Category: phthalazine

Name is 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one, as a common heterocyclic compound, it belongs to phthalazine compound, and cas is 1242156-59-7, its synthesis route is as follows.,1242156-59-7

To a 3 L round bottom flask were added 6-tert-butyl-8-fluoro-2H-phthalazin-1-one (132.3 g, 0.6 mol), 2-chloro-6-fluorobenzaldehyde (104.8 g, 0.66 mol) and cesium carbonate (117.4 g, 0.36 mol). The flask was evacuated and backfilled with Nitrogen three times. Then, ethoxytrimethylsilane (142 g, 1.2 mol) and DMF (1.6 L) were added to the reaction flask, and the resulting mixture was heated to 60 C. After 4 h stirring, the solution was allowed to cool down to ambient temperature and the reaction was quenched by addition of 800 mL of H2O dropwise. The desired product started to precipitate from DMF and water mixture. The solid was collected by filtration after cooling down to 5 C., and washed with DMF/water (2/1, 750 mL, pre-cooled to 6 C.) and H2O (400 mL). The filter cake was dried under vacuum oven at 65 C. overnight to afford 147 g of the title compound (68.2% isolated yield) as a yellow solid. MS (ESI) 358, 360 (M+H)-.

With the complex challenges of chemical substances, we look forward to future research findings about 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one

Reference£º
Patent; Berthel, Steven; Firooznia, Fariborz; Fishlock, Daniel; Hong, Jun-Bae; Lou, Yan; Lucas, Matthew; Owens, Timothy D.; Sarma, Keshab; Sweeney, Zachary Kevin; Taygerly, Joshua Paul Gergely; US2010/222325; (2010); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

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

General procedure: Intermediates 8 (1 eq) and respective 9-chloroacridine derivatives 4a-4f (1.1 eq) were added to a round flask, and then excessphenol was added as solvent. The reaction system was warmed up to 60 C until phenol was melted and stirred for 0.5 h under argonprotection. Then the mixture was warmed up to 120 C and continued to reaction for more 2 h. After the reaction was completed, themixture was added to ethyl ether drop by drop [2]. The precipitate was filtered and washed twice with new ethyl ether to give pureproducts 9a-9f, which were then characterized by 1H NMR, 13C NMR, melting point and high resolution mass spectrum (HRMS, ESI).

With the complex challenges 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
Article; Dai, Qiuzi; Chen, Jiwei; Gao, Chunmei; Sun, Qinsheng; Yuan, Zigao; Jiang, Yuyang; Chinese Chemical Letters; vol. 31; 2; (2020); p. 404 – 408;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

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

EXAM PLE A.2. Compound c-1 (127l): 4-(4-fluoro-3-(4-(3-iodobenzoyl)piperazine-l-carbonyl)benzyl)- phthalazin-l(2H)-one. (0301) [0148] To a solution of 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one (10 mg, 0.0275 mmol), triethylamine (40 mu, 0.3 mmol) a nd H BTU (16 mg, 0.0413 mmol) in dimethyl formamide (DM F, 500 mu) was added to 3-iodobenzoic acid (6 mg, 0.0275 mmol). The mixtu re was stirred at room temperature for 20 h. The crude product was then purified by preparative HPLC and dried under vacuum, yielding a white solid (6.9 mg, 48% yield). 1H NM R (CDCIs) delta = 10.00 (s, 1H), 8.40-8.38 (m, 1H), 7.71-7.69 (m, 4H), 7.64-7.63 (m, 1H), 7.30-7.26 (m, 3H), 7.09 (m, 1H), 7.04-6.87 (m, 1H), 4.21 (s, 2H), 3.71-3.29 (m, 8H). LC-ESI-MS (+) m/z = 597.1 [M+H+]+. H RMS-ESI [M-H+]” m/z calculated for [C27H22FIN4O3]- 595.0642, found 595.0660.

With the complex challenges 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

1242156-59-7, 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 109a 3-Bromo-5-(6-tert-butyl-8-fluoro-1-oxo-1,2-dihydrophthalazin-2-yl)pyridine-4-carbaldehyde 109a A sealed tube equipped with a magnetic stirrer was charged with 6-tert-butyl-8-fluoro-1,2-dihydrophthalazin-1-one 101h (220 mg, 1.0 mmol), 3,5-dibromopyridine-4-carbaldehyde (530 mg, 2.0 mmol), CuI (190 mg, 1.0 mmol), 4,7-dimethoxy-1,10-phenanthroline (244 mg, 1.0 mmol), Cs2CO3 (652 mg, 2.0 mmol) and dioxane (8 mL). After three cycles of vacuum/argon flush, the mixture was heated at 110 C. for 5 h. It was then filtered and the filtrate was evaporated in vacuo. The residue was purified by silica gel column chromatography eluting with ethyl acetate/petroleum ether (1:3, V/V) to afford 109a (118 mg, 29.3%) as a solid. LCMS: [M+H]+ 406, 1242156-59-7

1242156-59-7 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one 59473765, aphthalazine compound, is more and more widely used in various fields.

Reference£º
Patent; GENENTECH, INC.; Crawford, James John; Ortwine, Daniel Fred; Wei, BinQing; Young, Wendy B.; US2013/116246; (2013); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

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

At 50 C,To the reaction kettle by adding N, N-dimethylacetamide 2000ml,Was added with stirring 4- (4-fluoro-3- (piperazine-1-carbonyl) benzyl) -1-naphthyridine (2-hydro) – one (40g, 0.109mol),HATU (48 g, 0.126 mol),Cyclopropanecarboxylic acid (12 g, 0.139 mol)Finally, N, N-diisopropylethylamine (0.218 mol, 28.17 g, 38 ml) was added,30 C for 6 hours,Add 800ml of water,Slowly precipitate solid,Filter,washing,dry,To give 44 g of a white solid,That is,HPLC purity 99.87%Yield 92.8%.

With the complex challenges 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; Sichuan Kelun Drug Research Institute Co., Ltd.; Li, Hongming; Wu, Wei; Tuo, Shichuan; Wang, Lichun; Wang, Jingyi; (8 pag.)CN105985294; (2016); A;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

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

4-[[4-Fluoro-3-(piperazine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one (11) (250 mg, 0.68 mmol), HBTU (337 mg, 0.89 mmol) and triethylamine (285 muL, 1.18 mmol) were added to a solution of 6-hydroxyhexanoic acid (180 mg, 1.36 mmol) in DMF (3.0 mL) and the reaction mixture was stirred at room temperature for 60 minutes, before dichloromethane (8 mL) and water (8 mL) were added, the organic phase separated and washed with water (3*8 mL). The organic phase was dried over MgSO4, volatiles removed in vacuo and the resulting crude material purified via HPLC, yielding the title compound as a clear solid (55.6 mg, 0.12 mmol, 17%).

With the complex challenges 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; THE GENERAL HOSPITAL CORPORATION; Reiner, Thomas; Keliher, Edmund J.; Weissleder, Ralph; US2013/309170; (2013); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

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

The dried radiola beled 131l-N HS-benzoate precursor was dissolved in 200 mu of acetonitrile and an excess of H BTU (1 mg, 2.6 nmol) and 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)phthalazin- l(2H)-one (1 mg, 2.7 nmol) was added and allowed to react for 3 h at 32 C. The final product was purified by H PLC, using water and acetonitrile as solvents with a gradient elution from 5% to 100% of solvent B over 15 min and then 100% of B from 15 to 25 min. The retention time of C-2d was 13.1 min and its identity was esta blished by co-elution with the reference cold compound. The radiochemical yield was 72 ¡À 8 % (n=12) and the radiochemical purity > 95%. The collected fraction containing C-2d was concentrated to dryness under reduced pressure

With the complex challenges 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

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

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 ambient temperature. PdCl2(dppf) (0.04 g, 0.055 mmol) was added at ambient temperature, and the reaction mixture was heated to 80 C. for 2 h. The reaction mixture was cooled to ambient temperature 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.

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

Reference£º
Patent; Dow AgroSciences LLC; Lo, William C.; Hunter, James E.; Watson, Gerald B.; Patny, Akshay; Iyer, Pravin S.; Boruwa, Joshodeep; US9211280; (2015); B2;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

6-Amino-2,3-dihydrophthalazine-1,4-dione, cas is 3682-14-2, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,3682-14-2

Example 334: Preparation of 6-((4-(cyclopropyIamino)-5-(trifluoromethyl)pyrimidin-2- yl)amino)-2,3-dihydrophthalazine-l,4-dione2-Chloro-N-cyclopropyl-5-(trifluoromethyl)pyrimidin-4-amine (0.055 g, 0.231 mmol) and 6-amino-2,3-dihydrophthalazine-1 ,4-dione (0.041 g, 0.231 mmol) were mixed in acetic acid (2 ml). The mixture was microwaved at 1 10 ¡ãC for 20 min and then concentrated. Added MeOH and 5percent DMF and filtered the solid to give 35 mg of product. MS calcd for [Ci6H13F3N602+H]+: 379.12, found 379.00.

3682-14-2 is used more and more widely, we look forward to future research findings about 6-Amino-2,3-dihydrophthalazine-1,4-dione

Reference£º
Patent; SALK INSTITUTE FOR BIOLOGICAL STUDIES; SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE; YALE UNIVERSITY; SHAW, Reuben J.; EGAN, Daniel F.; COSFORD, Nicholas; TURK, Benjamin; VAMOS, Mitchell; PANICKAR, Dhanya Raveendra; CHUN, Matthew; SHEFFLER, Doug; (315 pag.)WO2016/33100; (2016); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one, cas is 1242156-59-7, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,1242156-59-7

To a 100 mL round bottom flask series added compound 4-1 (1.77 g, 8.04 mmol), commercially available starting material 4-2 (1.40 g, 8.84 mmol) and cesium carbonate (1.90 g, 4.82 mmol). The flask was evacuated and back filled with nitrogen three times. Then ethoxytrimethylsilane (1.90 g, 16.07 mmol) and DMF (20 mL) were added to the reaction flask, and the resulting mixture was heated 62C. After 5 h stirring, the solution was allowed to cool down to ambient temperature and the reaction was quenched by addition 20 mL of water. The desired product started to precipitate from DMF and watermixture. The solid was collected by filtration after cooling down to 5C, and washed with water. The filter cake was dried under vacuum oven at 50C to afford crude compound 3 (2.88 g, yield:99.8%) as a light yellow solid which was used for next step without purification.

1242156-59-7 is used more and more widely, we look forward to future research findings about 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one

Reference£º
Patent; CHEN, Yi; WO2015/50703; (2015); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem