Month: December 2020

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

694499-26-8, To a solution of 3-(4-bromophenyl)propionic acid (42 mg, 0.18 mmol) in anhydrous N,N-dimethylformamide (2 mL) was treated HATU (139 mg, 0.36 mmol) andthe mixture was stirred at room temperature for 30 minutes. A solution of 4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)-aniline (50 mg, 0.18 mmol) and triethylamine (37 mg, 0.36 mmol) in anhydrous N,N-dimethylformamide (1.0 mL) was added. The reaction mixture was stirred at room temperature for 2 hours and partitioned between H20 (50 mL) and ethyl acetate (50 mL). The aqueous layer was extracted withethyl acetate (50 mL x 2). The combined organic extracts were washed with brine (100 mL), dried over sodium sulfate and concentrated in vacuum. The residue was purified by flash chromatography (Redisep silica gel, 9:1 dichloromethane/methanol) to afford 3 -(4- bromophenyl)-N- {4- [(4-methylpiperazin- 1 -yl)methyl] -3 -(trifluoromethyl)phenyl } -propanamide. ESI MS: m/z 486.05.

The synthetic route of 694499-26-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH (A*STAR); CHERIAN, Joseph; DURAISWAMY, Athisayamani Jeyaraj; NACRO, Kassoum; WO2014/88519; (2014); 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.54699-92-2,4-Methyl-1-piperazineacetic acid,as a common compound, the synthetic route is as follows.

54699-92-2, Example 13; General Method for the Preparation of Active Esters of N-Substituted Piperazine Acetic Acid from Trifluoroacetate Esters; A solution of the trifluoroacetate in THF (0.58 M, 1.2 equiv) was added to a solid sample of N-methyl piperazine acetic acid and mixed in a vortex or shaker until a homogeneous solution was obtained. The reaction of the carboxylic acid with the trifluoroacetate ester was generally complete within 30 min for all cases except N-hydroypyrrolidinone (NHP, 18 h). The progress of conversion to the active ester was monitored by ES-MS. The amount of product and any starting material (N-MPA) could be determined by direct infusion of a sample of the reaction (in ethanol) into the ES-MS. In some cases the active ester product was precipitated as dihydrochloride salt by the addition of a solution by addition of HCl solution in dioxane (4 M, 50% volume of the reaction) followed by washing with THF, ethyl acetate and hexanes. In other cases the product was isolated from the reaction as the mono TFA salt. Addition of TFA could be performed if the bis-TFA salt was desired. Dhbt ester, Calculated MH+ = 304.14 Found = 304.20 NHP ester, Calculated MH+ = 242.15 Found = 242.20 4-NP ester, Calculated MH+ = 280.13 Found = 280.20 1H NMR (400 MHz, CDCl3) d 8.20 (d, 2H, J=9.2 Hz, aromatic protons), 7.25 (d, 2H, J=9.2 Hz, aromatic protons), 3.69-3.40 (broad, 2H, ring protons), 3.57 (s, 2H, -CH2-CO-), 3.15-2.90 (broad, 6H, ring protons), 2.78 (s, 3H, -CH3). Pfp ester, Calculated MH+ = 325.10 Found = 325.10 Pcp ester, Calculated MH+ = 404.95 Found = 405.90 3-NP ester, Calculated MH+ = 280.13 Found = 280.20 NHS ester, Calculated MH+ = 256.13 Found = 256.10

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

Reference£º
Patent; Applera Corporation.; US2005/148771; (2005); A1;; ; Patent; Applera Corporation.; US2005/148774; (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.278788-66-2,(R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To the solution of tert-butyl (3R)-3-(hydroxymethyl)piperazine-l-carboxylate (1044 mg, 4.83 mmoi) in N,N-Diisopropylethylamine (2.57 mL, 14.48 mmoi) and DMF (7 niL) was added (E)- 2-cyano-4,4-dimethyl-pent-2-enoic acid (1109.1 mg, 7.24 mmoi) followed by HATU (486.6 mg, 5.79 mmoi). The mixture was stirred at rt for 1 h. The mixture was diluted with DCM and water and partitioned. The organic layer was dried with MgSOa and concentrated. The cmde mixture was purified by column chromatography to obtain tert-butyl (3R)-4-[(E)-2-cyano-4,4-dimethyl-pent-2-enoyl]-3- (hydroxymethyl)piperazine-l-carboxylate (1340 mg) as an oil., 278788-66-2

The synthetic route of 278788-66-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRINCIPIA BIOPHARMA INC.; LOU, Yan; OWENS, Timothy, Duncan; BRAMELD, Kenneth, Albert; GOLDSTEIN, David, Michael; (230 pag.)WO2018/136401; (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.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

A mixture containing (4-chlorophenyl)phenyl methylamine free base (4.1 g, 18.8 mmol), N,N-bis(2-chloroethyl)benzyl carbamate (7 g, 26.7 mmol) potassium iodide (1.7 g, 10 mmol) and diisopropyl ethylamine (10 ml) was stirred at 135 C. (oil bath), for 4 hours.While cooling down, 60 ml dichloromethane was added. The mixture was stirred at ambient temperature for 20 min. 35 ml HCl (1M) was added to the dichloromethane. The organic layer was separated, washed with NaCl (10 ml) dried and concentrated to give an oily material (10 g). The impure material was purified with AcOEt/heptane column (3?50%).0.5 grams of above pure material was dissolved in a solution containing 1.3 g NaOH in 1.2 ml H2O and 5 ml 2-propanol. The mixture was heated til 100 C. for 5 h. The mixture was concentrated in vacuo to get rid of 2-propanol and redissolved in 10 ml toluene and 5 ml H2O. The mixture was stirred for 20 min and layers were separated. The organic layer was dried over Na2SO4 and concentrated. To the crude product ethyl acetate (10 ml) was added, followed by addition of 0.2 g oxalic acid dissolved in 1 ml EtOH. The suspension was stirred 4 h at ambient temperature and overnight at 5 C. The solid obtained was filtered off and dried at air to give a solid material (0.3 g, 38.5% yield). 98.86% ee purity.

300543-56-0, 300543-56-0 (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine 668697, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Zhu, Jie; US2009/143582; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9,548762-66-9, (2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-fluorobenzoyl chloride(1.0 g, 7.14 mmol) in acetonitrile (10 mL) were added DIPEA (3.74 mL, 21.41 mmol) and HATU (3.53 g, 9.28 mmol) at room temperature. After 30 min., tert-butyl (2S,5R)-2,5-dimethylpiperazine-1- carboxylate (1.83 g, 8.56 mmol) was added and the reaction mixture was stirred overnight. The reaction mixture was concentrated under reduced pressure to remove volatiles and the residue dissolved in ethyl acetate (100 mL) and washed with water (50 mL). The aqueous layer was back extracted with ethyl acetate (100 mL x 2) and the combined organic layer was washed with brine, dried over anhydrous Na2SO4, concentrated under reduced pressure to obtain the crude product, which was purified by silica gel chromatography (50-100% EtOAc in petroleum ether; 40 g column) to afford tert-butyl (2S,5R)-4-(4-fluorobenzoyl)-2,5-dimethylpiperazine-1-carboxylate (1.99 g, 83 % yield). LCMS: m/z = 337.1 (M+H); retention time 1.62 min. [LCMS Condition: Column: Waters Acquity UPLC BEH C18 (2.1 x 50 mm) 1.7 mm, Mobile phase A: 10 mM NH4OAc:acetonitrile (95:5); Mobile phase B: 10 mM NH4OAc:acetonitrile (5:95), 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].

As the paragraph descriping shows that 548762-66-9 is playing an increasingly important role.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5308-25-8,1-Ethylpiperazine,as a common compound, the synthetic route is as follows.,5308-25-8

At Step 1, obtained 2-chloro-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine 80.0 g was in the dimethylformamide 560 ml and the temperature was raised to 70C after the input and the ethylpiperazine 47.29 g and diisopropylethylamine 46.38 g were reacted for 5 hours. The temperature of this reaction solution was cooled to the room temperature and the purified water 560ml was cooled after doing injection to 10C . Here, the generated Decision was filtered to the Nutsche filtration (Buchner funnel, Coors) and the residue was washed with the purified water 250 ml. This Decision was recrystallized as ethanol and it dried in 70C and the white blonanserin 100 g (yield 98.6 %) was obtained.

5308-25-8 1-Ethylpiperazine 79196, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SAM-OH PHARMACEUTICAL CO., LTD.; KIM, DAE SIK; HO, CHEOL; (6 pag.)KR2015/117123; (2015); A;,
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: Amine 15 (hydrochloride) (4.3 mmol) was dissolved in CH2Cl2 (5 ml), and the solution was cooled with an ice bath. A solution of ethyl chloroglyoxylate (4.7 mmol) in CH2Cl2 (2 ml) was added dropwise, and the mixture was stirred at 0C for 0.5-1 hour. The reaction solution was diluted with ethyl acetate. The organic layer was washed with an aqueous saturated sodium chloride solution and dried with anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure to obtain crude product. This crude product was dissolved in ethanol (13 ml), 2 mol/L sodium hydroxide (6.5 ml 13 mmol) was added, and the mixture was stirred at room temperature for 1.5 hour. The solvent was distilled off under reduced pressure, and 2 mol/L hydrochloric acid was added to the residue to acidic, and the precipitated crystal was collected by filtration. The crystal was washed with water and dried to obtain carboxylic acid 16 (yield 77-99%). To carboxylic acid 16 (1.0 mmol) were added DMF (10 ml), aniline (1.2 mmol), HOBt (1.2 mmol), triethylamine (1.2 mmol), DMAP (0.05 mmol) and WSCD¡¤HCl (1.2 mmol). The mixture was stirred at room temperature for overnight. An aqueous saturated sodium bicarbonate solution was added, and the aqueous layer was extracted with EtOAc. The organic layer was washed with brine, dried over MgSO4, and concentrated under reduced pressure. The residue was purified by amino silica gel column chromatography (CHCl3/MeOH, gradient: 0-10% MeOH) to afford oxamide 6a-v (yield 46-91%).

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

Reference£º
Article; Anan, Kosuke; Masui, Moriyasu; Tazawa, Aya; Tomida, Minoru; Haga, Yoshihiro; Kume, Masaharu; Yamamoto, Shoichi; Shinohara, Shunji; Tsuji, Hiroki; Shimada, Shinji; Yagi, Shigenori; Hasebe, Nobuyoshi; Kai, Hiroyuki; Bioorganic and Medicinal Chemistry Letters; vol. 29; 9; (2019); p. 1143 – 1147;,
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.

5464-12-0, 10.0 g 2-chloro-3-methyl-4-(4,4, 5, 5-tetramethyl-l, 3,2-dioxaborolan-2-yl)phenol (from Step K) (37.2 mmol), 8.7 g 2-(4-methylpiperazin-l-yl)ethanol (60.3 mmol) and 15.8 g PPh3 (60.3 mmol) were dissolved in 100 mL dry toluene and then 27 mL diethyl azodicarboxylate (60.3 mmol, 40 percent solution in toluene) was added dropwise. The mixture was stirred at 50 ¡ãC under argon for 1.5 hours. The volatiles were evaporated under reduced pressure and 100 mL Et20 was added. The precipitated white crystals were filtered off and washed with Et20. The filtrate was concentrated under reduced pressure and purified via flash chromatography using CHC13 and MeOH as eluents. The resulting light brown oil was crystallized from hexane to give l-[2-[2-chloro-3-methyl-4-(4,4,5,5- tetramethyl-l,3,2-dioxaborolan-2-yl)phenoxy]ethyl]-4-methyl-piperazine as an off-white solid. 1H NMR (500 MHz, DMSO-d6): 7.56 (d, 1H), 6.99 (d, 1H), 4.15 (t, 2H), 2.72 (t, 2H), 2.51 (s, 3H), 2.50 (br s, 4H), 2.29 (br s, 4H), 2.13 (s, 3H), 1.29 (s, 12H)

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; PACZAL, Attila; BALINT, Balazs; KOTSCHY, Andras; CHANRION, Maia; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; SIPOS, Szabolcs; PROSZENYAK, Agnes; (102 pag.)WO2016/207216; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

74879-18-8, A mixture of 2-(4-bromophenyl)-5-methylpyrimidine 78 (250mg, 1.008mmol), palladium acetate (50mg), cesium carbonate (400mgf1.23mmol), (S)-2-methyl piperazine(200mg, 2mmol) and 2-Di-t-butylphosphino)-biphenyl (50mg, 0.167mmol) was stirred in dioxane:water (10ml,v/v 5:1 ) at reflux temperature for 4 hours. The reaction was cooled.diluted with MeCI2 (100ml) and H2O (50ml). The organic layer was separated, dried (MgSO4), filtered and solvent evaporated. The residue was purified by chromatography eluting with 100% EtOAc then with 10% v/v MeOHZEtOAcZIVJH4OH yielding product 79 as a white solid. (220mg.81%) ESMS (MH, 269).

The synthetic route of 74879-18-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SCHERING CORPORATION; WO2007/70398; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

74879-18-8, (S)-(+)-2-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

74879-18-8, Triethylamine (2.85 ml) was added to a solution of (S)-2-methyl piperazine (1 g) in methanol (25 ml), this was followed by portionwise addition of BOC anhydride (2.18 g). The reaction mixture was stirred for 17 h, then concentrated under reduced pressure. Water was added to the residue and extracted EtOAc (¡Á3), dried (MgSO4) and evaporated under reduced pressure. The residue was purified by chromatography on silica (eluent EtOAc, then 9:1:1 EtOAc:MeOH:NH3) to give the sub-title compound as a colourless oil, yield 1.3 g.1H NMR CDCl3: delta 4.04-3.82 (2H, m), 2.95 (1H, d), 2.81-2.66 (3H, m), 2.48-2.32 (1H, m), 1.47 (9H, s), 1.05 (3H, d).

As the paragraph descriping shows that 74879-18-8 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; US2008/255150; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics