Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.373608-48-1,tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

JQ-acid (176.6 mg, 0.441 mmol, 1 eq) was dissolved in DMF (4.4 mL) at room temperature. HATU (176 mg, 0.463 mmol, 1.05 eq) was added, followed by DIPEA (0.23 mL),1.32 mmol, 3 eq). After 10 minutes, tert-butyl 4-(3 -aminopropyl)piperazine- 1 -carboxylate (118 mg, 0.485 mmol, 1.1 eq) was added as a solution in DMF (0.44 mL). After 24 hours, the mixture was diluted with half saturated sodium bicarbonate and extracted twice with DCM and once with EtOAc. The combined organic layer was dried over sodium sulfate, filtered and condensed. Purification by column chromatography (ISCO, 24 g silica column, 0-15% MeOHIDCM, 23minute gradient) gave a yellow oil (325.5 mg, quant yield)1H NMR (400 MHz, Chloroform-cl) 7.67 (t, J 5.3 Hz, 1H), 7.41 – 7.28 (m, 4H), 4.58 (dd, J 7.5, 5.9 Hz, 1H), 3.52-3.23 (m, 8H), 2.63 (s, 9H), 2.37 (s, 3H), 1.80- 1.69 (m, 2H), 1.64 (s, 3H), 1.42(s,9H). ?3CNIVIR(100IVIHz,cdcl3) 171.41, 164.35, 155.62, 154.45, 150.20, 136.92, 136.64,132.19, 131.14, 130.98, 130.42, 129.98, 128.80, 80.24, 56.11, 54.32, 52.70, 38.96, 37.85, 28.42,25.17, 14.43, 13.16, 11.82. LCMS 626.36 (M+H)., 373608-48-1

373608-48-1 tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate 17750945, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; BRADNER, James; ROBERTS, Justin; BEHMAN, Nabet; WINTER, Georg; PHILLIPS, Andrews, J.; HEFFERNAN, Timothy, P.; BUCKLEY, Dennis; (617 pag.)WO2018/148440; (2018); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.,163765-44-4

Example 129: Synthesis of N -(( E )-5-hydroxyadamantan-2-yl)-6-(( R )-2-methylpiperazin-1-yl)picolinamide (Intermediate 10) [325] [326] Step 1: Synthesis of ( R )-tert-butyl 4-(6-((( E )-5-hydroxyadamantan-2-yl)carbamoyl)pyridin-2-yl)-3-methylpiperazine-1-carboxylate [327] 6-Bromo-N-((E)-5-hydroxyadamantan-2-yl)picolinamide(1.0 g, 2.847 mmol), (R)-tert-butyl 3-methylpiperazine-1-carboxylate (855 mg, 4.271 mmol), Pd2(dba)3 (52 mg, 0.057 mmol), xantphos (99 mg, 0.171 mmol), and sodium-tert-butoxide (410 mg, 4.271 mmol) were suspended in toluene (20 ml), and then the resulting liquid was stirred at 100oC under nitrogen stream for 3 hours. A saturated aqueous ammonium chloride solution (20 ml) was added to the resulting reaction liquid, followed by extraction with MC (40 ml x 2). The organic layer was dried over anhydrous sodium sulfate, followed by filtration and concentration, and then the residue thus obtained was subjected to MPLC (90% EtOAc/Hexanes), to obtain 720 mg of pale yellow solid (54%).

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; SK Chemicals Co.,Ltd.; RYU, Je Ho; KIM, Shin Ae; RYU, Keun Ho; KIM, Jae Sun; KIM, Nam Ho; HAN, Hye Young; KIM, Yong Hyuk; YOUN, Won-No; LEE, Yoon-Jung; SON, Hyun Joo; LEE, Bong-yong; PARK, Sung Hoon; LEE, Ju Young; LEE, Hyun Jung; JUNG, Hoe Chul; SHIN, Young Ah; LEE, Jung A; LEE, Bo Ram; SA, Joon Ho; WO2011/139107; (2011); A2;,
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70261-82-4,70261-82-4, 4-(4-Methylpiperazin-1-ylmethyl)phenylamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

C. 4-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-7-(trifluoromethyl)quinoline A solution of 4-chloro-7-trifluoromethylquinoline (400 mg, 0.0018 M), 1-methyl-4-[(4-aminophenyl)methyl]piperazine (400 mg, 0.0019 M) and 1.4 ml of ethanolic hydrogen chloride in 10 ml of ethanol is heated to reflux, under nitrogen for 15 minutes. The reaction mixture is quenched with ice, neutralized with aqueous 10% sodium hydroxide and extracted with methylene chloride. The methylene chloride solution is washed with water, saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated to a white solid. This solid, after recrystallization from ethyl acetate, gives 250 mg (32%) of white crystalline 4-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-7-(trifluoromethyl)quioline of melting point 218-220 C. Anal. Calcd. for C22 H23 F3 N4: Calcd. C, 65.98; H, 5.79; H, 13.99. Found C, 64.82; H, 5.98; N, 13.44.

As the paragraph descriping shows that 70261-82-4 is playing an increasingly important role.

Reference£º
Patent; The Upjohn Company; US4140775; (1979); A;,
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694499-26-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

Step 12.2: 3-Bromo-4-methyl-N-[4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-benzamide To a solution of 6.1 g (0.025 mol) 3-bromo-4-methylbenzoic acid chloride in 50 mL of acetonitrile are added at 10 C. 7 mL (0.05 mol) triethylamine followed by dropwise addition of a solution of 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine in 50 mL of acetonitrile (exothermic reaction). The brown suspension is stirred for 5 h at rt and is then allowed to stand over night. Ethyl acetate is added and the solution washed with saturated sodium bicarbonate solution and brine, dried with sodium sulphate and evaporated. Flash-chromatography on silica gel using dichloromethane/ethanol 93:7 containing 1% conc. ammonia gives pure title product: Rf (dichloromethane/ethanol 93:7 with 1% conc. ammonia)=0.4; HPLC tR=3.14 min; MS-ES+: (M+H)+=470, 472.

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

Reference£º
Patent; Caravatti, Giorgio; Furet, Pascal; Imbach, Patricia; Martiny-Baron, Georg; Perez, Lawrence Blas; Sheng, Tao; US2006/35897; (2006); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step C. 2-Ethyl-N-(3-fluoro-4-piperazin-1-yl-phenyl)-butyramide. To a solution of 4-(4-amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (2.0 g, 8.9 mmol) and Et3N (1.4 mL, 10.0 mmol) in DCM (60 mL) was added 1-ethylbutyryl chloride (1.4 mL, 10.0 mol). The mixture was stirred for 18 h, quenched with 1 N NaHCO3 (50 mL), and extracted with DCM (3*50 mL). The organic layers were combined, dried (Na2SO4), and concentrated. Chromatography of the residue (SiO2; EtOAc/hexanes) gave 4-[4-(2-ethyl-butyrylamino)-2-fluoro-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. Step A. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenyl]-piperazine-1-carboxylic acid tert-butyl ester. To a solution of 4-(4-amino-2-fluoro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (2.96 g, 10.0 mmol) and TEA (1.52 g, 15.0 mmol) in DCM (60 mL) was added 2-ethyl butyryl chloride (2.08 g, 15.0 mmol). After 18 h, the mixture was diluted with DCM (50 mL) and washed with satd. aq. NaHCO3 (1¡Á30 mL) and water (2¡Á30 mL). The organic layer was dried (Na2SO4) and concentrated. The residue was purified (SiO2; acetone/DCM and EtOAc/DCM) to yield the title compound (2.00 g, 51%). 1H NMR (CDCl3): 7.55-7.45 (m, 1H), 7.15 (br s, 1H), 7.14-7.08 (m, 1H), 6.86 (t, J=9.0, 1H), 3.62-3.54 (m, 4H), 3.01-2.93 (m, 4H), 2.04-1.96 (m, 1H), 1.76-1.65 (m, 2H), 1.60-1.50 (m, 2H), 1.48 (s, 9H), 0.94 (t, J=7.4, 6H).; Step A. 4-[4-(2-Ethyl-butyrylamino)-2-fluoro-phenyl]-piperazine-1-carboxylic acid tert-butyl ester.; To a solution of 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylic acid-tert-butyl ester (3.11 g, 10.5 mmol) and TEA (1.60 g, 15.8 mmol) in DCM (50 mL) was added 2-ethylbutyryl chloride (2.17 mL, 15.8 mmol) slowly. After 18 h, the mixture was washed with water, dried (Na2SO4), and concentrated. The residue was purified twice [SiO2; 1) acetone/DCM, 2) EtOAc/hexanes] to give the title compound. (2.07 g, 50%)., 154590-35-9

154590-35-9 tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate 16203630, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; Bonaventure, Pascal; Carruthers, Nicholas I.; Chai, Wenying; Dvorak, Curt A.; Jablonowski, Jill A.; Rudolph, Dale A.; Seierstad, Mark; Shah, Chandravadan R.; Swanson, Devin M.; Wong, Victoria D.; US2007/100141; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

5521-39-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5521-39-1,2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol,as a common compound, the synthetic route is as follows.

General procedure: To a stirred solution of compound 7, 8, or 9 (1 equiv) in 1-butanol was added compounds 12(1.1 equiv) and p-toluenesulfonic acid (1 equiv). The mixture was placed in a pressure flask, and heated to 100C for 15h. The reaction mixture was quenched by saturated Na2CO3 aqueous solution, and then was extracted with DCM and the organic phase was washed with water, dried over anhydrous Na2SO4. The combined organic layer was concentrated under reduced pressure and was further purified by flash column chromatography using dichloromethane/methanol as eluent to afford product H1-H14, Y1-Y14, or L1-L14 as a pale yellow solid.

5521-39-1 2-(4-(4-Aminophenyl)piperazin-1-yl)ethanol 767100, apiperazines compound, is more and more widely used in various fields.

Reference£º
Article; Hou, Yunlei; Zhu, Liangyu; Li, Zhiwei; Shen, Qi; Xu, Qiaoling; Li, Wei; Liu, Yajing; Gong, Ping; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 690 – 709;,
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Piperazines – an overview | ScienceDirect Topics

5747-48-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5747-48-8,11-(Piperazin-1-yl)dibenzo[b,f][1,4]thiazepine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of isocyanate (1.877mmol) in toluene (2.5mL) was added a solution of a monosubstituted piperazine (1.877mmol) in toluene (1.0mL). The reaction mixture was heated at 40-45C for 30 to 60min. The reaction mixture was then cooled down to room temperature (22-25C) and the resulting solids were filtered and washed with more toluene (2.0mL). The wet solids were then placed in 2.0mL of toluene, stirred at room temperature for about 30min, filtered and washed with toluene (1.0mL) to obtain the crude disubstituted piperazine derivative. Finally, all crude derivatives were purified by silica-gel column chromatography using a mixture of dichloromethane/methanol (9:1) to afford pure piperazines products.

As the paragraph descriping shows that 5747-48-8 is playing an increasingly important role.

Reference£º
Article; Patil, Mahadev; Noonikara Poyil, Anurag; Joshi, Shrinivas D.; Patil, Shivaputra A.; Patil, Siddappa A.; Bugarin, Alejandro; Bioorganic Chemistry; vol. 92; (2019);,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

674792-05-3, (S)-1-Boc-2-Isopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,674792-05-3

[00339] To a solution of (5)-tert-butyl 2-isopropylpiperazine-1-carboxylate (400 mg, 1.76 mmol) in anhydrous toluene (10 mL) was added methyl 4-bromo-2-(methylsulfonyl)benzoate (1.03 g, 4.8 mmol), X-phos (80 mg, 0.17 mmol), Cs2CO3 (1.50 g, 4.62 mmol) and Pd2(dba)3 (200 mg, 0.22 mmol) under N2. The reaction mixture was stirred at 100 oC overnight. The reaction was quenched with water (20 mL), and extracted with EtOAc (4 X 20 mL). The combined organic layers were dried over anhydrous Na2504, filtered, concentrated and then purified by preparative TLC with petroleum ether / EtOAc 5/1 to afford (5)-tert-butyl 2- isopropyl-4- (4- (methoxycarbonyl)-3- (methylsulfonyl)phenyl)piperazine- 1 -carboxylate (500 mg, 65% yield) as a grey solid.

As the paragraph descriping shows that 674792-05-3 is playing an increasingly important role.

Reference£º
Patent; VITAE PHARMACEUTICALS, INC.; CLAREMON, David, A.; DONG, Chengguo; FAN, Yi; LEFTHERIS, Katerina; LOTESTA, Stephen, D.; SINGH, Suresh, B.; TICE, Colin, M.; ZHAO, Wei; ZHENG, Yajun; ZHUANG, Linghang; (185 pag.)WO2016/22521; (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.30459-17-7,1-(4-Trifluoromethylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: Carbonyldiimidazole (0.97g, 0.006mol) in 5mL of dry THF was added to a solution of intermediates 1 (1.11g, 0.006mol), 2 (1.19g, 0.006mol), 3 (1.19g, 0.006mol) or 4 (1.28g, 0.006mol) dissolved in 10mL of anhydrous THF while stirring. After the end of gaseous (carbon dioxide) evolution (c.a. 0.5h), the respective secondary amines (0.006mol) dissolved in 5mL of anhydrous THF was added dropwise. The mixture was stirred at room temperature (approx. 24h) and evaporated to dryness. The crude product was purified by column chromatography (dichloromethane/methanol, 9:0.3, v/v). The final amides were obtained as solid substances followed by concentration of organic solvents under reduced pressure, and recrystallization from 2-propanol.

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

Reference£º
Article; Kami?ski, Krzysztof; Zagaja, Miros?aw; Rapacz, Anna; ?uszczki, Jarogniew J.; Andres-Mach, Marta; Abram, Micha?; Obniska, Jolanta; Bioorganic and Medicinal Chemistry; vol. 24; 4; (2016); p. 606 – 618;,
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

Intermediate 1 from Method X (50 mg) was dissolved in anhydrous dichloromethane (3 mL) and treated with 41 mg of tert-butyl 2-methylpiperazine- 1 – carboxylate. To the resulting solution was added activated 4 A molecular sieves, and the mixture was stirred 2 hrs at room temperature. 33 mg of sodium triacetoxy borohydride was added, and the reaction was stirred overnight, after which it was diluted with dichloromethane, washed with water and brine, and dried over MgS04 to yield the title compound.

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

Reference£º
Patent; UNIVERSITY OF ROCHESTER; BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA; GELBARD, Harris A.; DEWHURST, Stephen; GENDELMAN, Howard E.; WO2014/85795; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics