Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.

To a solution of 6b (1eq.) in isopropanol the amine 11 (2.5 eq.) and N,N-diisopropylethylamine(4 eq.) were added. The reaction mixture was irradiated with microwaves for 10min at 160 C. The reaction mixture was evaporated under reduced pressure. Theyellow residue was diluted with EtOAc and washed with water. The organic phasewas washed with ammonium chloride, dried over Na2SO4 andfinally evaporated under reduced pressure. The crude mixture was purified byflash chromatography on silica gel (CH2Cl2:MeOH 98:2) togive the desired compound 9b as awhite solid (67%). 1H NMR (400 MHz, CDCl3): delta(ppm)3.31(t, J=8, 4H); 4.07 (t, J=8, 4H), 4.55(s, 2H); 4.91-4.85 (2m, 2H); 5.47 (t,J=8, 1H); 6.88 (d, J=8, 2H); 7.19-7-33 (m, 6H), 7.89 (s,1H); 8.30 (s,1H). 13CNMR (CDCl3): delta(ppm) 44.98; 48.83; 53.59; 59.22; 64.99; 116.20;128.53; 128.82; 132.82; 134.80; 136.51; 150.24; 155.27. MS: m/z 483 [M+H]+.Anal. Calcd. For C24H25Cl2N7: C,59.75; H, 5.22; N, 20.32; found: C, 59.55; H, 5.12; N, 20.21, 216144-45-5

The synthetic route of 216144-45-5 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Radi, Marco; Bernardo, Vincenzo; Vignaroli, Giulia; Brai, Annalaura; Biava, Mariangela; Schenone, Silvia; Botta, Maurizio; Tetrahedron Letters; vol. 54; 38; (2013); p. 5204 – 5206;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

A mixture containing (4-chlorophenyl)phenyl methylamine free base (4.1 g, 18.8 mmol), N,N-bis(2-chloroethyl) 4-nitrophenyl carbamate (6.4 g, 20.8 mmol) potassium iodide (1.7 g, 10 mmol) and diisopropyl ethylamine (10.2 ml) was stirred at 140 C. (oil bath) for 4 hours.While cooling down, 60 ml dichloromethane was added. The mixture was stirred at ambient temperature for 20 min. 30 ml HCl (1M) was added to the dichloromethane. The organic layer was separated washed with NaCl (5 ml) dried and concentrated to give an oily material (13.6 g).Above crude material was dissolved in a solution containing 5.3 g NaOH in 10 ml H2O and 42 ml 2-propanol. The mixture was heated til 50 C. for 3 h 30 min.The mixture was concentrated in vacuo to get rid of 2-propanol and redissolved in 40 ml toluene and 20 ml H2O. The mixture was stirred for 30 min, the solid was filtered off and layers were separated. 40 ml HCl (2M) was added to the toluene layer and stirred for 20 min. Separated toluene layer was extracted again with 40 ml HCl (1M). Acidic layers were combined, washed with 40 ml toluene and basified. The mixture was extracted with toluene (80 ml). The separated organic layer was washed with H2O (10 ml), NaCl (10 ml) dried and concentrated in vacuo to give the desired product (1.2 g oil). To the crude product ethyl acetate (25 ml) was added, followed by addition of 0.9 g oxalic acid dissolved in 2 ml EtOH. Suspension was stirred 4 h at ambient temperature and overweekend at 5 C. Solid obtained was filtered off and dried at air to give a solid material (1.3 g, 17.6% yield). 98.56% ee purity., 300543-56-0

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

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

5747-48-8, 11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5747-48-8

Example I. Synthesis of quetiapine by reductive alkilation of 11-piperazindibenz[b,f][1,4]thioazepine with (2-hydroxyethoxy)acetaldehyde in the presence of sodium borohydride. The mixture of 11-piperazindibenz[b,f][1,4]thioazepine (1 g, 0,0034 mol), sodium acetate (0,8 g, 0,01 mol), glacial acetic acid (4 cm3), (2-hydroxyethoksy)acetaldehyde (0,35g, 0,0034 mol) and water (50 cm3) is cooled to 0C. Next sodium borohydride was slowly (40 min) added (5 g, 0,13 mol) in temperature 0C. After this time the mixture was stirred for 1 h in temperature 10C and 10% aq NaOH was added (to pH about 8-9). The mixture was extracted with diethyl ether (3×30 cm3), organic faze was dried by sodium sulfate. The product (1.17g) was obtain with purity about 98% (HPLC)

The synthetic route of 5747-48-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Celon Pharma Sp. z o.o.; EP1602650; (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.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.

Diethylcyanophosphonate (Aldrich, Buchs, Switzerland; 0.50 mL, 3.0 [MMOL)] is added to a stirred mixture of 3-[[4-(3-pyridinyl)-2-pyrimidinyl] amino] -benzoic acid (438 mg, [1.] 5 [MMOL),] 4- [[ (4-METHYL-1-PIPERAZINYL) METHYL]] benzeneamine (308 mg, 1.5 [MMOL)] and triethylamine (840 [.//L,] 3.0 [MMOL)] in 10 mL N,N-dimethylformamide at [10C.] After stirring for 12 hours at [60C,] the mixture is treated with an aqueous solution of sodium hydrogen carbonate and extracted three times with ethyl acetate. The combined extracts are washed with water, and the solvent is evaporated off under reduced pressure to give a residue. The residue is resuspended in water and filtered to afford the crude product which is recrystallised from tetrahydrofuran- ethyl acetate to give N-[3-[[4-(3-Pyridinyl)-2-pyrimidinyl]amino]-N-[(4-methyl-1-piperazinyl)- methyl] benzamide as a crystalline solid, m. p. [220-224C.], 70261-82-4

70261-82-4 4-(4-Methylpiperazin-1-ylmethyl)phenylamine 3153996, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2004/5281; (2004); 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.262368-30-9,N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide,as a common compound, the synthetic route is as follows.

A solution of methyl (Z)-3-((4-((tert-butyldimethylsilyl)oxy)phenyl)chloromethylene)-2-oxoindoline-5-carboxylate (200 mg, 0.45 mmol), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (136 mg, 0.52 mmol) and TEA (0.13 mL, 0.90 mmol) in EtOH (1.3 mL) was stirred under refluxed for overnight. The reaction solvent was evaporated under reduced pressure, and the residue was purified by column chromatography with dichloromethane/ethanol (50/1, v/v) to obtain the final compound 99 (166 mg, 54% yield): 1H NMR (500 MHz, CDCl3) _ 11.93 (s, 1H), 10.08 (s, 1H), 7.74 (dd, J = 8.2, 1.6 Hz, 1H), 7.31 (d, J = 8.5 Hz, 2H), 7.05 (s, 1H), 7.00 (dd, J = 8.3, 1.7 Hz, 3H), 6.97 (d, J = 8.4 Hz, 2H), 6.75 (d, J = 8.8 Hz, 2H), 3.75 (s, 3H), 3.19 (s, 3H), 2.84 (s, 2H), 2.44 (bs, 6H), 2.27 (s, 3H), 1.04 (s, 9H), 0.91 (s, 2H), 0.29 (s, 6H); 13C NMR (125 MHz, CDCl3) _ 171.5, 169.6, 167.5, 157.9, 157.4, 139.9, 139.4, 138.5, 130.4, 127.8, 126.2, 124.9, 124.4, 123.6, 122.7, 121.4, 120.5, 109.1, 98.3, 59.7, 54.9, 53.3, 51.8, 46.1, 37.5, 25.7, 18.4, -3.4, -4.3.

262368-30-9, As the paragraph descriping shows that 262368-30-9 is playing an increasingly important role.

Reference：
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; DALBY, Kevin N.; EDUPUGANTI, Ramakrishna; TALIAFERRO, Juliana; LEE, Juhyeon; (0 pag.)WO2018/160967; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

262368-30-9, N-(4-Aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of methyl (Z)-3-(chloro(4-(hydroxymethyl)phenyl)methylene)-2-oxoindoline- 5-carboxylate (17 mg, 0.05 mmol), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (15 mg, 0.06 mmol) and TEA (0.1 muL, 0.10 mmol) in EtOH (0.1 muL) was stirred under refluxed for overnight. The reaction solvent was evaporated under reduced pressure, and the residue was purified by column chromatography with dichloromethane/ethanol (50/1, v/v) to obtain the final compound 100 (15 mg, 52% yield): 1H NMR (500 MHz, DMSO-d6) _ 11.97 (s, 1H), 11.13 (s, 1H), 7.57 (d, J = 8.2 Hz, 1H), 7.51 (d, J = 7.8 Hz, 2H), 7.44 (d, J = 7.8 Hz, 2H), 7.13 (d, J = 8.2 Hz, 2H), 6.93 (d, J = 8.3 Hz, 1H), 6.90 (d, J = 8.2Hz, 2H), 6.51 (s, 1H), 5.49 (bs, 1H), 4.64 (s, 2H), 3.63 (s, 3H), 3.05 (bs, 2H), 2.69 (bs, 2H), 2.18 (bs, 6H), 2.10 (s, 3H); 13C NMR (125 MHz, DMSO-d6) _ 170.4, 168.6, 166.4, 157.2, 145.0, 140.4, 139.8, 130.3, 128.3, 127.8, 127.7, 127.0, 125.5, 124.0, 123.6, 121.3, 119.6, 108.8, 97.6, 62.4, 59.2, 54.6, 52.5, 52.4, 51.6, 51.5, 45.8, 36.7; HRMS (ESI-TOF) m/z calcd for C31H32N6O6 [M + H+] 569.2638 found 570.2713.

262368-30-9, The synthetic route of 262368-30-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM; DALBY, Kevin N.; EDUPUGANTI, Ramakrishna; TALIAFERRO, Juliana; LEE, Juhyeon; (0 pag.)WO2018/160967; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of 2-(3-bromopropyl) isoindoline-1,3-dione (1.0 g, 1 mmol) in N,N-dimethyl formamide DMF(5 mL), N-phenyl piperazine derivatives (1 mmol) andK2CO3 (1.1 g, 3 mmol) were added at room temperature.The reaction mixture was stirred at room temperature for 24h. The resulting solution was poured into ice cold water,which was then extracted with ethyl acetate. Ethyl acetatewas separated, dried over Na2SO4, and concentrated undervacuum to afford corresponding compounds 8a-g.

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

Reference：
Article; Venkatesh, Ramineni; Kasaboina, Suresh; Janardhan, Sridhara; Jain, Nishant; Bantu, Rajashaker; Nagarapu, Lingaiah; Medicinal Chemistry Research; vol. 25; 9; (2016); p. 2070 – 2081;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

(b) (2S,5R)-4-[5-(4-Bromo-3-trifluoromethoxy-phenylcarbamoyl)-pyridin-2-yl]-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester The product of the previous step (3.86 g, 10.2 mmol) (2S,5R)-2,5-dimethyl-piperazine-1-carboxylic acid tert-butyl ester (2.62 g, 12.2 mmol) and N,N-diisopropylethylamine (5.32 mL, 30.5) was dissolved in DMSO (12 mL). The reaction mixture heated at 120 C. for 3 h, diluted with EtOAc (100 mL), washed with water, and saturated NH4Cl, water, and brine. The reaction mixture was evaporated to about 40% volume and 3 M HCl in cyclopentyl methyl ether (4.24 mL, 12.7 mmol) was added slowly. Seeds from a previous run at smaller scale were added and the reaction mixture was stirred for 2 days and filtered to provide the HCl salt of the title intermediate (5.15 g, 83% yield). HPLC method C: Retention time=21.1 min

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

Reference：
Patent; THERAVANCE, INC.; US2012/114600; (2012); 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.

General procedure: Arylpiperazines (1.2 equiv) and potassium carbonate (4.0equiv) were added to a solution of 1 (1 equiv) in acetonitrile(CH3CN, 20 mL). The reaction mixture was heated to 85 Cand stirred for 12 h. Afterward the mixture was cooled toroom temperature. The reaction mixture was filtered, and thefiltrate was concentrated in vacuo. The residue was extractedwith ethyl acetate (60 mL) and water (20 mL). After dryingthe organic layer with anhydrous Na2SO4and evaporatingthe solvent under reduced pressure, a solid was appeared.The solid was recyrstallized from ethanol to obtain intermediates2.

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

Reference：
Article; Chen, Hong; Jia, Huixia; Qian, Yuna; Shen, Jianliang; Yu, Yuzhong; Zhang, Haibo; Zhao, Shanchao; Pharmacological Reports; (2020);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

161357-89-7, 1-(Methylsulfonyl)piperazine hydrochloride is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

4-(5-Chloro-2-methyl-2,3-dihydro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (100 mg) is added to a mixture of 1-(methylsulfonyl)piperazine hydrochloride (70 mg), Pd2(dba)3 (65 mg), Xantphos (123 mg), and potassium tert-butylate (75 mg) in toluene (4 mL) under an argon atmosphere. The reaction mixture is stirred in an oil bath at 105 C. over night. After cooling to room temperature water is added and the mixture is extracted with ethyl acetate. The combined extracts are concentrated in vacuo and the residue is chromatographed on silica gel (cyclohexane/ethyl acetate 50:50?0:100) to give the title compound. LC (method 1): tR=1.03 min; Mass spectrum (ESI+): m/z=481 [M+H]+., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2012/322784; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics