Tag: M.W:200-300

1030377-21-9, (S)-1-Boc-2-(Hydroxymethyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (S)-tert-butyl 2-(hydroxymethyl)piperazine-l -carboxylate (850.9 mg, 3.93 mmol) and 2-(tert-butoxymethyl)oxirane (850 mg, 6.46 mmol) in ethanol (10 mL) was heated at 120 C for 30 min using microwave. The mixture was concentrated to dryness. The residue was purified with flash column chromatography on silica gel using 1-10% methanol in dichloromethane to afford a oil as the product in quantitative yield. 1H NMR (500 MHz, Chloroform-^ delta 4.09 (s, lH), 3.84 (m, 3H), 3.38 (dt, J= 9.0, 3.7 Hz, l H), 3.28 (m, 3H), 3.04 (dd, J = 24.2, 1 1.7 Hz, 1H), 2.88 – 2.80 (m, 2H), 2.48 – 2.32 (m, 3H), 2.26 – 2.21 (m, 1H), 2.13-2.08 (m, 1H), 1.44 (s, 9H), 1.17 (d, 9H). MS for ^Eta34Nu205: 347.2 (MH+).

1030377-21-9, 1030377-21-9 (S)-1-Boc-2-(Hydroxymethyl)piperazine 22884145, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NEKTAR THERAPEUTICS (INDIA) PVT. LTD.; NEKTAR THERAPEUTICS; SHARMA, PANKAJ; KHATRI, VIJAY KUMAR; GU, XUYUAN; SONG, YUAN; SHEN, MICHAEL LIXIN; SAUTHIER, JENNIFER RIGGS; ANAND, NEEL K.; KOZLOWSKI, ANTONI; ODINECS, ALEKSANDRS; RILEY, TIMOTHY A.; REN, ZHONGXU; MU. YONGQI; SHEN, XIAOMING; YUAN. XUEJUN; AURRECOECHEA, NATALIA; O’MAHONY, DONOGH JOHN ROGER; WO2015/92819; (2015); 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.548762-66-9,(2S,5R)-tert-Butyl 2,5-dimethylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate (500 mg, 2.33 mmol) in dry acetonitrile (10 mL), methyl 2-bromopropanoate (468 mg, 2.80 mmol) and DIPEA (1.22 mL, 7.00 mmol) were added at room temperature. The reaction mixture was heated to 85 C for 16 h. The reaction mixture was cooled to room temperature and concentrated under reduced pressure to obtain the crude product, which was purified by Combi flash 24 g silica gel chromatography by using 0-30% ethyl acetate in petroleum ether as eluent to obtain tert-butyl (2S,5R)-4-(1-methoxy-1-oxopropan-2- yl)-2,5-dimethylpiperazine-1-carboxylate (620 mg, 88 % yield) as a light yellow liquid. LCMS: m/z, 301.2 (M+H); retention time 2.941 and 3.094 min. Column: Kinetex XB- C18 (3 x 75 mm) 2.6 mm; Mobile phase A: 10 mM ammonium formate: acetonitrile (98:2), Mobile phase B: 10 mM ammonium formate: acetonitrile (2:98), Gradient = 20- 100 % B over 4 minutes, then a 0.6 minute hold at 100 % B; Temperature: 27 C; Flow rate: 1.0 mL/min; Detection: UV at 220 nm, 548762-66-9

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

Reference：
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

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

Example 2 1-(2,4-Difluorophenyl)-1,4-dihydro-4-oxo-6-fluoro-7-(3-methyl-4-tert-butyloxycarbonyl-piperazin-1-yl)-3-quinoline carboxylic acid A 50 gallon glass lined reactor was purged with nitrogen and charged with 44.5 kg of dimethylsulfoxide, 2.3 kg of triethylamine, 6 kg of methanol, 5.0 kg of 1-(2,4-difluorophenyl)-6-fluoro-7-chloro-1,4-dihydro-4-oxo-quinoline carboxylic acid (see U.S. Patent No. 4,730,000) and 12 kg of 1-tert-butyloxycarbonyl-2-methylpiperazine. The slurry was stirred and heated to 95 +- 2C. After 2 hours, 3 kg more of 1-tert-butyloxycarbonyl-2-methylpiperazine and 3 liters of methanol were added. After 4 and 27 hours, respectively 5 kg and 3 kg more of 1-tert-butyloxycarbonyl-2-methylpiperazine were added. After 36 hours, the reaction temperature was lowered to 60C. To the stirred mixture was added 41 liters of isopropanol that had been preheated to 55C. The slurry resulting from the above reaction was cooled to room temperature, filtered and washed with isopropanol. The filter cake was added to 25 liters of 100C acetic acid and heated to reflux. The slurry was cooled to 19C, filtered and washed with isopropanol. The solid was dried at 40C overnight, yielding 3.1 kg of the title compound. m.p. 254-256C. 300 MHz 1H NMR 8.60 (s, 1H), 8.10 (d, 1H), 7.50 (m, 1H), 7.28-7.15 (m, 3H), 6.21 (d, 1H), 4.33 (br d, 1H), 3.94 (br d, 1H), 3.41-3.18 (m, 4H), 2.91 (m, 1H), 2.72 (m, 1H), 1.46 (s, 9H), 1.30 (d, 3H)., 120737-78-2

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

Reference：
Patent; ABBOTT LABORATORIES; EP350950; (1990); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

16154-72-6, 3-Chloro-4-(4-methylpiperazin-1-yl)benzenamine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of 4-anilino-pyrimidine intermediate 3 (50 mg, 1.0 equiv.), the corresponding aniline B-ring aniline (1.0 equiv.), 2 drops of 4 M HC1, and EtOH (1 mL) was heated in a microwave reactor at 100 C for 1 h. Sodium bicarbonate (ca. 100 mg) was added to the mixture, stirred for 30 min at room temperature, and concentrated under reduced pressure. Unless otherwise mentioned, all products were purified via column chromatography using DCM/MeOH (0-10%).

16154-72-6, The synthetic route of 16154-72-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC.; SCHOeNBRUNN, Ernst; LAWRENCE, Nicholas J.; LAWRENCE, Harshani R.; (293 pag.)WO2017/66428; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

(E)-(3-(3-(2-(2-Pyridyl))vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole was added to a round bottom flask. 6-yl) thio)propionic acid (50 mg) followed by N,N-dimethylformamide (5 ml), 4-((4-methylpiperazin-1-yl)methyl)aniline (28 mg ),2-(7-oxidized benzotriazole)-N,N,N’,N’-tetramethylureaFluorophosphate (70 mg) and triethylamine (0.05 ml).The reaction system was stirred at room temperature for 14 hours under argon atmosphere.After the reaction is over,The system was evaporated to dryness under reduced pressure.The resultant was diluted with water and extracted with ethyl acetate.Organic phase with water,After washing with saturated brine, it was dried over anhydrous sodium sulfate.The organic phase is filtered,After evaporation under reduced pressure, the crude product was dissolved in anhydrous dichloromethane (5ML),Trifluoroacetic acid (1 mL) was added.The reaction system was stirred at room temperature for 14 hours under argon atmosphere.After the reaction,The system is evaporated to dryness under reduced pressure.The resultant was diluted with water and neutralized to pH > 10 with a saturated sodium hydrogen carbonate solution.The aqueous phase was extracted with ethyl acetate.Organic phase with water,After washing with saturated brine, it was dried over anhydrous sodium sulfate.The organic phase is filtered,After evaporation under reduced pressure, a crude product was obtained.The crude product was purified by column chromatography on silica gel to yield purified compound 134.

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

Reference：
Patent; Chinese Academy Of Sciences Hefei Matter Sciences Institute; Liu Jing; Liu Qingsong; Liu Xuesong; Wang Beilei; Jiang Zongru; Yu Kailin; Chen Cheng; Zou Fengming; Liu Qingwang; Liu Xiaochuan; Wang Wei; Wang Wenliang; Hu Chen; Wang Wenchao; Wang Junjie; Wang Li; (82 pag.)CN109942544; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

373608-48-1, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 50 mL RBF was added tert-butyl 4-(3-aminopropyl)piperazine-1-carboxylate (1.105 g, 4.54 mmol), DCE (Volume: 10.32 ml), 5-methylpicolinaldehyde (0.5 g, 4.13 mmol) and STAB-H (1.575 g, 7.43 mmol). The reaction was stirred overnight then diluted with DCM and quenched with 2M NaOH. The organic layer was dried with Na2SO4, filtered and concentrated to a yellow oil which was purified via silica gel chromatography (DCM 2 minutes, 10% B(80:20:3, DCM:MeOH:NH4OH) 5 minutes and 50% B 9 minutes) to afford tert-butyl 4-(3-(((5-methylpyridin-2-yl)methyl)amino)propyl)piperazine-1-carboxylate (0.75 g, 2.152 mmol, 52 % yield). 1H NMR (400 MHz, CDCl3): delta = 8.36 (d, J= 2.0 Hz, 1H), 7.44 (dd, J= 7.9, 2.2 Hz, 1H), 7.18 (d, J= 7.9 Hz, 1H), 3.87 (s, 2H), 3.42 (t, J= 5.1 Hz, 4H), 2.73 (t, J= 6.8 Hz, 2H), 2.42 (t, J= 7.1 Hz, 2H), 2.38 (t, J= 5.0 Hz, 4H), 2.31 (s, 3H), 1.75 (pent, J= 6.9 Hz, 2H), 1.45 (s, 9H);

373608-48-1, The synthetic route of 373608-48-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; WILSON, Robert James; NGUYEN, Huy Hoang; KIM, Michelle Bora; WILSON, Lawrence; MILLER, Eric James; TAHIROVIC, Yesim Altas; TRUAX, Valarie; KAISER, Thomas; (311 pag.)WO2018/156595; (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.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: A solution of the pyridine (1.0 eq.) in dry. THF (0.1 M) was treated dropwise with s-BuLi solution (1.4 M in cyclohexane, 1 eq.) at 78 C and stirred at this temperature for 1 h. The reaction solution was then treated with a solution of the aldehyde or the isocyanate (2.5 eq.) in dry THF (1.2 M), and the reaction mixture was slowly warmed to rt overnight. After the addition of water and sat. amMonium chloride solution, the heterogeneous mixture was extracted three times with EtOAc. The combined organic layers were washed with sat. sodium chloride solution, dried over anhydrous magnesium sulfate, and the crude product was concentrated in vacuo. The product was isolated by means of flash chromatography on silica gel.

197638-83-8, The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J.L.; Laraia, Luca; Waldmann, Herbert; Tetrahedron; vol. 74; 35; (2018); p. 4531 – 4537;,
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.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

3-Iodo-4-fluoro-methyl nicotinic acid (225 mg, 0.8 mmol) was dissolvedin N, N- dimethylformamide (5 mL), was added N, N- diisopropylethylamine (180mu, 1.09 mmol) and 2- (7-BTA) -Nu, Nu, Nu ‘, Nu’- tetramethyluroniumhexafluorophosphate (610 mg, 1.6 mmol), stirred for 5 min add 3 -trifluoromethyl-4- (4-methyl-piperazinyl small ylmethyl) aniline (198 mg, 0.72mmol), the reaction mixture was stirred at room temperature 26 h. Aftercompletion of the reaction system was added water, extracted with ethyl acetatetwice. The combined organic layer was purified by column chromatography togive 4-fluoro-3-iodo -N- [4- (4- methyl – piperazin-1-ylmethyl)-3-trifluoromethyl – phenyl] – nicotinamide (white solid, 420 mg)., 694499-26-8

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

Reference：
Patent; Shanghai Pharmaceuticals Holding Co.,Ltd .; WAN, HUIXIN; LI, CHUNLI; SHI, Chen; Liu, Haiyan; Li, Ping; XIA, Guangxin; HAN, Yanan; (52 pag.)CN103420977; (2016); B;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

548762-66-9,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.

(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). Analytical HPLC: Retention time=21.1 min.

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

Reference：
Patent; Thalladi, Venkat R.; Nzerem, Jerry; Huang, Xiaojun; Zhang, Weijiang; US2013/295048; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step D: tert-butyl (3)-4-[2-(3-cyano-4-fluorophenyl)-2-oxoethyl]-3-(hydroxymethyl)piperazine-1-carboxylate; 5-(Bromoacetyl)-2-fluorobenzonitrile (590 mg, 2.44 mmol) and (S)-4-N-BOC-2-hydroxymethyl-piperazine (527 mg, 2.44 mmol) were dissolved in THF (40 mL) at 0C thenTEA (247 mg, 2.44 mmol) was added. The reaction mixture was stirred at RT for 16 h, thenpoured into water and extracted with ethyl acetate. The organic layer was dried over Na2S04,filtered, and evaporated to dryness. The crude product was purified by MPLC through an 80g Redi-sep column using 0-100% EtOAc/hexane to yield the title compound., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; WO2013/28474; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics