Month: August 2020

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.

Compound (e) (222.11 mg, 511.45 muiotaetaomicronIota, 1.5 eq.) was taken in a flask along with DMF as a solvent (approx. 1.5 mL per 1 mmol). (4-((4-methylpiperazin-l- yl)methyl)phenyl)methanamine (70 mg, 340.97 muiotaetaomicronIota, 1 eq.), HOBT (92.14 mg, 681.93 muiotatauiotaomicronIota, 2 eq.), and DIC (93.43 muIota_, 596.69 muiotaetaomicronIota, 1.75 eq.) were added respectively at room temperature and under N2. After 18 hours, the reaction was finished. The solution was quenched with water and then extracted with ethyl acetate. The organic layer was combined and dried with anhydrous MgS04 and concentrated in vacuo. The crude solid was purified through column chromatography using silica gel and eluent ethyl acetate and methanol (up to 2%). The product, 32, was obtained as a brown solid with 51% yield. (0153) FT-IR (Neat) : v (cm”1) = 2941, 2797, 1720, 1634, 1548, 1514, 1451, 1435, 1290, 1275, 1174, 1142, 1112; 1H-NMR (400 MHz, CDCI3) : delta ppm 7.98 (d, J = 9.1 Hz, 2H), 7.33 (s, 1H), 7.25 – 7.30 (m, 2H), 7.21 (d, J = 8.6 Hz, 2H), 6.89 (d, J = 8.6 Hz, 2H), 6.40 (t, J = 4.78 Hz, NH), 4.46 (d, J = 5.54 Hz, 2H), 3.91 (s, 3H), 3.33 (s, 3H), 3.18 – 3.24 (m, 4H), 2.55 – 2.62 (m, 4H), 2.36 (s, 3H) ; 13C-NMR (100 MHz, CDCI3) : delta 166.20, 159.32, 151.02, 144.67, 140.53, 136.40, 130.56, 129.23, 129.05, 127.84, 127.52, 127.33, 126.03 (2C), 116.11 (2C), 115.83 (2C), 55.01 (2C), 52.35 (2C), 48.87, 46.12, 43.76, 30.36; HRMS-ESI (m/z) : calcd. for C26H29BrN405S2 = 621.0763, found = 621.0828.

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference£º
Patent; KING’S COLLEGE LONDON; THURSTON, David Edwin; KHONDAKER, Mirazur Rahman; JAMSHIDI, Shirin; NAHAR, Kazi Sharmin; (77 pag.)WO2019/30538; (2019); A1;,
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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.

[0240] Example 23: Synthesis of 2-[Benzenesulfonyl-(2-chloro-5-trifluoromethyl-phenyl)- amino]-N-[4-(4-methyl-piperazin-l-yl)-benzyl]-acetamide. [0241] To a stirred mixture of 2-(N-(2-chloro-5-(trifluoromethyl)phenyl) phenylsulfonamido)acetic acid (40.3 mg, 0.10 mmol), l-ethyl-3-(3- dimethylaminopropyl)carbodiimide HCl (24.2 mg, 0.13 mmol), and hydroxybenzotriazole (17.6 mg, 0.13 mmol) in methylene chloride (1 mL) was added a solution of (4-(4-methylpiperazin-l- yl)phenyl)methanamine (20 mg, 0.10 mmol) in N,N-dimethylformamide: methylene chloride (0.1 mL : 1 mL). The resulting solution was stirred at room temperature for a week. The mixture was concentrated, purified on silica gel eluted with a gradient of methanol: methylene chloride from 0 : 1 to 1 : 9 to provide the title product (39.2 mg). lU NMR (300 MHz, CDC13): delta 7.64-7.56 (m, 3H), 7.50-7.41 (m, 4H), 7.15-7.12 (m, 1H), 7.11-7.04 (m, 2H), 6.97 (t, = 5.3 Hz, 1H), 6.85-6.78 (m, 2H), 4.30 (d, = 5.3 Hz, 2H), 4.13 (broad s, 2H), 3.18-3.10 (m, 4H), 2.56-2.46 (m, 4H), 2.29 (s, 3H); Calculated for C27H28C1F3N403S, 580.15; observed MS (ESI) (m/z) 581.2 (M + 1)+

As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.

Reference£º
Patent; INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH; CUCONATI, Andrea; GUO, Haitao; BLOCK, Timothy M.; GUO, Ju-Tao; XU, Xiaodong; LU, Huagang; CAI, Dawei; WO2013/130703; (2013); 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.67455-41-8,4-(Piperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of 4-(piperazin-l-yl)aniline (348 mg, 1.968 mmol), (E)-methyl 3-(2-(2-chloropyrimidin-5-yl)vinyl)-5-methoxybenzoate (600 mg, 1.968 mmol) and TFA (672 mg, 5.904 mmol) in propan-2-ol (30 mL) was stirred at 150 C for 40 min under microwave. The resulting mixture was concentrated, basified with ammonia water, purified via ISCO (DCM/MeOH) to afford the title compound as a yellow solid (320 mg, 36.6% yield). MS (m/z): 446.3(M+H)+.

67455-41-8 4-(Piperazin-1-yl)aniline 422925, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; HUTCHISON MEDIPHARMA LIMITED; SU, Wei-Guo; ZHANG, Weihan; LI, Jinshui; WO2014/139465; (2014); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5317-33-9,3-(4-Methylpiperazin-1-yl)propan-1-ol,as a common compound, the synthetic route is as follows.

4-Methyl-l-(hydroxypropyl)-piperazine (0.27 g, 1.7 mmol) and KOH (freshly ground, 0.15 g, 2.7 mmol) were added sequentially to a solution of tert-butyl {[trans-4-({[(2- chloroquinolin-4-yl)carbonyl]amino}methyl)cyclohexyl]-methyl} carbamate (Example 35) (0.15 g, 0.35 mmol) in a mixture of THF (1 mL) and ACN (3 mL). The reaction mixture was heated at 500C for 12h and then DMSO was added and the mixture purified by HPLC (Standard method G). The fractions containing the title compound were partly concentrated in vacuo and then a saturated aq. solution OfNaHCO3 was added. DCM was added and the layers were separated. The organic layer was dried (phase separator) and concentrated in vacuo to give the title compound (90 mg, 47%). 1H NMR (400 MHz, CDCl3) delta 8.05 (d, IH), 7.82 (d, IH), 7.63 (t, IH), 7.40 (t, IH), 6.92 (s, IH), 6.16-6.02 (m, IH), 4.65-4.56 (m, IH), 4.52 (t, 2H), 3.37 (t, 2H), 2.97 (t, 2H), 2.62-2.36 (m, 10H), 2.28 (s, 3H), 2.09-1.96 (m, 2H), 1.91-1.75 (m, 4H), 1.63-1.52 (m, IH), 1.44 (s, 9H), 1.42-1.35 (m, IH), 1.13-0.85 (m, 4H); m/z (M+H)+ 554.1.

The synthetic route of 5317-33-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2009/82346; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

259808-67-8, 1-Boc-3,3-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 21 (200 mg, 0.93 mmol) in CH2C12 (5.0 mL) was charged with TFA (1.0 mL) at 0C. The reaction mixture was stirred at room temperature for 3 h. The reaction mixture was concentrated in vacuo to afford 22 [100 mg (cmde), 94%j as a liquid.

The synthetic route of 259808-67-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IOMET PHARMA LTD.; MERCK SHARP & DOHME CORP.; COWLEY, Phillip, M.; WISE, Alan; BROWN, Thomas, J.; MCGOWAN, Meredeth, A.; ZHOU, Hua; HAN, Yongxin; (223 pag.)WO2017/7700; (2017); 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.

11 g (2.35 g, 10 mmol) was dissolved in a methanol solvent,Under nitrogen protection, 200 mg of Pd / C was added,And then through the H2 reaction,6h after the reaction is complete.The filtrate was collected by filtration, and concentrated to give 1.89 g of a solid. Yield 92%.

The synthetic route of 70261-81-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Nantong University; Ling, Yong; Mou, Jiefei; Xu, Qibing; Feng, Jiao; Zhu, Peng; Liu, Ji; Wang, Tingting; Ge, Xiang; Liang, Shanshan; (26 pag.)CN106432235; (2017); 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.122833-04-9,2-Methoxy-4-(4-methylpiperazin-1-yl)aniline,as a common compound, the synthetic route is as follows.

A mixture of II-l-c (30 mg, 0.12 mmol), 2-methoxy-4-(4-methylpiperazin-l- yl)benzenamine (26.5 mg, 0.12 mmol), X-Phos (5.1 mg), Pd2(dba)3 (6.6 mg) andK2CO3 (49.8 mg, 0.36 mmol) in t-BuOH (1.5 mL) was heated at 100 “C in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The solvent was removed in vacuo and the residue was purified by reverse-phase prep-HPLC using a water (0.05% TFA)/acetonitrile (0.05% TFA) gradient to afford the title compound II-l as TFA salt (19 mg). 1H NMR (600 MHz, CD3OD) delta 7.76 (s, IH), 7.62 (s, br, IH), 6.77 (d, J= 2.4 Hz, IH), 6.67 (dd, J= 2.4, 8.4 Hz, IH), 4.08- 4.06 (m, IH), 3.95-3.85 (m, 6H), 3.77 (dd, J= 8.4, 12.6 Hz, IH), 3.65-3.60 (m, 2H), 3.40-3.25 (m, 5H), 3.15-3.05 (m, 2H), 2.98 (s, 3H), 2.90 (dd, J= 10.8, 14.4 Hz, IH), 2.75 (d, J= 15 Hz, IH), 2.31-2.27 (m, IH), 2.09-2.06 (m, IH), 1.98-1.93 (m, IH), 1.75-1.72 (m, IH). MS (ESI) m/z 438 (M+H)+

122833-04-9 2-Methoxy-4-(4-methylpiperazin-1-yl)aniline 20136253, apiperazines compound, is more and more widely used in various.

Reference£º
Patent; DANA FARBER CANCER INSTITUTE; GRAY, Nathanael, S.; DENG, Xianming; KWIATKOWSKI, Nicholas, Paul; WO2010/80712; (2010); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

154590-34-8, tert-Butyl 4-(2-fluoro-4-nitrophenyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Dissolve the product of Step 2 (2.18 g, 6.7 mmol) in 1:1 CH3OH/EtOAc (40 ml) and add 5% Pd/C (0.50 g). Hydrogenate at 55 psi 1.5 h, filter through Celite and concentrate to obtain the arylamine as a brown oil.

As the paragraph descriping shows that 154590-34-8 is playing an increasingly important role.

Reference£º
Patent; Schering Corporation; US2005/239795; (2005); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

112257-24-6, 1-Boc-3-Carbamoylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1 -benzhydrylazetidin-3 -yl methanesulfonate (2.69 g, 8.5mmol), K2C03 (1.76 g, 12.8 mmol), tert-butyl 3-carbamoylpiperazine-1-carboxylate (1.95 g, 8.5 mmol) in CH3CN (40 mL)was stirred atreflux for 16 h. The mixture was partitioned between ethyl acetate and water. The organic layer was washed with water and brine, dried over Na2SO4, and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel (dichloromethane/methanol = 50:1) to afford the desired product. (2.08 g, 54% yield).

The synthetic route of 112257-24-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARAXES PHARMA LLC; JANES, Matthew, Robert; PATRICELLI, Matthew, Peter; LI, Liansheng; REN, Pingda; LIU, Yi; (397 pag.)WO2016/44772; (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.3022-15-9,Piperazine-2-carboxylic acid dihydrochloride,as a common compound, the synthetic route is as follows.

Step A. To a solution of piperazine-2-carboxylic acid dihydrochloride (10 g, 49 mmol) in 40 ml water was added an aqueous solution of sodium hydroxide (39 ml, 2.5 N). A solution of copper (II) sulfate (6.5 g, 26 mmol) in 80 ml water was added, and the deep blue solution was cooled to 5 C. Sodium bicarbonate (5 g, 59 mmol) was added in one portion, followed by the dropwise addition of benzylchloroformate (7.7 ml, 54 mmol) in 40 ml dioxane over 10 minutes. Sodium bicarbonate was added as needed to maintain a basic solution. The reaction was allowed to warm to rt and was stirred for 16 h. The precipitate was filtered and dried to afford 4-carbobenzyloxypiperazine-2-carboxylic acid, copper chelate residue used directly in the next step.

The synthetic route of 3022-15-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Robichaud, Albert; Mitchell, Ian S.; Lee, Taekyu; Chen, Wenting; US2002/177596; (2002); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics