Month: September 2020

7-Bromophthalazin-1(2H)-one, cas is 152265-57-1, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,152265-57-1

Example 807-(4-(trifluoromethoxy)phenyl)phthalazin-1(2H)-one (Compound III-1) A mixture of 7-bromophthalazinone (1.09 g, 4.84 mmol), 4-trifluoromethoxyphenyl boronic acid (1.20 g, 5.81 mmol), dppf(Pd)Cl2 (177 mg, 0.242 mmol), potassium carbonate (1.34 g, 9.68 mmol) in degassed toluene (4 mL), degassed water (2 mL) and degassed isopropanol (2 mL) was heated at 90 C. for 12 hours. The layers were separated, the organic layer was concentrated and the residue was purified by trituration with hexanes/ethyl acetate to provide 7-(4-(trifluoromethoxy)phenyl)phthalazin-1(2H)-one as a white powder. C15H9F3N2O2. 307.2 (M+1).

152265-57-1 is used more and more widely, we look forward to future research findings about 7-Bromophthalazin-1(2H)-one

Reference£º
Patent; Gilead Sciences, Inc.; US2012/289493; (2012); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.75884-70-7,6-Bromophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.,75884-70-7

Step 3. 6-vinylphthalazine-1(2H)-one (BI27); A solution of 6-bromophthalazine-1(2H)-one (0.25 g, 1.11 mmol), potassium vinyl trifluoroborate (0.446 g, 3.33 mmol) and K2CO3 (0.46 g, 3.33 mmol) in DMSO (2 mL) was degassed with argon for 20 min at RT. PdCl2(dppf) (0.04 g, 0.055 mmol) was added at RT, and the reaction mixture was heated to 80 C. for 2 h. The reaction mixture was cooled to RT and filtered through celite bed under vacuum and washed with ethyl acetate. The reaction mixture was extracted with ethyl acetate and the combined ethyl acetate layer dried over Na2SO4 and concentrated under reduced pressure to afford the crude product. The crude compound was purified by column chromatography (SiO2, 100-200 mesh; 50% ethyl acetate/petroleum ether) to afford the title compound as a brown solid (0.12 g, 63%): 1H NMR (400 MHz, DMSO-d6) delta 13.61 (br, 1H), 8.33 (m, 1H), 8.19 (m, 1H), 8.01 (m, 2H), 6.97 (m, 1H), 6.15 (m, 1H), 5.56 (d, J=10.8 Hz, 1H); ESIMS m/z 172.93 ([M+H]+); IR (thin film) 1748, 1655, 3241 cm-1.

The synthetic route of 75884-70-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hunter, James E.; Lo, William C.; Watson, Gerald B.; Patny, Akshay; Gustafson, Gary D.; Pernich, Dan; Brewster, William K.; Camper, Debra L.; Lorsbach, Beth; Loso, Michael R.; Sparks, Thomas C.; Joshi, Hemant; Mandaleswaran, Adiraj; Sanam, Ramadevi; Gundla, Rambabu; Iyer, Pravin S.; US2012/329649; (2012); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.152265-57-1,7-Bromophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.

Example 807-(4-(trifluoromethoxy)phenyl)phthalazin-1(2H)-one (Compound III-1) A mixture of 7-bromophthalazinone (1.09 g, 4.84 mmol), 4-trifluoromethoxyphenyl boronic acid (1.20 g, 5.81 mmol), dppf(Pd)Cl2 (177 mg, 0.242 mmol), potassium carbonate (1.34 g, 9.68 mmol) in degassed toluene (4 mL), degassed water (2 mL) and degassed isopropanol (2 mL) was heated at 90 C. for 12 hours. The layers were separated, the organic layer was concentrated and the residue was purified by trituration with hexanes/ethyl acetate to provide 7-(4-(trifluoromethoxy)phenyl)phthalazin-1(2H)-one as a white powder. C15H9F3N2O2. 307.2 (M+1)., 152265-57-1

As the paragraph descriping shows that 152265-57-1 is playing an increasingly important role.

Reference£º
Patent; Gilead Sciences, Inc.; US2012/289493; (2012); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO271,mainly used in chemical industry, its synthesis route is as follows.,763111-47-3

4-[[4-Fluoro-3-(piperazine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one (11) (86 mg, 0.24 mmol), HBTU (116 mg, 0.30 mmol) and triethylamine (164 muL, 1.18 mmol) were added to a solution of 2-hydroxyacetic acid (36 mg, 0.48 mmol) in DMF (1.5 mL) and the reaction mixture was stirred at room temperature for 40 minutes, before dichloromethane (4 mL) and water (4 mL) were added, the organic phase separated and washed with NaOH (0.2 M, 3*4 mL) and water (3*4 mL). The organic phase was dried over MgSO4, volatiles were removed in vacuo and the resulting crude material was purified via HPLC, yielding the title compound as a clear solid (24.3 mg, 0.06 mumol, 50%).

With the synthetic route has been constantly updated, we look forward to future research findings about 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one,belong phthalazine compound

Reference£º
Patent; THE GENERAL HOSPITAL CORPORATION; Reiner, Thomas; Keliher, Edmund J.; Weissleder, Ralph; US2013/309170; (2013); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

75884-70-7, 6-Bromophthalazin-1(2H)-one is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,75884-70-7

Step a 6-Bromo-2-(3-carboxypropyl)phthalazin-1(2H)-one To a slurry of 56 gm 6-bromophthalazin-1(2H)-one (0.25 mole) in 600 ml DMSO was added 110 ml 45% KOH followed by 58.5 gm ethyl 4-bromobutyrate. The temperature of the mildly exothermic reaction was moderated with a water bath (ca. 25C) and was stirred for 20 hours. Ethanol (750 ml) was added, then the mixture was acidified with 125 ml concentrated HCl, diluted with 2500 ml water over about 30 minutes, stirred an additional 30 minutes, filtered, washed with water and isopropanol and dried. The product weighed 63.6 g. A tlc of the product showed product, Rf = 0.43 plus a trace of starting material, Rf = 0.63.

75884-70-7 6-Bromophthalazin-1(2H)-one 11535918, aphthalazine compound, is more and more widely used in various.

Reference£º
Patent; FISONS CORPORATION; EP309765; (1990); A3;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,763111-47-3

A QMA cartridge containing cyclotron -produced [18F] fluoride ion was euted with a solution containing 9 mg Kryptofix [2.2,2] (4,7.13, 16,21,24- hexaoxa- l,10-diaza bicycloi8.8.8]hexacosane), 0.08 m L 0.15 M K2C03 and 1.92 m L MeCN into a 5 m L reaction vial. Water was removed azeotropically at 120 C. 500 mug of ethyl 4-nitrobenzoate dissolved in 100 mu of DMSO was then added to the reaction vial and heated to 150 C for 15 minutes. The reaction via l was then allowed to cool as 50 mu of 1M NaOH was added. The reaction mixture was stirred for 1 min and 50 mu of 1M HCI was added to quench. Then, 2 mg of 4-(4-fiuoro-3-(piperazine-l-carbonyl)benzyi)phthaiazin- l(2H)-one dissolved in 100 mu of DMSO was added , followed by 10 mg of HBT U dissolved in 100 mu of DMSO and 20 mu. of Et3N. The reaction mixture was stirred for 1 minute. 400 mu MeCN followed by 700 mu H20 was then added and the solution was injected onto a C6-Pheny analytical HPLC column and eluted under isocratic conditions (Method B: 30% acetonitrile in water for 35min). Compound C- 2f eluted at (tR = 25.5 min), which was well resolved from the nitro analogue (4-(4-fluoro-3-(4-(4- nitrobenzoyl)piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one; tR = 30.1 min). For intravenous administration, the product-containing fraction was passed through a CIS light-SepPak cartridge preconditioned with EtOH (10 m L) and water (10 mL). The cartridge was washed with water (3 m L) and C-2f was eluted using EtOH (400 mu). The solution was then diluted with 0.9% saline to 10% EtOH. The radiochemical purity of the final formulation was confirmed using analytical HPLC.

With the rapid development of chemical substances, we look forward to future research findings about 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

Reference£º
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; REINER, Thomas; LEWIS, Jason S.; WEBER, Wolfgang; RODRIGUEZ, Beatriz Salinas; CARNEY, Brandon; CARLUCCI, Giuseppe; (89 pag.)WO2016/33293; (2016); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

5-Nitrophthalazine, cas is 89898-86-2, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,89898-86-2

To 0.88g (5.0mmol) of 5-nitrophthalazine in 30mL of tetrahydrofuran at 50C was added 4.37g (25.1mmol) of sodium hydrogen sulfite in 15mL of water. The reaction mixture was stirred at 50C for 15min. The organic solution was extracted with ethyl acetate (3¡Á100mL), washed with brine (50mL), and dried over magnesium sulfate. Filtration and removal of the solvent under reduced pressure gave the product as a bright yellow precipitate. The precipitate was recrystallized in a hot methanol solution to afford 0.49g (67%) of 5-aminophthalazine. 1H NMR (400MHz, DMSO-d6) delta: 9.80 (s, 1H), 9.60 (s, 1H), 7.60 (dd, J=4. 6, 7.6Hz, 1H), 7.20 (dd, J=1.9, 4.6Hz, 1H), 7.02 (d, J=7.6Hz, 1H), 6.50 (s, 2H). 13C NMR (100.17MHz, DMSO-d6) delta: 150.1, 146.5, 145.1, 133.2, 126.1, 114.7, 114.1, 112.2.

With the rapid development of chemical substances, we look forward to future research findings about 5-Nitrophthalazine

Reference£º
Article; Paige, Mikell; Kosturko, George; Bulut, Guellay; Miessau, Matthew; Rahim, Said; Toretsky, Jeffrey A.; Brown, Milton L.; Ueren, Aykut; Bioorganic and Medicinal Chemistry; vol. 22; 1; (2014); p. 478 – 487;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,763111-47-3

4-(4-Fluoro-3-(piperazin-1-yl-carbonyl)-benzyl)pyridazine-1(2H)one (5) (1.56 g, 4.26 mmol) was added to a 25 ml three-necked flask.And added dichloromethane (6.5 ml), trans-4-dimethylamino crotonic acid (0.78 g, 6.04 mmol),HOBT (0.87 g, 6.44 mmol), EDCI (1.23 g, 6.42 mmol), and then cooled to 0-10 C, then DIPEA (4.42 g, 34.3 mmol) was added dropwise, and the mixture was allowed to warm to room temperature and stirred for 2 h.After TLC showed that the reaction was completed, the reaction mixture was quenched with water (30 mL).The solid crude product was added to the acid water, the impurities were extracted with dichloromethane, the aqueous phase was made alkaline, and the product was extracted with dichloromethane (20 mL¡Á3);The combined organic phases were dried over anhydrous sodium sulfate, filtered and evaporatedThe white solid product was then beaten with n-hexane (5 ml).Filter and dry to give 470 mg of a white solid.The yield was 23%.

As the rapid development of chemical substances, we look forward to future research findings about 763111-47-3

Reference£º
Patent; Shanghai Bobang Pharmaceutical Technology Co., Ltd.; Gao Heyong; Liu Zhende; Zhang Wensheng; (28 pag.)CN108383798; (2018); A;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

6-Bromophthalazine-1,4-diol, cas is 76240-49-8, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,76240-49-8

To a solution of 6-bromo-2,3-dihydrophthalazine-1,4-dione (CAS 76240-49-8, 36.0 g, 150 mmol) and Et3N (37.5 g, 375 mmol) in DCM (1.0 L) was added Tf20 (42.3 g, 150 mol) dropwise over 1 h. The mixture was stirred at 0 C for 2 h and then kept at 15 C for 16 h. The mixture was filtered and the filtrate was concentrated. The residue was purified by flash column(petroleum ether: EtOAc from 5:1 to 3:1) to give a mixture of the title compounds (9.0 g, 16% yield) as a white solid.

As the rapid development of chemical substances, we look forward to future research findings about 76240-49-8

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CUMMING, John G.; LIN, Xianfeng; LIU, Haixia; NAJERA, Isabel; QIU, Zongxing; SANDRIN, Virginie; TANG, Guozhi; WU, Guolong; (204 pag.)WO2018/1948; (2018); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

Name is 6-Bromophthalazin-1(2H)-one, as a common heterocyclic compound, it belongs to phthalazine compound, and cas is 75884-70-7, its synthesis route is as follows.,75884-70-7

To a suspension of 6-bromophthalazine-l-(2H)-one (563 mg, 2.5 mmol) in DMF (25 mL) under an argon atmosphere was added sodium hydride (140 mg of 60% oil dispersion, 3.5 mmol) and the resulting mixture was allowed to stir at room temperature for 15 min. before addition of (2-(chloromethoxy)ethyl)trimethylsilane (0.53 mL, 3 mmol). The reaction mixture was stirred at room temperature overnight, then poured onto water and ether and extracted with ether (3X). The combined organic layer was washed with water, then brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The resulting residue was slurried in DCM and filtered. The solid was washed with DCM. The combined filtrate and wash was purified by chromatography to provide 6-bromo-2-((2-(trimethylsilyl)ethoxy)methyl)phthalazin-l(2H)-one (625 mg, 70% yield) as a white solid. NMR (300 MHz, Chloroform-^ delta 8.37 – 8.29 (m, 1H), 8.12 (s, 1H), 7.93 – 7.85 (m, 2H), 5.57 (s, 2H), 3.84 – 3.62 (m, 1H), 1.10 – 0.89 (m, 1H), 0.01 (s, 9H).

With the complex challenges of chemical substances, we look forward to future research findings about 6-Bromophthalazin-1(2H)-one

Reference£º
Patent; UNIVERSITY OF HAWAII; TURKSON, James; YUE, Peibin; TIUS, Marcus; BROTHERTON-PLEISS, Christine; LOPEZ TAPIA, Francisco, Javier; (420 pag.)WO2018/136935; (2018); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem