Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.78818-15-2,Benzyl 3-oxopiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,78818-15-2

Preparation 57; 4-{5-[4-(2-Methoxy-(1S)-methyl-ethoxy)-phenyl]-[1,3,4]oxadiazol-2-ylmethyl}-3- oxo-piperazine-1-carboxvlic acid benzyl ester; A solution of potassium carbonate (136mg, 2. 4mmol) suspended in tetrahydrofuran (3mL) was cooled to 0C. Tetrabutylammonium bromide (130mg, 0. 40mol), 4-benzyloxycarbonyl piperazin-2-one (568mg, 2. 43mmol), and the product of preparation 48 (572mg, 2. 02mmol), were added in tetrahydrofuran (3mL) and the mixture was allowed to warm to room temperature and stir for 18 hours. The solvent was then evaporated under reduced pressure and the residue was dissolved in ethyl acetate and washed with water and brine. The organic phase was dried over magnesium sulfate and concentrated in vacuo to give an oil. Purification by column chromatography on silica gel, eluting with pentane: diethyl ether 90: 10 to 20: 80, gave the title compound as a pale brown foam in 70% yield, (679mg). ‘H NMR (CDCI3, 400MHz) d : 1.40 (d, 3H), 3.40 (s, 3H), 3.50 (m, 1H), 3.55 (t, 2H), 3.60 (m, 1H), 3.80 (t, 2H), 4.15 (s, 2H), 4.64 (m, 1H), 4.90 (s, 2H), 5.15 (s, 2H), 7.00 (d, 2H), 7.40 (m, 5H), 7.95 (d, 2H). MS APCI+ m/z 481 [MH] +

78818-15-2 Benzyl 3-oxopiperazine-1-carboxylate 736777, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; PFIZER LIMITED; PFIZER INC.; WO2005/82866; (2005); 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.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 (4.0 equiv)were added to a solution of 2 (100 mg, 0.43 mmol) in acetonitrile(CH3CN, 15 mL). The reaction mixture was heated to 85 C and stirred for 16 h. Afterward the mixture was cooled to room temperature. The reaction mixture was filtered, and the filtrate was concentrated invacuo. Then the residue was purified by chromatography on silica-gel column (petroleum ether: ethyl acetate=3:1, v/v) to obtain the corresponding products (3-24).

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

Reference：
Article; Chen, Hong; Zhang, Jingxiao; Hu, Peixin; Qian, Yuna; Li, Jing; Shen, Jianliang; Bioorganic and Medicinal Chemistry; vol. 27; 20; (2019);,
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.76003-29-7,1-Boc-3-Oxopiperazine,as a common compound, the synthetic route is as follows.,76003-29-7

NaH (60 % in mineral oil) (0.24 g; 5.99mmol) was added to a solution of Int. 177 (1 g; 4.99 mmol) in DMF (8 ml) and cooled to 0 C under N2-gas atmosphere. The mixture was stirred at this temperature for 10 min. Methyl bromoacetate (0.522 mL; 5.49 mmol) was added. The cooling bath was removed and the reaction stirred overnight. Subsequently, the reaction was quenched with H20 (2 ml ). A saturated NaCl aqueous solution (20 ml) was added and the mixture was extracted with EtOAc (14 ml ). The organic layer was dried over MgS04, filtered and concentrated to dryness. The residue was purified by chromatography over silica gel eluting with a gradient from 100 % DCM to 40 % DCM and 60 % DCM/MeOH 9/1, v/v. The desired fractions were collected and the solvent was evaporated. Yield: 1.14 g of Int. 178 (84 %).

As the paragraph descriping shows that 76003-29-7 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICA NV; DIELS, Gaston, Stanislas, Marcella; SCHOENTJES, Bruno; VERSELE, Matthias, Luc, Aime; BERTHELOT, Didier, Jean-Claude; WILLEMS, Marc; VIELLEVOYE, Marcel; EMBRECHTS, Werner, Constant, Johan; WROBLOWSKI, Berthold; MEERPOEL, Lieven; WO2015/150555; (2015); 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(p-tolyl)methylene)-2-oxoindoline-5-carboxylate (100 mg, 0.31 mmol), N-(4-aminophenyl)-N-methyl-2-(4-methylpiperazin-1-yl)acetamide (92 mg, 0.35 mmol) and TEA (0.09 mL, 0.61 mmol) in EtOH (1.0 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 94 as a yellow solid (169 mg, quant. yield): 1H NMR (500 MHz, DMSO-d6) _ 11.94 (s, 1H), 11.12 (s, 1H), 7.57 (dd, J = 8.2, 1.7 Hz, 1H), 7.40 – 7.36 (m, 4H), 7.14 (d, J = 8.1 Hz, 2H), 6.93 (d, J = 8.2 Hz, 1H), 6.90 (d, J = 8.3 Hz, 2H), 6.50 (s, 1H), 3.64 (s, 3H), 3.05 (bs, 2H), 2.69 (bs, 1H), 2.43 (s, 3H), 2.19 (bs, 6H), 2.10 (s, 3H); 13C NMR (125 MHz, DMSO-d6) _ 170.4, 168.6, 166.4, 157.3, 140.4, 140.0, 139.8, 137.5, 130.0, 129.3, 128.4, 127.8, 125.4, 124.1, 123.6, 121.3, 120.0, 108.8, 97.5, 59.2, 54.6, 52.4, 51.6, 45.8, 36.7, 21.1; HRMS (ESI-TOF) m/z calcd for C31H32N6O6 [M + H+] 553.2689 found 554.2772., 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.883554-88-9,4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester,as a common compound, the synthetic route is as follows.,883554-88-9

To a solution of tert-butyl4-carbamoylpiperazine-1-carboxylate (0.16 g, 0.7 mmol) in DCM (2 mL) was addeda HCl in EtOAc solution (4 M, 2 mL) . The mixture was stirred at rt for 30 min andconcentrated to give the title compound as a white solid (0.16 g, 100) . 1H NMR (600 MHz, CD3OD): delta ppm 3.71-3.73 (m, 4H) , 3.25-3.27 (m, 4H) and MS-ESI: m/z 130.10[M+H-HCl] + .

883554-88-9 4-Carbamoyl-piperazine-1-carboxylic acid tert-butyl ester 17750351, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); 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.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 24 2-[4-((4S,5R)-4,5-Bis-(4-chloro-phenyl)-1-{4-[2-(11,1-dioxo-isothiazolidine-2-yl)-ethyl]-piperazine-1-carbonyl}-4,5-dimethyl-4,5-dihydro-1H-imidazol-2-yl)-3-ethoxy-phenyl]-2-methyl-propionitrile To a stirred solution of 1-Boc-4-(2-aminoethyl)-piperazine (1.26 g, 6.8 mmol, Aldrich) and triethylamine (1 mL) in tetrahydrofuran (10 mL), 3-chloro-propylsulfonyl chloride (0.68 mL, 6.94 mmol, Aldrich) was added slowly at room temperature. The mixture was stirred for 30 min at room temperature and the reaction was quenched with water. It was extracted with ethyl acetate and the extracts were combined and dried over anhydrous sodium sulfate. The solids were filtered off, and the filtrate was concentrated in vacuo to give 4-[2-(3-chloro-propane-1-sulfonylamino)-ethyl]-piperazine-1-carboxylic acid tert-butyl ester., 192130-34-0

The synthetic route of 192130-34-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Ding, Qingjie; Graves, Bradford James; Kong, Norman; Liu, Jin-Jun; Lovey, Allen John; Pizzolato, Giacomo; Roberts, John Lawson; So, Sung-Sau; Vu, Binh Thanh; Wovkulich, Peter Michael; US2007/129416; (2007); 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

To a solution of Intermediate 2 (1.0 g, 4.1 mmol) in anhydrous dichloromethane (40 mL) was added triethylamine (0.82 mL, 5.9 mmol) and 3-methoxy-4-tert-butylbenzoyl chloride* (1.11 g, 4.9 mmol). The resultant mixture was stirred at ambient temperature for 18 hours and washed with water. The organic phase was separated and evaporated to a gum, then purified by chromatography over silica gel using cyclohexane-ethyl acetate (4: 1, 3: 1 and then 2: 1 v/v) as eluent. The fractions containing the desired product were combined and evaporated to give the title compound as an amorphous solid. MS calcd for (C23H34N206 + H) + : 435. Found: (M+H) + = 435. * Prepared from 3-methoxy-4-tert-butylbenzoic acid (J. Org. Chem. (1961) 26,1732) using thionyl chloride., 129799-08-2

129799-08-2 1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 2756819, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; GLAXO GROUP LIMITED; WO2005/79799; (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.187669-60-9,1-(4-(Methylsulfonyl)phenyl)piperazine,as a common compound, the synthetic route is as follows.

Example 80; 4-{2-[4-(4-Mcthancsulfonylphcnyl)pipcrazin-l-yl]-2-oxocthyl}pipcridinc-l- carboxylic acid ferf-butyl ester; To a solution of l-(4-methanesulfonylphenyl)piperazine (0.22 g, 0.91 mmol), 4-carboxy methylpiperidine-1-carboxylic acid tert-butyl ester (0.20 g, 0.80 mmol), HOBT.H2O (0.14 g, 0.91 mmol) and DIPEA (0.47 mL, 2.72 mmol) in DMF (5mL) was added EDCI (0.19 g, 0.99 mmol) and the mixture was stirred for 18h. The solvent was removed under vacuum and the resulting residue was partitioned between EtOAc and saturated NaHCO3 solution. The aqueous phase was re-extracted with EtOAc, the organic extracts were combined, washed with brine, dried (MgSO4) and adsorbed onto SiO2. The adsorbed sample was purified by flash chromatography eluting with 50:50 EtOAc:hexane to afford the title compound: RT = 3.26 min; m/z (ES+) = 466.33 [M+H]+., 187669-60-9

The synthetic route of 187669-60-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PROSIDION LIMITED; WO2007/3964; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,129799-15-1

Potassium carbonate (1 .2 g, 8.7 mmol) was added to a solution of 3-(2-bromo-thiazol-4-yl)-5-(2,6-difluoro-phenyl)-4,5-dihydro-isoxazole (1.25 g, 3.6 mmol) and 1-N-Boc-2-piperazinecarboxylic acid methyl ester (1 .1 g, 4.4 mmol) in 15 ml of acetonitrile. The reaction mixture was stirred for 150 h at 90 00 and subsequently cooled and filtered. The solid potassium salt was washed with ethyl acetate and the filtrate as well as the washing layers were combined and evaporated. The remainder was purified by column chromatography onsilica gel (cyclohexane I ethyl acetate 4: 1) to obtain 4-{4-[5-(2,6-difluoro-phenyl)-4,5- di hydro-isoxazol-3-yl]-th iazol-2-yl}-piperazine-1 ,2-d icarboxylic acid 1 -tert-butyl ester 2-methyl ester as a light yellow foam. M.p. 68 – 72 00 1H-NMR (400 MHz, 0D013): oe = 1.42 – 1.53 (m, 9H), 3.09 (dd, 1 H), 3.33 (dt, 2H), 3.52 (dd, 1 H), 3.69 (t, 1 H), 3.74 (s, 3H), 3.91- 4.08 (m,2H), 4.42 (dd, 1H), 4.70 -4.93 (m, 1H), 6.02 (t, 1H), 6.89 (t, 2H), 7.00 (s, 1H), 7.24- 7.31 (m, 1H). MS: mlz = 509 (M+1).

As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference：
Patent; SYNGENTA PARTICIPATIONS AG; LAMBERTH, Clemens; SULZER-MOSSE, Sarah; CEDERBAUM, Fredrik; UMARYE, Jayant; SONAWANE, Ravindra; WO2013/127784; (2013); 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.70261-81-3,1-Methyl-4-(4-nitrobenzyl)piperazine,as a common compound, the synthetic route is as follows.

70261-81-3, EXAMPLE 3 4-((4-methyl-1-piperazinyl)methyl)aniline (I-c) Crude I-a (8.5g, 36.2mmol), FeO(OH)/C, 2.0 g as catalyst and 95% ethanol (100 ml) were added into a 500 mL single neck flask, which was refluxed. Into the reaction system were added slowly and dropwise a mixture of 25 mL hydrazine hydrate and 20 mL 95% ethanol. The depletion of the starting materials was confirmed by TLC (methanol: chloroform = 1:15). Suction filtration was performed while the reaction mixture was hot. The filter cake was washed with hot ethanol twice (30 ml *2). After removal of the solvent under reduced pressure, white solid was obtained, which was dried under vacuum to give 6.7 g (I-c); Yield: 90.3%. The product was used for subsequent reaction without further purification. 1H-NMR[300MHz, DMSO-d6]: delta2.1 (3H, s, -CH3), 2.3-2.5 (8H, m, -CH2-*4), 3.5 (2H, s, -CH2-), 4.0(2H, s, -NH2), 7.5 (2H, d, J = 8.7 Hz, ArH), 8.1 (2H, d, J = 8.7 Hz, ArH).

As the paragraph descriping shows that 70261-81-3 is playing an increasingly important role.

Reference：
Patent; China Pharmaceutical University; LU, Tao; WANG, Yue; CHEN, Yadong; LU, Yi; WANG, Zhanwei; JIN, Qiaomei; YANG, Taotao; LIN, Guowu; GUO, Qinglong; ZHAO, Li; EP2955185; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics