Tag: M.W:200-300

300543-56-0, (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

40.0 g of 1-[(R)-(4-chlorophenyl) (phenyl) methyl] piperazine, 14.1 g of sodium hydrogen carbonateAnd a mixture of 78.1 g of N-methyl-2-pyrrolidoneHeat to 120 C, ethyl (2-chloroethoxy) acetateAfter 27.9 g was dropped over 30 minutes, the mixture was stirred for 6 hours.After cooling the obtained suspension to room temperature, 200 g of waterAnd toluene 69gAnd the mixture was separated.120 g of water is added to the obtained organic layer, and liquid separation is performed again to obtain the formula (6).; Example 1 32 g of water was added to a toluene solution of the compound (6) obtained in Reference Example 1, and a solution of 7.0 g of lithium hydroxide monohydrate dissolved in 44 g of water was added dropwise at room temperature. It stirred until it became 0.2% or less. Liquid separation was carried out after the obtained solution, 8 g of N-methyl-2-pyrrolidone for washing, 139 g of toluene and 25 g of acetone were mixed. To the separated aqueous layer were added 139 g of toluene and 13 g of acetone to carry out liquid separation again. Further, 139 g of toluene and 9 g of acetone were added to the separated aqueous layer, and liquid separation was performed again. 35 g of toluene and 193 g of methyl ethyl ketone were added to the obtained aqueous layer, and 29.1 g of 35% hydrochloric acid was dropped to adjust the pH to 2.4, and the solution was heated to 45 C. to separate. After 35 g of toluene was added to the obtained organic layer, concentration was performed until the remaining amount became 95 g. Furthermore, 97 g of methyl ethyl ketone and 35 g of toluene were added and concentrated until the remaining amount reached 99 g, and further 24 g of methyl ethyl ketone and 9 g of toluene were added and concentrated until the remaining amount became 101 g. After adding methyl ethyl ketone 64g and acetone 411g at room temperature and dropping 7.3g of 35% hydrochloric acid,0.04 g of levocetirizine dihydrochloride was added.Subsequently, 316 g of acetone was dropped, and after stirring for 1.5 hours, 6.9 g of 35% hydrochloric acid was dropped. After filtering the obtained suspension, the obtained solid was washed with 95 g of acetone. The obtained crystals were dried under reduced pressure at 40 C. to obtain 54.6 g of levocetirizine dihydrochloride. The purity was 99.8% or more, 300543-56-0

The synthetic route of 300543-56-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Chemical Co., Ltd.; Yoshida, Kazuhiro; Ando, Kenichi; (13 pag.)JP2019/43885; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

122323-88-0, Methyl piperazine-2-carboxylate dihydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 16 A solution of di-tert-butyl dicarbonate (5.0 g) in dichloromethane (30 ml) is added dropwise, taking one hour at 0 C while stirring, to a mixture of methyl piperazine-2-carboxylate dihydrochloride (5.0 g), triethylamine (7 g) and dichloromethane (70 ml). The reaction mixture is poured into ice-water and extracted with dichloromethane. The organic layer is washed with water and dried, then the solvent is distilled off under reduced pressure. The residue is purified by means of a silica gel column chromatography (eluent, dichloromethane:acetone:ethanol = 5:5:1) to afford methyl 4-tert-butoxycarbonylpiperazine-2-carboxylate as a colorless oily product (4.9 g)., 122323-88-0

As the paragraph descriping shows that 122323-88-0 is playing an increasingly important role.

Reference£º
Patent; Takeda Chemical Industries, Ltd.; EP368670; (1990); 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.303-26-4,1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

13.O g (0.2 mol) pulverized zinc are added to the mixture of 300 ml of toluene, 30 ml (0,52 mol) of glacial acetic acid (96% by weight) and 30 ml of methanol with stirring. Subsequently, in three equal portions during 15 minutes, 50.0 g (0.10 mol) (R)-(+)-4-(4-chlorophenyl)-rhohenylmethyl- piperazine- 1 -(2,2,2-trichloroethyl-carbamate) hydrochloride (compound of the Example 6) are added. The temperature of the greyish suspension is raising to approximately 41 to 45 0C in 10 minutes and intense evolution of carbon dioxide occurs.After one hour, the suspension is filtered, the filtrate is mixed with 40 ml of water and 38.5 ml of 25 % by weight ammonium hydroxide solution. The layers are separated, the toluene layer is dried over potassium carbonate and the solvent is evaporated.The thus obtained yellow, oily evaporation residue (approx. 42 g) having the content of 75.5 % calculated as free base, is dissolved in 500 ml of acetone and 12.8 g (0.11 mol) fumaric acid are added. The product, which initially separates in an oily form, is stirred for three hours at the temperature of 25 0C. The crystalline product is filtered and dried until constant weight.Yield, 31.3 g (77.8%) off-white crystals Melting temperature, 146-148 0C. Elemental Analysis {calculated on the basis of the Formula C21Hi3ClN2O4 (402.9)}:Calculated^: 62.61 H: 5.75 Cl: 8.80 N: 6.95 Measured: C: 62.27 H: 5.72 Cl: 8.79 N: 6.84Optical purity (chiral high performance liquid chromatography): 99.S %, 303-26-4

303-26-4 1-((4-Chlorophenyl)(phenyl)methyl)piperazine 9340, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; EGIS GYOGYSZERGYAR NYRT.; WO2007/66163; (2007); A2;,
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.169448-87-7,(R)-tert-Butyl 2-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

(E)-3-[4-(2-Ethyl-5,7-dimethyl-pyrazolo[1,5-a]pyrimidin-3-ylmethyl)-phenyl]-propenal (7) (100 mg, 0.313 mmol), (R)-tert-butyl 2-(hydroxymethyl)piperazine-1-carboxylate (67.7 mg, 0.313 mmol), NaBH(OAc)3 (103 mg, 0.485 mmol) and DIPEA (0.063 ml, 0.363 mmol) were dissolved in 2 ml of dichlorethane and stirred for 4 h at rt. Then the mixture was diluted with EtOAc, washed with NaCl-solution and dried over Na2 SO4. Evaporation gave a yellow oil. The crude product was purified by chromatography (silica gel, ethyl acetate/methanol) to yield a white foam.

169448-87-7, As the paragraph descriping shows that 169448-87-7 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; MILTZ, Wolfgang; OBERHAUSER, Berndt; VAUPEL, Andrea; VELCICKY, Juraj; WEIGAND, Klaus; LELETI, Rajender Reddy; LIU, Yugang; DU, Zhengming; US2012/252778; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

30459-17-7, 1-(4-Trifluoromethylphenyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of substituted piperazine (10 mmol), 4-uoroben-zaldehyde (10 mmol) and K2CO3 (2 mmol) were reuxed at130 C in DMF for 15-24 h. Thereafter, the reaction mixture waspoured into ice cold water and the precipitate that appeared wasltered and dried to accomplish formyl derivatives (14-25) in ayield of 80-90%, 30459-17-7

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

Reference£º
Article; Mishra, Chandra Bhushan; Manral, Apra; Kumari, Shikha; Saini, Vikas; Tiwari, Manisha; Bioorganic and Medicinal Chemistry; vol. 24; 16; (2016); p. 3829 – 3841;,
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.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

mixture of tert-butyl 2-methylpiperazine- I -carboxylate (0.077 mL, 0.383 mmol), rac-(6S,7R,8R)-5-acetyl-6-cyclopropyl-7-methyl-8-(phenylamino)-5,6,7,8-tetrahyd ro- I ,5-naphthyridin-2-yltrifluoromethanesulfonate (for a preparation see Intermediate 102, 90 mg, 0.192 mmol) and cesium carbonate (187 mg, 0.575 mmol) in 1,4-dioxane (7 mL) had nitrogen bubbled through it for 10 mm. BINAP (23.87 mg, 0.038 mmol) and Pd2(dba)3 (17.55 mg, 0.019 mmol) were added and the reaction mixture was stirred at 90 C under nitrogen for 3 h. The reaction mixture was allowed to cool to rtthen filtered through celite, rinsed with ethyl acetate and concentrated under a stream of nitrogen. The sample was dissolved in 1:1 MeOH:DMSO (2×1 mL) and purified by MDAP (HpH). The appropriate fractions were combined and concentrated in vacuo. The sample was dissolved in DMSO:MeOH (1:1, 1 mL) and purified by MDAP (Formic). The appropriate fractions were combined and concentrated in vacuo to give the product (11 mg, 0.021 mmol, 11.04%) as a yellow gum. Thiswas a racemic mixture of diastereoisomers. LCMS (2 mm Formic): Rt = 1 .40 mi [MH] = 520.

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

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; AMANS, Dominique; ATKINSON, Stephen John; HARRISON, Lee Andrew; HIRST, David Jonathan; LAW, Robert Peter; LINDON, Matthew; PRESTON, Alexander; SEAL, Jonathan Thomas; WELLAWAY, Christopher Roland; WO2014/140076; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

General procedure: A mixture of compound 9 (200mg, 0.8mmol), sodium iodine (289mg, 1.93mmol) and substituted amines (1.61mmol) in methanol (30mL) was stirred at 40C for 5h. After the reaction was completed (monitored by TLC), the solution was concentrated under vacuum. Then the crude residue was purified by column chromatography (dichloromethane/methanol), affording pure product 10., 208167-83-3

208167-83-3 tert-Butyl 4-(2-chloroethyl)piperazine-1-carboxylate 22106269, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Liang, Yu-Kun; Yue, Zhi-Zhou; Li, Jia-Xin; Tan, Cun; Miao, Ze-Hong; Tan, Wen-Fu; Yang, Chun-Hao; European Journal of Medicinal Chemistry; vol. 84; (2014); p. 505 – 515;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The compound (R) -4-Boc-2- methylpiperazine (528mg, 2.64mmol), glacial acetic acid (190mg, 3.16mmol), 1-ethyl-3- (3- Dimethylaminopropyl) carbodiimide hydrochloride (758mg, 3.95mmol) and N- hydroxy-7-azabenzotriazole(897mg, 6.59mmol) was dissolved In dichloromethane (20 mL), and under conditions of 0 C tothis solution was added dropwise N, N- diisopropylethylamine (1.8mL, 10.54mmol), stirred at roomtemperature Stirred 12h, was added water (10mL ¡Á 2) washing the organic phase was dried over anhydrous Na 2SO 4, the solvent was removed concentrate was separated by column chromatography (leaching Lotion: DCM /MeOH (v / v) = 40/1), to give 580mg colorless oil: Compound N- acetyl-4-tert-butoxycarbonyl -2- (R) – methylPiperazine, yield: 90%., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); 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.692058-21-2,1-Boc-4-(2,2,2-trifluoroethyl)piperazine,as a common compound, the synthetic route is as follows.

692058-21-2, tert-Butyl-l-piperazinecarboxylate (1.00 g, 5.37 mmol) and pyridine (0.868 mL, 10.7 mmol) were combined in methylene chloride (27 mL) and cooled to 0 C. Trifluoroacetic anhydride (0.910 mL, 6.44 mmol) was then added and the reaction mixture was allowed to warm to ambient temperature and stirred 1 h. The reaction mixture was then diluted with ethyl acetate (150 mL) and washed with aqueous potassium hydrogen sulfate (2 x 50 mL), saturated aqueous sodium bicarbonate (50 mL) and brine (50 mL), then dried over sodium sulfate and evaporated to yield tert-butyl 4-(2,2,2-trifluoroacetyl)piperazine-l-carboxylate (1.50 g, 99%) as an oil which solidified over time. tert-Butyl 4-(2,2,2-trifluoroacetyl)piperazine-1-carboxylate (0.908 g, 3.22 mmol) was added to a solution of borane-tetrahydrofuran complex (8 mmol) in tetrahydrofuran (24 mL) and the reaction mixture was heated at reflux for 2 h. After cooling, 2 N hydrochloric acid (4 mL) was carefully added and the reaction mixture was stirred until gas evolution ceased and then diluted with ethyl acetate (200 mL). Aqueous sodium hydroxide (0.2 M, 75 mL) was then added and the phases were separated. The organic layer was dried over sodium sulfate and evaporated. The residue was purified by column chromatography (eluting with 20% ethyl acetate in hexanes) to give tert-butyl 4-(2,2,2-trifluoroethyl)piperazine-1-carboxylate (0.627 g, 73%) as a white solid. A solution of hydrochloric acid (4.0 M, 10 mL) in dioxane was added to a solution of tert-butyl 4-(2,2,2-trifluoroethyl)piperazine-l-carboxylate (0.736 g, 2.74 mmol) in dioxane (5 mL). The reaction mixture was stirred until analysis by thin layer chromatography indicated completion of reaction (approx. 3 h). The volatiles were evaporated and the residue was dried under vacuum to yield 1- (2,2,2-trifluoroethyl)piperazine (0.631 g, 95%) as a white solid.

The synthetic route of 692058-21-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F.HOFFMANN-LA ROCHE AG; WO2005/110996; (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.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, To a stirred solution of tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (0.35 g, 1.63 mmol) in acetonitrile (8 mL) were added DIPEA (0.9 mL, 4.9 mmol) and methyl 2-bromo-2-(5-(trifluoromethyl)pyridin-2-yl)acetate (0.54 g, 1.79 mmol) at room temperature. The reaction mixture was heated at 85 C for 16 h. The reaction mixture was cooled to room temperature, concentrated under reduced pressure to obtain the crude product, which was purified by silica gel chromatography (24 g; using 6 % -10 % ethyl acetate/ petroleum ether) to obtain tert-butyl (2S,5R)-4-(2-methoxy-2-oxo-1-(5- (trifluoromethyl)pyridin-2-yl)ethyl)-2,5-dimethylpiperazine-1-carboxylate (0.52 g, 74 % yield). LCMS: m/z = 432.2 (M+H); retention time 2.19 min [LCMS method: Column: Waters Acquity UPLC BEH C18 (2.1 x 50 mm), 1.7 mm; Mobile phase A: 0.1% TFA in water; Mobile phase B: 0.1 % TFA in acetonitrile; Gradient = 20-90 % B over 1.1 minute, then a 0.6 minute hold at 90 % B; Temperature: 50 C; Flow rate: 0.7 mL/min; Detection: UV at 220 nm].

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

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; VELAPARTHI, Upender; CHUPAK, Louis S.; DARNE, Chetan Padmakar; DING, Min; GENTLES, Robert G.; HUANG, Yazhong; KAMBLE, Manjunatha Narayana Rao; MARTIN, Scott W.; MANNOORI, Raju; MCDONALD, Ivar M.; OLSON, Richard E.; RAHAMAN, Hasibur; JALAGAM, Prasada Rao; ROY, Saumya; TONUKUNURU, Gopikishan; VELAIAH, Sivasudar; WARRIER, Jayakumar Sankara; ZHENG, Xiaofan; TOKARSKI, John S.; DASGUPTA, Bireshwar; REDDY, Kotha Rathnakar; RAJA, Thiruvenkadam; (0 pag.)WO2020/6018; (2020); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics