Category: piperazines

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.509073-62-5,tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,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, fitted 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).

509073-62-5 tert-Butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate 2764459, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; DOBROVOLSKY, Dennis; HUANG, Hai-Tsang; (182 pag.)WO2018/98288; (2018); A1;,
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252990-05-9, Methyl (R)-1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Lithium aluminium hydride (1M in THF, 26 ml) was added to a solution of L-TERT- butyl 2-methyl (2R)-piperazine-1, 2-dicarboxylate (2. 55 g) in THF (70 ml) AT-40C, then the reaction was warmed to room temperature. The solution was stirred for 1 hour, then cooled to 0C and quenched by sequential addition of water (1 ml), sodium hydroxide (2N, 1 ml) and then water (2 ml). The resulting slurry was filtered and concentrated in vacuo to give TERT- butyl (2R)-2-(hydroxymethyl) piperazine-1-carboxylate (2.37 g, > 100%); NMR spectrum (DMSO-d6,373K) 1.40 (s, 9H), 2.58 (m, 1H), 2. 82 (M, 3H), 2. 92 (bs, 1H), 2.98 (d, 1H), 3.43 (m, 1H), 3.65 (M, 2H), 3.80 (M, 1H) ; Mass spectrum MH+ 217.

252990-05-9, The synthetic route of 252990-05-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/26152; (2005); 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.57260-71-6,tert-Butyl piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

57260-71-6, A mixture of compound tert-butyl piperazine-1 carboxylate (3.725 g, 20 mmol) and potassium carbonate (5.53 g, 40 mmol) in anhydrous dichloromethane (30 mL) was cooled to 0 C., cyclopropanecarbonyl chloride (2.30 g, 22 mmol) was then added dropwise. After the addition, the mixture was stirred at room temperature overnight. The mixture was diluted with dichloromethane (100 mL), washed with 10% citric acid (50 mL), followed by saturated sodium bicarbonate (50 mL), brine (100 mL), dried over anhydrous sodium sulfate, and concentrated to give tert-butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate (3.7 g, yield 73%) as a white solid. 1H-NMR (400 MHz, CDCl3) delta (ppm): 0.76-0.81 (m, 2H), 0.98-1.03 (m, 2H), 1.49 (s, 9H), 1.69-1.75 (m, 1H), 3.46-3.48 (m, 4H), 3.63-3.65 (m, 4H); LC-MS (ESI) m/z: 255(M+1)+.

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

Reference£º
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); A1;,
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21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of the compound obtained in step a (120 mg, 0.42 mmol) in DCE (2 mL), DIPEA (166 mg, 1 .28 mmol), c/’s-2,6-dimethylpiperazine (122 mg, 1 .06 mmol) and NaBH(OAc)3 (181 mg, 0.85 mmol) were added and the mixture was stirred at rt for 16 h. NaHCC>3 sat solution was added, extracted with DCM and the organic layer was concentrated under vacuum. Purification by flash chromatography, silica gel, gradient Hex to 100% acetone afforded the title product (126 mg, 78% yield). HPLC (Method B): Ret, 4.10 min; ESI+- MS m/z, 379.1 (M+H).

21655-48-1, The synthetic route of 21655-48-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ESTEVE PHARMACEUTICALS, S.A.; ALMANSA-ROSALES, Carmen; CUEVAS-CORDOBES, Felix; (77 pag.)WO2019/77106; (2019); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.115761-79-0,1-(2,4-Difluorophenyl)piperazine,as a common compound, the synthetic route is as follows.

The dimethyl acetal intermediate (40 mg, 0.13 mmol) from subpart (a) above was suspended in 2 mL of CH2Cl2 and 0.2 mL of 2: 1 solution of TFA/H2O was added. The resulting reaction mixture was stirred at room temperature for 4 hours. It was then neutralized with 0.25 mL of triethylamine. 1-(2,4-Difluoro-phenyl)-piperazine (40 mg, 1.5 eq. , prepared by reacting piperazine with 1-bromo-2,4-difluorobenzene according to the procedure described in WO 01/92264 A1), was added, followed by 140 mg of Na(OAc)3BH. The resulting reaction mixture was stirred at room temperature for 2 hours. It was then concentrated and then purified by preparative HPLC to afford N5-{2-[4-(2,4-difluoro-phenyl)-piperazin-1-yl]-ethyl}-2-furan-2-yl-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine. 1H NMR (DMSO-d6) delta 7.90 (br s, 2 H), 7.80 (d, J = 1.0 Hz, 1 H), 7.05 (d, J = 3.6 Hz, 1 H), 7.10-7.50 (m, 3 H), 6.68 (dd, J = 3.6 Hz, 1.0 Hz, 1 H) 3.20-2.75 (m, 12 H) ppm. MS: m/z: 442 [M + H] +., 115761-79-0

115761-79-0 1-(2,4-Difluorophenyl)piperazine 2734637, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOGEN IDEC MA INC.; WO2004/92170; (2004); A2;,
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208167-83-3, tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) Preparation of N-[1-butyl-4-[3-{2-(4-tert-butoxycarbonyl-1-piperazinyl)ethoxy}phenyl]-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N’-(2,6-diisopropylphenyl)urea STR99 The title compound was obtained in the same manner as in Example 41 from N-[4-(3-hydroxyphenyl)-1,2-dihydro-2-oxo-1,8-naphthyridin-3-yl]-N’-(2,6-diisopropylphenyl)urea and 1-tert-butoxycarbonyl-4-(2-chloroethyl)piperazine. 1 H-NMR delta (CD3 OD) 8.63 (1H, dd, J=4.6 Hz, 1.7 Hz), 7.75 (1H, dd, J=7.9 Hz, 1.7 Hz), 7.47 (1H, dd, J=8.2 Hz, 7.9 Hz), 7.04-7.30 (5H, m), 6.93-7.04 (2H, m), 4.60-4.73 (2H, m), 4.05-4.10 (2H, m), 3.38-3.53 (4H, m), 2.92-3.10 (2H, m), 2.55-2.68 (2H, m), 2.36-2.54 (4H, m), 1.95-2.10 (2H, m), 1.70-1.90 (2H, m), 1.45-1.62 (2H, m), 1.49 (9H, s), 1.15 (12H, d, J=6.6 Hz), 1.05 (3H, t, J=7.3 Hz)

208167-83-3, The synthetic route of 208167-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Pharmaceuticals Company, Ltd.; US5843957; (1998); A;,
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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.

To a solution of 2-CHLORO-5-METHANESULFONYL-BENZOIC acid (102mg, 0.43 mmol) in dimethylformamide (20 ml) were successively added TBTU (153mg, 0.48 mmol), N- ETHYLDIISOPROPYLAMINE (0.28 ML, 2.17 mmol) and 1- (4-TRIFLUROMETHYLPHENYL) piperazine (ABCR F07741NB, [30459-17-7], 100 mg, 0.43 mmol). The reaction was then stirred at room temperature for two hours, then concentrated in vacuo and purified by column chromatography (SI02, 50g, heptane/ethylacetate = 0 to 100%), to give the title compound as a colorless gum (170 mg, 0.38 mmol). MS (m/e): 464.3 (M+NH4+, 100%), 30459-17-7

30459-17-7 1-(4-Trifluoromethylphenyl)piperazine 121718, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2005/23260; (2005); A1;,
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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

To a suspension of carboxylic acid 17b (3.5 g, 11.4 mmol) in THF (15 mL)containing a drop of DMF was added 1?1?-carbonyldiimidazole (1.24 g, 13.7mmol) in a single portion. The mixture was left to stir at room temperature for 18hours. A stock solution of free-base guanidine was prepared as follows:Guanidine HCl (3.22 g, 34.2 mmol) was added to an aqueous NaOH solution (2M, 10 mL). The THF solution of the acyl imidazole was then added to the freebaseguanidine solution (10 mL) and stirred for 2 hours after which TLC indicatedcomplete consumption of the acyl imidazole and a more polar spot was observedon TLC. Spot stayed on the TLC baseline when using a solvent system of 10%MeOH in DCM but move to an RF ~of 0.4 when a few drop of 7 N NH3 in MeOHwas added to the TLC solvent. The mixture was concentrated in vacuo resulting in the formation of a pale yellowresidue which was dissolved in EtOAc (35 mL). The organic layer was washedwith water (3 x 25 mL), brine (1 x 30 mL), dried (Na2SO4), filtered, andconcentrated under vacuo to give a pale yellow syrup. The crude product wasfurther purified by flash column chromatography (silica gel, Silica Flash-Silicycle) using an eluent of dichloromethane, 5% MeOH in dichloromethane, and10% MeOH in dichloromethane to give an off-white syrup which was converted tothe hydrochloride salt using 1.25 M HCl in methanol. The methanolic solutionwas concentrated under vacuo to give 16 as a light yellow solid (540 mg, 11%)., 162046-66-4

As the paragraph descriping shows that 162046-66-4 is playing an increasingly important role.

Reference£º
Article; Jalily, Pouria H.; Eldstrom, Jodene; Miller, Scott C.; Kwan, Daniel C.; Tai, Sheldon S.-H.; Chou, Doug; Niikura, Masahiro; Tietjen, Ian; Fedida, David; Molecular Pharmacology; vol. 90; 2; (2016); p. 80 – 95;,
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5317-33-9, 3-(4-Methylpiperazin-1-yl)propan-1-ol is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-ethoxy-7-fluoro-3- quinolinecarbonitrile (200 mg, 0.49 mmol), 3- (4-methyl-piperazin-1-yl) propanol (155 mg, 0.98 mmol) (WO 20047212) and sodium hydride (196 mg, 4.6 mmol) in 5 mL of N, N-dimethylformamide was heated at 125C for 3 hours. The reaction mixture was poured into saturated sodium bicarbonate and stirred for 1 hour. The aqueous solution was extracted with 10% methanol in dichloromethane. The organic layer was washed with brine, dried over magnesium sulfate and concentrated in vacuo. The residue was purified by preparative thin layer chromatography, eluting with 15% methanol in dichloromethane. Trituation with hexane provided 116 mg of 4-[(2, 4- dichloro-5-methoxyphenyl) amino]-6-ethoxy-7- [3- (4-methylpiperazin-1- yl) propoxy] quinoline-3-carbonitrile as a light brown solid, mp 137-138C. MS 542.0 (M-H) – Analysis for C27H31CI2N503-0. 6 H20 Calcd : C, 58.40 ; H, 5.84 ; N, 12. 61. Found: C, 58.31 ; H, 5.71 ; N, 12.43., 5317-33-9

As the paragraph descriping shows that 5317-33-9 is playing an increasingly important role.

Reference£º
Patent; WYETH; WO2005/47259; (2005); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.

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 resin-supported triphenyl-phosphine (3 mmol/g of resin) diluted in 14.5 ml of anhydrous tetrahydrofuran, is added dropwise at 0C under argon 0.614 ml (3.07 mmol) of diisopropyldiazene-1,2-dicarboxylate. The reaction mixture is stirred at room temperature for 20h. The solid is filtered then rinsed in dichloromethane. The filtrate is concentrated and diluted in a sodium hydroxide solution (1M) and the product is extracted several times with ethyl acetate. The organic phases are combined, dried over magnesium sulfate, and concentrated. The residue is purified by chromatography on silica (cyclohexane/ethyl acetate eluent: 4:6 to 100% ethyl acetate) to yield 0.58 g of tert-butyl 4-(3-(4-formylphenoxy)propyl)piperazine-l-carboxylate in the form of a colourless oil.LCMS (ESI, m/z): (M+l) 348.91H-NMR: deltaEta pm 400 MHz, DMSO: 9.87 (1H, s, CHO), 7.86 (2H, d, CH^), 7.12 (2H, d, CHaro , 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, As the paragraph descriping shows that 132710-90-8 is playing an increasingly important role.

Reference£º
Patent; PIERRE FABRE MEDICAMENT; BEDJEGUELAL, Karim; RABOT, Remi; KALOUN, El Bachir; MAYER, Patrice; MARCHAND, Arnaud; RAHIER, Nicolas; SCHAMBEL, Philippe; BIENAYME, Hugues; WO2011/45344; (2011); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics