Category: phthalazine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1021298-68-9,2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzonitrile,as a common compound, the synthetic route is as follows.

Preparation of 2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid To the mixture of 2-fluoro-5-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrile (1.2 g, 4.5 mmol) in water (6.5 ml) was added aqueous sodium hydroxide (0.84 g in 1.6 ml of water) drop-wise, then heated at 90 for 1 h. After cooled to 70, hydrazine hydrate (6.4 ml) was added and the reaction mixture was heated at 70 for overnight. Then the reaction mixture was cooled to room temperature, and adjusted to PH 3-4 by adding aqueous HCl (2N). The precipitated solid was collected by filtration, washed with water, and dried in vacuo to afford the target compound (0.9 g, 70%) as a pink solid, used in next step without further purification. m/z [M-1]- 296.90 1HNMR (DMSO-d6): delta 13.22 (1H, brs), 12.61 (1H, s), 8.27 (1H, m), 7.99-7.81 (4H, m), 7.59 (1H, m), 7.25 (1H, m), 4.36 (2H, s)

As the paragraph descriping shows that 1021298-68-9 is playing an increasingly important role.

Reference£º
Patent; SHANGHAI DE NOVO PHARMATECH CO LTD.; Gao, Daxin; US2013/224107; (2013); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

253-52-1, Phthalazine is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1A1,2-phenylenedimethanamine[0168]Phthalazine (21.5 g, 0.165 mol), 10percent palladium on carbon (2 g), and methanol (125 mL) were combined in a pressure bottle and shaken at room temperature under 60 psi of hydrogen for 5 days. Raney-nickel? slurry (6.42 g) and 10percent palladium on carbon (0.50 g) were added, and the mixture was shaken at 50¡ã C. under 60 psi of hydrogen for 16 hours. The mixture was filtered through a nylon membrane and concentrated to give the titled compound: 1H NMR (300 MHz, DMSO-d6) delta ppm 7.32 (dd, J=5.4, 3.5 Hz, 2H), 7.17 (dd, J=5.6, 3.4 Hz, 2H), 3.74 (s, 4H); MS (DCI/NH3) m/z 137 (M+H)+.

As the paragraph descriping shows that 253-52-1 is playing an increasingly important role.

Reference£º
Patent; AbbVie Inc.; Cowart, Marlon D.; Liu, Huaqing; Altenbach, Robert; US2013/40940; (2013); 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

To a suspension of NaH (60%>, 145 mg, 3.63 mmol) in DMF (3 mL) was added dropwise a solution of 6-tert-butyl-8-fluoro-2H-phthalazin-l-one (which may be prepared as described in Berthel, S. et al. US 20100222325 Column 139; 400.0 mg, 1.82 mmol) in DMF (2 mL) at 0 C. The mixture was stirred at room temperature for 5 min and then heated at 70 C for 30 min. The mixture was cooled to room temperature, a solution of l-bromo-4-bromomethyl-2- methoxymethoxymethyl-benzene (684 mg, 2 mmol) in DMF (2 mL) was added and the mixture was stirred for 4 h at room temperature. Water (5 mL) was added, and the mixture was extracted with EtOAc (3 x 20 mL). The combined organic layers were washed with water (3 x 5 mL) and brine (5 mL), dried (Na2S04), filtered, and evaporated. The residue was purified by chromatography (silica gel, 12% EtOAc/hexane) to give 2-(4-bromo-3-methoxymethoxymethyl- benzyl)-6-tert-butyl-8-fluoro-2H-phthalazin-l-one (230 mg, 27%) as a yellow gum. MS calcd. for C22H25BrFN203 [(M+H)+] 463, obsd. 462.8.

As the paragraph descriping shows that 1242156-59-7 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; DOMINIQUE, Romyr; LOPEZ-TAPIA, Francisco Javier; MERTZ, Eric; SO, Sung-Sau; WO2014/76104; (2014); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

763111-47-3, 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE A.6. Compound c-5 (127l): 4-(4-fluoro-3-(4-(3-(3-iodophenyl)propanoyl)piperazine-1-carbonyl)benzyl)phthalazin-l(2H)-one. A solution of 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one (10 mg, 0.0275 mmol), HBTU (16 mg, 0.0413 mmol) triethylamine (40 mu, 0.3 mmol) and 3-(3-iodophenyl)propionic acid (7.6 mg, 0.0275 mmol) in 400 mu of acetonitrile was stirred overnight at room temperature. The crude product was then purified by preparative HPLC and the isolated product dried at vacuum to obtain a white solid (5.1 mg, 38%). 1H NMR (CDCI3) delta = 10.33 (s, 1H), 8.41-8.39 (d, 1H), 7.71-7.63 (m, 3H), 7.51-7.45 (m, 2H), 7.27-7.25 (m, 2H), 7.12-6.92 (m, 3H), 4.22 (s, 2H), 3.65-3.12 (m, 8H), 2.88- 2.83 (m, 2H), 2.59-2.48 (m, 2H). LC-ESI-MS (+) m/z = 647.1 [M+Na+]+. HRMS-ESI [M+H+]+ m/z calculated for [C29H26FIN403 625.1112, found 625.1111.

As the paragraph descriping shows that 763111-47-3 is playing an increasingly important role.

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

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

A dry 2-neck flask was evacuated and backflushed with argon (3X). Sodium t-butoxide (360 mg, 3.75 mmol), 6-bromophthalazin-l(2H)-one (338 mg, 1.5 mmol), (4-cyclohexylphenyl)methanamine (340 mg, 1.8 mmol), (+/-)BINAP (280 mg, 0.45 mmol) and Pd2(dba)3 (137 mg, 0.15 mmol) were added to the flask. Toluene (30 mL) was then added and the mixture was degassed with stirring under vacuum and backflushed with argon (3X). The reaction mixture was stirred at reflux for 3 hours and then allowed to cool to room temperature. The reaction mixture was poured onto water and EtOAc and extracted with EtOAc (3X) and then extracted with DCM (2X). The combined organic extract was washed with brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The crude residue was slurred in DCM and filtered and the solid cake washed several times with DCM. The combined filtrate and washes were concentrated in vacuo to provide crude product, 6-((4-cyclohexylbenzyl)amino)phthalazin-l(2H)-one, as an off-white powder (118 mg).

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

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1242156-59-7,6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.

To a stirred solution of 6-tert-butyl-8-fluoro-2H-phthalazin-l-one (which may be prepared as described in Berthel, S. et al. US 20100222325 Column 139; 100 mg, 0.45 mmol) in DMF (5 mL) were added 2-bromo-6-fluoro-benzaldehyde (available from Aldrich; 101.5 mg, 0.5 mmol), cesium carbonate (325 mg, 0.27 mmol) and methoxytrimethylsilane (0.1 mL, 0.91 mmol). The mixture was heated at 60 C for 4 h, then cooled to room temperature and diluted with water (25 mL). The resulting mixture was extracted with ethyl acetate, dried (Na2S04), filtered, and evaporated. The residue was purified by chromatography (silica gel, 10% EtOAc/hexane) to give 2-bromo-6-(6-tert-butyl-8-fluoro-l-oxo-lH-phthalazin-2-yl)-benzaldehyde (105 mg, 57%) as a yellow gum. MS calcd. for Ci9Hi7BrFN202 [(M+H)+] 404, obsd. 404.

The synthetic route of 1242156-59-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; DOMINIQUE, Romyr; LOPEZ-TAPIA, Francisco Javier; MERTZ, Eric; SO, Sung-Sau; WO2014/76104; (2014); 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

In a 50 mL pear-shaped flask, 6-bromophthalazin-l(2H)-one (214 mg, 951 muiotaetaomicron, Eq: 1.00) and CS2CO3(372 mg, 1.14 mmol, Eq: 1.20) were combined with DMF (3 ml) to give a light brown suspension. Methyl iodide (202 mg, 89.0 mu, 1.43 mmol, Eq: 1.50) was added and the reaction mixture was stirred at 25 C for 20 h. The reaction was diluted with dichloromethane and water. The aqueous layer was back-extracted with dichloromethane (3 x 20 mL). The combined organic layers were washed with H20 (1 x 25 mL), dried over Na2S04and concentrated in vacuo. The crude material was recrystallized from dichloromethane to give a light yellow solid. The solid was dried under vacuum to afford 112 mg (49%) of the desired product as a light yellow crystalline solid.MS +m/z: 239/241 (M+l)

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

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHEN, Zhi; CHIN, Elbert; ERICKSON, Shawn David; GABRIEL, Stephen Deems; MERTZ, Eric; WEIKERT, Robert James; WO2014/135483; (2014); 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

Step 2. In a 25 mL container, 1-(3-bromo-2-formylphenyl)-1H-pyrazole-4-carbonitrile (100 mg, 362 mumol, Eq: 1.00), 6-tert-butyl-8-fluorophthalazin-1(2H)-one (160 mg, 724 mumol, Eq: 2) and copper (I) iodide (138 mg, 724 mumol, Eq: 2.00) were combined with DMSO (2.00 ml) to give a yellow suspension. Sodium bicarbonate (76.1 mg, 906 mumol, Eq: 2.5) was added to it. The mixture was heated in a microwave at 120 C. for 1 hr. The reaction mixture was poured into 25 mL sat NH4Cl and extracted with EtOAc (3¡Á25 mL). The organic layers were dried over MgSO4 and concentrated in vacuo. The organic layer was concentrated and purified through ISCO flash column chromatography using ethyl acetate (containing 5% methanol) in hexanes (5% to 80% linear gradient in 15 minutes, 24 g silica gel) to give the pure desired product which was triturated with ether in hexanes and filtered to obtain 1-[3-(6-tert-Butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-2-formyl-phenyl]-1H-pyrazole-4-carbonitrile (110 mg, 73%).

The synthetic route of 1242156-59-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Billedeau, Roland Joseph; Kondru, Rama K.; Lopez-Tapia, Francisco Javier; Lou, Yan; Owens, Timothy D.; Qian, Yimin; So, Sung-Sau; Thakkar, Kshitij C.; Wanner, Jutta; US2012/295885; (2012); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

3682-14-2, 6-Amino-2,3-dihydrophthalazine-1,4-dione is a phthalazine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 400 mg (1.44 mM) of 4-chloro-6,7-diethoxy-quinoline-3-carbonitrile and 273 mg (1.54 mM) of 4-Aminophthalhydrazide Hydrate in 15 ml of 2-methoxyethanol was refluxed for 3 hours. To the warm solution was added 1 ml of 1M sodium carbonate and the sample was heated for 5 minutes at 100C, then poured into 300 ml of ice water. The solution was made acetic by addition of concentrated HCl and the solid was collected, washed with water followed by ether and dried under vacuum at 80C. The solid was taken up into 200 ml of methanol and 500l of 5 N sodium hydroxide and boiled for 20 minutes. To this heterogeneous mixture was added 100 ml of glacial acetic acid and the volume was reduced to a total of 100 ml by boiling. To the room temperature mixture, 500 ml of ice cold water was added and the solid was collected, washed with water followed by ether and dried under vacuum at 80C. The solid was digested in 400 ml of ethanol until the volume had been reduced to 150 ml. The hot solution was filtered and the solid was washed with ethanol and to dried under vacuum at 80C yield 121 mg of the title compound as a white solid: mass spectrum (electrospray, m/e): M+H 418.0, mp = >270C.

3682-14-2 6-Amino-2,3-dihydrophthalazine-1,4-dione 95014, aphthalazine compound, is more and more widely used in various.

Reference£º
Patent; Wyeth Holdings Corporation; EP1117659; (2003); B1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem