Month: November 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5271-27-2,1-Methyl-3-phenylpiperazine,as a common compound, the synthetic route is as follows.,5271-27-2

1 -Methyl-3-phenylpiperazine (17.6 g; 0.1 mol) was dissolved in 100 dichloromethane. Triethylamine (5 ml; 0.05 mol) was added. A solution of butyroyl chloride (11.6 g; 0.1 1 mol) in dichloromethane was slowly added under cooling. After the total addition a white suspension was formed. The mixture was quenched with 10percent sodium carbonate. The organic layer was washed again with carbonate, dried and evaporated to an oil (24g). Kugelrohr distillation of 22.5 g at >200 ¡ãC/0.05 mbar yielded 22.0 g oil (95 percent). Chiral GC: 12.87/12.98 min, severe overlap.

The synthetic route of 5271-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; N.V. ORGANON; WO2007/144409; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

113028-17-4, Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 8: Preparation of Ulifloxacin;Tertiary butanol (5.55It), 6-fluoro-l-methyl-4-oxo-7-(l-piperazinyl)-4H-[l,3]thiazeto [3,2- a]quinoline-3-carboxylic acid ethyl ester (1.1 lkg), potassium hydroxide (0.37kg) and water (2.75 It) were added at room temperature. The reaction mixture was heated to 600C and maintained for 1.5 hours. Reaction completion was checked by TLC. This was followed by the addition of water (22.2 It) and acetic acid (0.39 It). The reaction mixture was filtered, washed with water followed by slurry wash with acetone (2.22 It) twice and dried to obtain 0.95 kg of ulifloxacin having purity 97.56% by HPLC., 113028-17-4

The synthetic route of 113028-17-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IND-SWIFT LABORATORIES LIMITED; WO2009/93268; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

694499-26-8,694499-26-8, 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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%).

As the paragraph descriping shows that 694499-26-8 is playing an increasingly important role.

Reference£º
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.20327-23-5,1-Cyclopropylpiperazine,as a common compound, the synthetic route is as follows.

Ethyl 4-fluorobenzoate (0.153 mL, 1.04 mmol) and 1-cyclopropylpiperazine (0.2637 g, 2.09 mmol) were taken up in DMA (2 mL) and sealed into a microwave tube. The reaction was heated to 150 C. for 90 mins in the microwave reactor and cooled to room temperature. The reaction mixture was evaporated to afford a brown gum, which solidified on standing. The crude product was purified by silica column chromatography, eluting with 10% MeOH(containing 0.1% aqueous ammonia) in DCM. Pure fractions were evaporated to dryness to afford the impure product as a yellow solid. The impure product was purified again by silica column chromatography, eluting with a gradient of 0-2.5% MeOH in DCM. Pure fractions were evaporated to dryness to afford ethyl 4-(4-cyclopropylpiperazin-1-yl)benzoate (0.096 g, 33.6%) as a beige solid. 1H NMR (399.9 MHz, CDCl3) delta 0.45-0.52 (5H, m), 1.36 (3H, t), 2.75 (4H, t), 3.29 (4H, t), 4.32 (2H, q), 6.84-6.88 (2H, m), 7.90-7.93 (2H, m) m/z (ES+) (M+H)+=275, 20327-23-5

20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; US2008/153812; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

120737-78-2, tert-Butyl 2-methylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a stirring mixture of crude acyl chloride 7 (prepared from acid 17 6 (500mg, 1.5mmol)) in anhydrous 93 chloroform (30ml) a solution of 100 (R)-1-Boc-3-aminopyrrolidine (600mg, 3.4mmol) and 101 pyridine (0.6ml, 7.0mmol) in anhydrous chloroform (10ml) was added. The mixture was refluxed for 5min, diluted with chloroform (20ml), washed with aqueous solution of 102 HCl (0.3M), dried and evaporated. The residue was purified by column chromatography on a silica gel in 103 chloroform-methanol (10:0?10:1). The red solid obtained after evaporation was dissolved in hot chloroform (30ml). 104 Methanesulfonic acid (0.3ml, 4.6mmol) was added, the mixture was stirred overnight and evaporated. The residue was dissolved in boiling 105 water (5ml), filtered, the product was precipitated with acetone-ether mixture (3:1). The red solid was collected by filtration, washed with acetone, Et2O, n-hexane and dried.

120737-78-2, As the paragraph descriping shows that 120737-78-2 is playing an increasingly important role.

Reference£º
Article; Shchekotikhin, Andrey E.; Dezhenkova, Lyubov G.; Luzikov, Yuri N.; Treshalin, Michael I.; Shtil, Alexander A.; Preobrazhenskaya, Maria N.; Tsvetkov, Vladimir B.; Volodina, Yulia L.; Tatarskiy, Victor V.; Kalinina, Anastasia A.; Treshalina, Helen M.; Romanenko, Vladimir I.; Kaluzhny, Dmitry N.; Kubbutat, Michael; Schols, Dominique; Pommier, Yves; European Journal of Medicinal Chemistry; vol. 112; (2016); p. 114 – 129;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of tert-butyl 3,3- dimethylpiperazine-l-carboxylate (150 mg, 0.70 mmol) in dichloromethane (5 mL) was added 3- (2,6-dichlorophenyl)-5-(propan-2-yl)-l,2-oxazole-4-carbaldehyde (180 mg, 0.63 mmol) and sodium acetate (87 mg, 1.06 mmol). The mixture was stirred for 1 h at room temperature. Then STAB (404 mg, 1.91 mmol) was added. The resulting solution was stirred overnight at room temperature. The reaction was then quenched by adding water (15 mL). The resulting mixture was extracted with 5×5 mL of dichloromethane and the organic layers were combined. The organic phase was washed successively with water and brine. The residue was concentrated under vacuum after dried over anhydrous sodium sulfate. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (1 : 10). This resulted in 0.116 g (38%) of the title compound as a white solid. LC-MS (ESI, m/z): [M+H]+ = 482.4.

259808-67-8, The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; HEPAGENE THERAPEUTICS, INC.; XU, Xiaodong; (104 pag.)WO2018/85148; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

54699-92-2, 4-Methyl-1-piperazineacetic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

54699-92-2, A solution of 2-(4-methyl-1-piperazinyl)acetic acid (described in J. Med. Chem., 43, 1493 (2000); 2.5 g, 16 mmol) in water (30 ml) was cooled to 0C, and cesium carbonate (2.6 g, 7.9 mmol) was added thereto with stirring, then the mixture was stirred at room temperature for 1 hour. The mixture was concentrated under reduced pressure to give the title compound (4.49 g, 98% yield) as a pale yellow solid.

As the paragraph descriping shows that 54699-92-2 is playing an increasingly important role.

Reference£º
Patent; Sankyo Company, Limited; EP1362856; (2003); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6,630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-chloro-3-nitrobenzoic acid (1.0 g, 4.97 mmol) in dichioromethane(10 mL) were added oxalyl chloride (500 jiL, 5.30 mmol) followed by catalytic amount ofDMF and the mixture was stirred at RT for 2 h. The mixture was concentrated under reducedpressure and the residue was dissolved in dichloromethane. The solution was cooled to 0 C;4-((4-ethylpiperazin- 1 -yl)methyl)-3 -(trifluoromethyl)aniline (Intermediate Cl) (1.0 g, 3.30mmol) was added to the reaction mixture followed by DIPEA (1.5 mL, 8.30 mmol). The resultant mixture was stirred overnight at RT. The mixture was diluted with water and extracted twice with ethyl acetate. The combined organic extracts were washed with saturated sodium bicarbonate solution, water and brine. The solution was dried over anhydrous sodiumsulfate, filtered and concentrated. The residue thus obtained was purified by columnchromatography to yield 1.43 g of the desired product. ?H NMR (400 MHz, DMSO-d6) oe0.98 (t, J 7.2 Hz, 3H), 2.28-2.39 (m, 1OH), 3.57 (s, 2H), 7.74 (d, J 8.4 Hz, 1H), 7.98-8.04(m, 2H), 8.16 (s, 1H), 8.27 (dd, J, = 2.4 Hz, J2 = 8.4 Hz, 1H), 8.65 (s, 1H), 10.77 (s, 1H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); 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.170911-92-9,tert-Butyl 4-(4-aminophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of 97 3-(2-chlorophenyl)-7-methylsulfanyl-2H-pyrimido[5,4-e][1,3]oxazin-4-one (130 mg, 0.423 mmol, 1.0 eq) in 5 mL of 24 toluene was added 25 m-CPBA (224 mg, 0.84 mmol, 2.0 eq) and stirred at rt for 30 min. 66 Tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate (117 mg, 0.423 mmol, 1.0 eq) and 27 DIPEA (163 mg, 1.27 mmol, 3.0 eq) were added and allowed to stir at rt for 12 h. Reaction was monitored by LCMS. After completion of reaction, solvent was removed under reduced pressure. Residue was diluted with saturated NaHCO3 solution and extracted with CH2Cl2 (100 mL¡Á2). Combined organic layer was washed with brine solution (50 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure to give crude product which was purified by flash chromatography to afford 100 tert-butyl 4-[4-[[3-(2-chlorophenyl)-4-oxo-2H-pyrimido[5,4-e][1,3]oxazin-7-yl]amino]phenyl]piperazine-1-carboxylate (120 mg, 52.8%). LCMS: 296 [M+1]+, 170911-92-9

The synthetic route of 170911-92-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; giraFpharma LLC; Chakravarty, Sarvajit; PHAM, Son Minh; Kankanala, Jayakanth; AGARWAL, Anil Kumar; PUJALA, Brahmam; SONI, Sanjeev; ARYA, Satish K.; PALVE, Deepak; KUMAR, Varun; (360 pag.)US2019/106436; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-08-2, 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 29 Preparation of 6-(2-carbamoyl-4-methylpiperazin-l-yl)-2-(4-(4- (trifluoromethyl) phenoxy)phenyl)pyrimidine-4-carboxamide (Cpd No. 81) Scheme 61 1 -tert-butyl 3-methyl 4-(2-chloro-6-(methoxycarbonyl)pyrimidin-4-yl)piperazine- 1 ,3-dicarboxylate: A mixture of 1-tert-butyl 3-methyl piperazine-l ,3-dicarboxylate (5.133 g, 21.01 mmol), methyl 2,6-dichloropyrimidine-4-carboxylate (4.354 g, 21.03 mmol), and iPr2NEt (4.0 mL, 23.0 mmol) in acetonitrile (50 mL) was heated at 50C for 4 h. After cooling, the reaction mixture was evaporated in vacuo and the residue chromatographed over silica gel with 20-70% EtOAc in hexanes. The product fractions were evaporated in vacuo to give 1-tert-butyl 3-methyl 4-(2-chloro-6- (methoxycarbonyl)pyrimidin-4-yl)piperazine-l,3-dicarboxylate as a very pale yellow powder (6.626 g, 15.97 mmol, 76% yield). LC/MS: m/z= 415.2 [M+H]+., 129799-08-2

The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PURDUE PHARMA L.P.; NI, Chiyou; PARK, Minnie; SHAO, Bin; TAFESSE, Laykea; YAO, Jiangchao; YOUNGMAN, Mark; WO2013/30665; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics