Tag: M.W:200-300

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.

Step 1: tert-butyl 4-(5-bromopyridin-2-yl)-3-oxopiperazine-1-carboxylate A mixture of 2,5-dibromopyridine (1.00 g; 4.22 mmol), tert-butyl 3-oxopiperazine-1-carboxylate (562 mg; 2.80 mmol) and Cs2CO3 (1.37 g; 4.20 mmol) in toluene (20 mL) was purged with nitrogen and added Pd2(dba)3 (129 mg; 0.14 mmol) and XantPhos (97 mg; 0.17 mmol). The reaction mixture was stirred at 100 C. overnight, cooled to room temperature, diluted with EtOAc (50 mL), filtered through Celite, washed with water (50 mL), brine (50 mL), dried over anhydrous Na2SO4, filtered, concentrated, and purified by a silica gel chromatography (petroleum ether/EtOAc=10/1, v/v) to afford 955 mg (96%) of the title compound as a yellow oil. LC-MS: m/z 355.8 [M+H]+., 76003-29-7

76003-29-7 1-Boc-3-Oxopiperazine 3157178, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ITEOS THERAPEUTICS; Crosignani, Stefano; Cauwenberghs, Sandra; Driessens, Gregory; Deroose, Frederik; US2015/225367; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-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: (3S,9aR)-3-(3-Cyano-4-fluoro-2-methyl-phenyl)-3-hydroxy-hexahydro-pyrazino[2, 1-cli 1,4loxazine-8-carboxylic acid tert-butyl ester: Diisopropylethylamine (156 mL, 894 mmol)was added to a stirred, room temperature mixture of 3-(2-Bromo-acetyl)-6-fluoro-2-methyl-benzonitrile (176 g, 688 mmol) and (R)-4-N-Boc-2-hydroxymethyl-piperazine (149 g, 688 mmol)in THE (3500 mL) and the mixture was stirred at room temperature for 18 h. The reaction wasdiluted with 3 L EtOAc, washed 2x with 1500 mL 10% wlw NaHCO3 aqueous solution, dried over Mg504, filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80% EtOAc/Hexanes, linear gradient), to provide the title compound, 278788-66-2

As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

630125-91-6, To a solution 4-(2-(cyclopropanecarboxamido)thiazolo[4,5-b]pyrazin-6- yl)benzoic acid (50 mg, 0.15 mmol) in DMF (1.0 mL) was added N, N- diisopropylethylamine (70 muL, 0.44 mmol), 2-(lH-7-azabenzotriazol-l-yl)-l, 1,3,3- tetramethyl uronium hexafluorophosphate methanaminium (112 mg, 0.29 mmol) and A- ((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl)aniline (51 mg, 0.17 mmol). The reaction mixture was stirred at room temperature for 16 h. The crude product was diluted with DMSO (1 mL) and purified by preparative reverse-phase HPLC (acetonitrile/water gradient) to give the title compound as a TFA salt. 1H NuMR 600 MHz (DMSO-J6) delta 13.21 (s, IH), 10.65 (s, IH), 9.56 (bs, IH), 9.29 (s, IH), 8.36 (J, J= 7.2, IH), 8.24 (s, IH), 8.13 (m, 3H), 7.72 (J, J= 7.8 Hz, IH), 3.69 (s, 2H), 3.46 (m, 2H), 3.13 (m, 2H), 2.98 (m, 4H), 2.40 (m, 2H), 2.06 (m, IH), 1.19 (m, 3H), 1.02 (m, 4H), MS m/z : 610.25 (M + 1).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; CHOI, Hwan, Geun; SIM, Taebo; GRAY, Nathanael; ZHOU, Wenjun; CHANG, Jae, Won; ZHANG, Jianming; WEISBERG, Ellen; WO2010/144909; (2010); 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.34334-28-6,4-(4-Methylpiperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

Under nitrogen, 4- (4-methylpiperazin-1-yl) benzonitrile (500 mg, 2.48 mmol) and tetraisopropyl titanate (1.25 mL, 4.22 mmol) were added to ether (10 mL). Ethylmagnesium bromide (1.82 mL, 5.46 mmol, 3M ether solution) was added dropwise to the reaction system at 78 C.The reaction was stirred at room temperature for 1.5 hours.Boron trifluoride ether (0.94 mL, 7.45 mmol) was then dropped into the reaction system, and the reaction system was stirred at room temperature for 1 hour.The reaction solution was quenched with water, the reaction solution was extracted with ethyl acetate, the organic phase was separated, and the residue was purified by silica gel column chromatography (dichloromethane / methanol = 95/5) to obtain 1- (4- (4-methylpiperazine). Azin-1-yl) phenyl) cyclopropylamine (7A, 180 mg, yield: 31%) was a yellow oil., 34334-28-6

As the paragraph descriping shows that 34334-28-6 is playing an increasingly important role.

Reference：
Patent; Shanghai Dinuo Pharmaceutical Technology Co., Ltd.; Zhao Zhiming; (42 pag.)CN110467629; (2019); A;,
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.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

Example 2 6-(4-Methanesulfonyl-piperazin-l-vI)-2-morphoHn-4-yl-[4,5’lbipyriinidinyl-2′-ylamine (4) A mixture of Intermediate Al (198mg), Intermediate G (230mg) and potassium carbonate (293mg) was stirred in acetonitrile (10ml) at room temperature. After 24 hours the reaction mixture was diluted with ethyl acetate, washed with water, dried (MgSO4) and the solvent removed in vacuo. The residue was recrystallised from ethyl acetate/hexane to yield 4-[4-chloro-6-(4-methanesulfonyl-piperazin-l-yl)-yrimidin-2- yl]-morpholine (206mg). Reaction of 4-[4-chloro-6-(4-methanesulfonyl-piperazin- 1 -yl)-yrimidin-2-yl]- morpholine with 2-aminopyrimidine-5-boronic acid, pinacol ester using standard Suzuki conditions yielded the desired title compound. IH NMR (400MHz, CDCl3) 2.80 (3H,s), 3.28-3.24 (4H,m), 3.82-3.75 (12H,m), 5.20 (2H,s,br.), 6.16 (lH,s), 8.91 (2H,s)., 161357-89-7

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

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; WO2009/66084; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

655225-01-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The compound obtained in Example 35-2 (74 mg, 0.55 mmol) was dissolved in DMF (1.5 ml). There to cesium carbonate (214 mg, 0.66 mmol), tertiaryButyl 4- (2-bromomethyl) piperazine-1-Carboxylate(323 mg, 1.1 mmol), potassium iodide (183 mg, 1.1 mmol) and stirred overnight at 70 ° C. was added a. After the reaction, the solvent was evaporated. The residue was purified by silica gel column chromatography (Chromatorex NH 20 g, hexane / ethyl acetate) to give the title compound (184 mg, 96.3percent) as a yellow oil.

655225-01-7 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate 15946441, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Yakult Honsha Co., Ltd.; University of Occupational and Environmental Health; Ono, Masahiro; Kobayashi, Tsuneyuki; Yamazaki, Ryuta; Haibara, Hirotake; Nishiyama, Yukiko; Hokkyo, Atsuko; Nishiyama, Hiroyuki; Kurita, Akinobu; Matsuzaki, Ken; Kono, Kimitoshi; Izumi, Hiroto; (215 pag.)JP2016/124812; (2016); A;,
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.

694499-26-8, 3-Iodo-4-methy1-N-(4-((4-methy1piperazin-1-y1)methy1)-3-(trfluoromethy1)pheny1)Benzamide: 3-Iodo-4-methylbenzoyl chloride (0.48 g, 1.7 mmol), prepared from the reaction of3-iodo-4-methylbenzoic acid and SOCI2 (as previously described), was added to a solution of 4-((4-methylpiperazin-1 -yl)methyl)-3-(trifluoromethyl)aniline (0.47 g, 1.7 mmol), N,N5 diisopropylethylamine (0.26 g, 2.0 mmol), and a catalytic amount of DMAP in THF (10 mL).After stirring at rt for 2 h, the reaction was quenched with water. EtOAc was added and the layers separated. The combined organic layers were concentrated to dryness and purified by silica gel chromatography (eluted with 5% MeOH/DCM, MeOH was pre-saturated with ammonia gas), to provide 0.51 g of product as an off-white solid.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ARIAD PHARMACEUTICALS, INC.; GOZGIT, Joseph, M.; RIVERA, Victor, M.; SHAKESPEARE, William, C.; ZHU, Xiaotian; DALGARNO, David, C.; WO2013/162727; (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.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a solution of 1-tert-butyl 3-methyl piperazine-1,3-dicarboxylate (2.44 g, 10 mmol) in DCM (50 mL) was added phenylboronic acid (2.35 g, 20 mmol), Cu(OAc)2 (1.82 g, 10 mmol) and pyridine (1 .58 g, 20 mmol) in turns with stirring. The reaction mixture was stirred at ambient temperature for 24 hrs under an oxygen atmosphere. The reaction mixture was filtered and filtrate was concentrated. The residue was purified by column chromatography on silica gel(petroleum ether: EtOAc= 3:1) to afford compound Tnt 44-1 (2.74 g). MS-EST (mlz): 321 (M+1) Rf: 0.3 (PE : EtOAc= 3 : 1).

129799-08-2, The synthetic route of 129799-08-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; COBURN, Craig; MALETIC, Milana; LUO, Yunfu; QI, Zhiqi; YU, Tingting; SOLL, Richard; WO2015/70367; (2015); 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.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A 100 mL round-bottom flask was charged with 4-(morpholin-4-yl)-2- (trifluoromethyl)benzaldehyde (1.00 g, 3.86 mmol, 1.00 equiv), tert-butyl (2S)-2- methylpiperazine-l-carboxylate (0.850 g, 4.24 mmol, 1.10 equiv), 1 ,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.40 g, 1 1.3 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with H20 (20 mL), extracted with dichloromethane (3 x 15 mL). The organic layers were combined and washed with brine (50 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was chromatographed on a silica gel column with ethyl acetate/petroleum ether (20/80) to provide 1.70 g (99% yield) of tert- butyl (2S)-2-methyl-4-[[4-(morpholin-4-yl)-2-(trifluoromethyl)phenyl]methyl]piperazine-l- carboxylate as yellow oil. LCMS (ESI, m/z): 444 [M+H]+., 169447-70-5

The synthetic route of 169447-70-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F.; WO2013/103973; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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, General procedure: To amixture of substituted benzoic acid obtained in the last step (0.12 mmol) in 5mL DMF, 2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluroniumhexafluorophosphate (HATU, 0.18 mmol), ethyldiisopropylamine (DIPEA, 0.24 mmol)and 4-((4-methylpiperazin-1-yl)methyl)-3- (trifluoromethyl)aniline (0.1 mmol)was added. The resulting mixture was stirred at room temperature overnight. Thenthe reaction was extracted with ethyl acetate, washed with brine, dried overanhydrous Na2SO4, filtered and concentrated to give thecrude product, which was further purified by column chromatography to affordthe final compounds.

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

Reference：
Article; Han, Mei; Li, Shan; Ai, Jing; Sheng, Rong; Hu, Yongzhou; Hu, Youhong; Geng, Meiyu; Bioorganic and Medicinal Chemistry Letters; vol. 26; 23; (2016); p. 5679 – 5684;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics