90-3.05 (1H,br), 3.88 (1H, br). MS (ESI)m/z:215 (M+H)+.

120737-59-9, The synthetic route of 120737-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1621537; (2006); 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 A: (S)-tert-butyl 4-((S)-2-hydroxy-2-( 4-methyl-1-oxo-1 ,3-dihydroisobenzofuran-5-yl)ethyl)-3-(hydroxymethyl)piperazine-1-carboxylate: (S)-4-Methyl-5-( oxiran-2-yl)isobenzofuran-1 (3H)one(0.75g, 3.95 mmol) and (S)-tert-butyl3-(hydroxymethyl)piperazine-1-carboxylate (1.02 g,4.73 mmol) in ethanol (12 mL) were heated in microwave at 150 oc for 1.5 h. The reaction solution was concentrated and the residue was purified by MPLC on a Biotage system using 40-100% ethyl acetate/hexane to give the title compound. LC/MS: (M+1)+: 407.15., 314741-40-7

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

Reference£º
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

515162-19-3, 3-(4-Methylpiperazin-1-ylmethyl)benzylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 3-cyanobenzaldeliyde (3.25 mmol) was added iV-metliyl piperizine (3.25 mmol) followed by NaB(OAc)3H (4.25 (mmol). The mixture was stirred for 4 h and concentrated. The residual material was partitioned between CH2Cl2 and NaHCC>3 (sat.) and the organic phase was then collected. The organic phase was concentrated (0.70 g, 3.25 mmol) and dissolved in THF (5 mL). The solution was cooled in an ice bath, and to this was added lithium aluminum hydride (1.0 M in THF, 4.8 mL, 4.88 mmol). The solution was warmed to room temperature and stirred for 2 h. The reaction was quenched with excess sodium sulfate decahydrate (~1 g), and then filtered through diatomaceous earth. The material was concentrated to give a clear oil of the benzylamine which was used without further purification. 4-Phenoxy benzoic acid was dissolved in CH2Cl2 (2 mL) and to titiis was added EDCI (0.107 g, 0.56 mmol) followed by DIEA (0.048 mL, 0.56 mmol) and the benzyl amine obtained from the previous step (0.10 g, 0.50 mmol). The reaction was stirred for 2 h, and then partitioned between CH2Cl2 and NaHCO3 (sat.). The organic layer was concentrated and the residual oil chromatographed (SiO2, CH2Cl2/5% NH3 in MeOH, 95:5) to give the title compound as a white solid.1HNMR (CDCl3, 300 MHz) delta 2.30 (s, 3H), 2.49 (br s, 8H), 3.51 (s, 2H), 4.63 (d, 2H, J = 5.4 Hz), 6.27 (s, IH), 6.96-7.05 (m, 4H), 7.16 (t, IH, J = 7.5 Hz), 7.25 (m, IH), 7.30-7.39 (m, 5H), 7.75-7.78 (d, 2H, J = 7.8 Hz)., 515162-19-3

The synthetic route of 515162-19-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2006/130075; (2006); 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.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.

300 mg mixture of 2,6-dichloro-4- [4-chloro-6-(4-fluorophenyl)thieno [2,3 -d]pyrimidin-5 -yl] -3,5 -dimethyl-pheno 1 and 4- [4-bromo-6-(4-fluorophenyl)thieno [2,3 -d]pyrimidin-5 -yl] -2,6-dichloro-3 ,5 -dimethyl-pheno 1 (0.62 mmo 1), 286 mg 2-(4-methylpiperazin- 1 -yl)ethano 1(1.98 mmol) and 520 mg triphenyl phosphine (1.98 mmol) were dissolved in 10 mL drytoluene, then 460 mg ditertbutyl azodicarboxylate (1.98 mmol) was added. The mixturewas stirred at 50 ¡ãC under nitrogen until no further conversion was observed. The volatiles were evaporated under reduced pressure and the crude intermediate was purified via flash chromatography using EtOAc and methanol as eluents to obtain 4-chloro-5-[3,5-dichloro- 2,6-dimethyl-4- [2-(4-methylpiperazin- 1 -yl)ethoxy]phenyl] -6-(4-fluorophenyl)thieno [2,3 -d]pyrimidine and 4-bromo-5 -[3 ,5-dichloro-2,6-dimethyl-4- [2-(4-methylpiperazin- 1-yl)ethoxy]phenyl]-6-(4-fluorophenyl)thieno[2,3-d]pyrimidine as a 35:65 mixture of products.

5464-12-0, The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; SZLAVIK, Zoltan; SZABO, Zoltan; CSEKEI, Marton; PACZAL, Attila; KOTSCHY, Andras; BRUNO, Alain; GENESTE, Olivier; CHEN, I-Jen; DAVIDSON, James Edward Paul; MURRAY, James Brooke; ONDI, Levente; RADICS, Gabor; SIPOS, Szabolcs; PROSZENYAK, Agnes; PERRON-SIERRA, Francoise; BALINT, Balazs; (188 pag.)WO2016/207226; (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.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

3-4-3: Preparation of 2-[3-fluoro-4-(BOC-piperazino)]phenylamino-6-chloro-3-nitropyridine; To 100 ml of methanol were added 2.75 g (14.2 mmol) of 2,6-dichloronitropyridine and 2.38 ml (17.0 mmol) of triethylamine and 4.2 g (14.2 mmol) of [3-fluoro-4-(BOC-piperazino)]aniline obtained in Preparation Example 3-4-2 was then added thereto, followed by reaction at room temperature (20 to 30) for about 24 hours. After the reaction was complete, the reactant was filtered, washed with 20 ml of methanol and then dried under vacuum at about 40 to afford 4.47 g (yield: 70%) of the desired compound. Mass (M+): 452.0 1H-NMR (DMSO-d6): 1.42(s, 9H), 2.96(t, 4H), 3.48(m, 4H), 7.01(d, 1H), 7.07(t, 1H), 7.34(d, 1H), 7.53(d, 1H), 8.53(d, 1H), 10.08(s, 1H).

154590-35-9, The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ryu, Jei Man; Lee, Jin Soo; Park, Whui Jung; Hwang, Yun Ha; Kim, Ki Yoon; US2011/306606; (2011); 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.674792-05-3,(S)-1-Boc-2-Isopropylpiperazine,as a common compound, the synthetic route is as follows.

674792-05-3, [00356] A mixture of (5)-tert-butyl 2-isopropylpiperazine-1-carboxylate (1 g, 4.4 mmol), NaHCO3 (1.1 g, 13.2 mmol), CbzCl (1.1 g, 6.6 mmol) in water (2 mL) and THF (6 mL) was stirred at rt overnight. The mixture was added with water (20 mL) and extracted with EtOAc (3 X 20 mL). The combined organic layers were dried over anhydrous Na2504, filtered, concentrated under reduced pressure. The residue was purified by chromatography column on silica gel with eluting with petroleum ether / EtOAc 50/1 to afford crude (S)-4-benzyl 1- tert-butyl 2-isopropylpiperazine-1,4-dicarboxylate (1.8 g, 90%) as a colorless oil, which was used for the next step directly without further purification. LC-MS tR = 1.276 mm in 2 mm chromatography, m/z 263.2 [M+H-Boc] +

The synthetic route of 674792-05-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; VITAE PHARMACEUTICALS, INC.; CLAREMON, David, A.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen, D.; SINGH, Suresh, B.; TICE, Colin, M.; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; (185 pag.)WO2016/22521; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics