Month: September 2020

6-Bromophthalazine, cas is 19064-74-5, it is a common heterocyclic compound, the phthalazine compound, its synthesis route is as follows.,19064-74-5

Example 154 Synthesis of 5′-((3-endo)-3-amino-8-azabicyclo[3.2.1]octane-8-carbonyl)-3-fluoro-2′-(phthalazin-6-yl)-[1,1′-biphenyl]-4-carbonitrile The procedure of steps 1 to 5 in Example 41 was conducted using 6-bromophthalazine instead of 1-(4-bromo-3-fluoro-phenyl)-2-methyl-propan-2-ol to give the title compound.

With the rapid development of chemical substances, we look forward to future research findings about 6-Bromophthalazine

Reference£º
Patent; Taiho Pharmaceutical Co., Ltd.; OSADA, Akiko; EP3632443; (2020); A1;,
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

example 2 B (1 eq) dissolved in anhydrous second grade nitrile, then adding to bromine methyl cinnamic acid methyl ester (1 eq) and DIEA (2 eq), under the protection of nitrogen reaction at room temperature 2 hours, the reaction produces a large amount of white precipitate. Slightly static delayed filtering and washing the filter cake to a small amount of acetonitrile, the title compound obtained (white solid, yield 64%).

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; Graduate School at Shenzhen, Tsinghua University; Jiang Yuyang; Yuan Zigao; Gao Chunmei; Chen Shaopeng; (23 pag.)CN106946792; (2017); 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

6-Bromo-2,3-dihydrophthalazine-1 ,4-dione (25. g, 0.10 mol) was added to a mixture of phosphorus oxychloride (100. mL, 1 .06 mol) and thionyl chloride (100. mL, 1 .37 mol) under nitrogen, cooled to 0 C. Once the initial exotherm had subsided the reaction mixture was allowed to warm to ambient temperature and then heated at 100 C for 4 h. The mixture was then cooled to ambient temperature and then concentrated in vacuo. The residue was dissolved in iPrOAc (350 mL) and washed with saturated sodium bicarbonate solution (added until effervescence stopped), a precipitate formed, the two layers were filtered to isolate the first crop of the intermediate. The organic layer was collected and distilled to dryness to give the second crop of the intermediate. The solids were combined and partitioned between 1 ,4-dioxane (200 mL) and 2 N NaOH (100 mL). The resulting mixture was heated at 40 C overnight and then cooled to ambient temperature and left to stand. The solid precipitate was filtered (first crop of product) and the resulting solution partitioned between EtOAc (250 mL) and water (200 mL). Further precipitate formed which was filtered and combined with the first crop of the product, the organic phase was separated and evaporated to dryness to give the second crop of the product. Product isolated is a mixture of two regioisomers, 7-bromo-4-chloro-2H-phthalazin-1 -one and 6- bromo-4-chloro-2H-phthalazin-1 -one, total yield isolated (17.6 g, 68.0 mmol, 66%).1 H NMR (300MHz, DMSO-d6) delta = 13.02 (s, 1 H), 12.98 (s, 1 H), 8.36 (d, J = 2.1 Hz, 1 H), 8.22 (dd, J = 2.1 , 8.6 Hz, 1 H), 8.17 – 8.1 1 (m, 3H), 7.93 (d, J = 8.7 Hz, 1 H). 1 :1 mixture of the two regioisomers.

With the rapid development of chemical substances, we look forward to future research findings about 6-Bromophthalazine-1,4-diol

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; MCGONAGLE, Alison E.; JORDAN, Allan; WASZKOWYCZ, Bohdan; HUTTON, Colin; WADDELL, Ian; HITCHIN, James R.; SMITH, Kate Mary; HAMILTON, Niall M.; (497 pag.)WO2016/92326; (2016); A1;,
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) (0.78 g, 2.13 mmol) was added to a 25 ml three-necked flask.Dichloromethane (6.5 ml) and triethylamine (0.52 g, 5.14 mmol) were added, and the mixture was stirred and cooled to 1-10 C.Further, 2-butenyl chloride (268 mg, 2.56 mmol) was added dropwise, and the mixture was warmed to room temperature and stirred for 1 hour.TLC showed the reaction was complete; the reaction mixture was directly concentrated to dryness, and the residue was mixed with water and then stirred for 1 hour and then filtered.Obtained as an off-white solid.The yield was 37%.

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; Shanghai Bobang Pharmaceutical Technology Co., Ltd.; Gao Heyong; Liu Zhende; Zhang Wensheng; (28 pag.)CN108383798; (2018); A;,
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 -ylcarbonyl) benzyl] phthalazin-1 (2H)-one (IX) (40.0 g, 0.1 1 mol) and 1 H-benzotriazol-1 -yl(cyclopropyl)methanone (X) (26 g, 0.14 mol) were stirred in acetonitrile (320 mL) and the progress of reaction was monitored by HPLC. After completion of reaction, the resulted precipitate was filtered and washed with acetonitrile (40.0 mL) then dried to afford Olaparib (I) as a white to off- white solid. The PXRD pattern of Olaparib thus obtained matches with Form-A as illustrated in figure-3. (Yield: 90%, HPLC purity: 99.99%)

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; ALEMBIC PHARMACEUTICALS LIMITED; SIRIPRAGADA, Mahender Rao; VELISOJU, Mahendar; ANEGONDI, Shreenivasa Prasad; JOSHI, Yogesh Vasant; PANWAR, Amit; PATEL, Malvika; (35 pag.)WO2017/191562; (2017); 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 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.

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

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

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 stirred suspension of NaH (60%, 55 mg, 1.36 mmol) in DMF (5 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; 150.0 mg, 0.68 mmol) in DMF (10 mL) at 0 C. The mixture was heated to 70 C and stirred for 30 min. The mixture was cooled to room temperature, a solution of 4-bromo-l-chloromethyl-2-fluoro-benzene (available from Aldrich; 167.3 mg, 0.75 mmol) in DMF (5 mL) was added and the mixture was stirred for 4 h at room temperature. Aqueous NH4C1 solution was added. The mixture was extracted with EtOAc, and the EtOAc extract was dried, and evaporated. The residue was purified by chromatography (silica gel, 5% EtOAc/hexane) to give 2-(4-bromo-2-fluoro-benzyl)-6-tert-butyl-8-fluoro-2H- phthalazin-l-one (160 mg, 58%) as a white solid. MS calcd. for Ci9Hi8BrF2N20 [(M+H)+] 408, obsd. 408., 1242156-59-7

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,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.763111-47-3,4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.

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%).

763111-47-3 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one 11726399, aphthalazine compound, is more and more widely used in various fields.

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

763111-47-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.763111-47-3,4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.

To the reaction kettle was added 6 L of dichloromethane,4- (4-fluoro-3- (piperazine-1-carbonyl) benzyl) phthalazin-1 (2-hydro) -one (400 g, 1.09 mol)Cooled to 0 C,Triethylamine (153 g, 210 mL, 1.51 mol) was slowly added,Cyclopropanecarbonyl chloride (130 g, 1.24 mol)Stir at room temperature,After TLC detection reaction,Add 3L of water,2L dichloromethane,Dispensing,The organic phase was removed by distillation under reduced pressure,To obtain 320 g of a yellow solid;HPLC purity 96.13%Yield 67.5%.

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

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

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.

Under N2, acetic acid 2,6-dibromobenzyl ester (24.74 g, 80.3 mmol), 6-tert-butyl-8-fluoro-2H-phthazin-1-one (3.54 g, 16.1 mmol), Cs2CO3 (10.46 g, 32.1 mmol), CuI (4.61 g, 24.2 mmol) and N,N-dimethylethane-1,2-diamine (1.42 g, 16.1 mmol) were dissolved in DMF (70 mL). The reaction mixture was stirred at 150 C. for 4 h. The resulting mixture was cooled to room temperature and diluted with ethyl acetate (200 mL), and then 200 mL of water was added. The mixture was separated and the aqueous layer was extracted with ethyl acetate (200 mL¡Á2). The organic layers were combined and washed with water (200 mL) and brine (200 mL). The solution was dried over anhydrous sodium sulfate, filtered and concentrated. The resulting crude product was purified by silica gel chromatography (petroleum ether/ethyl acetate 4/1) to give 2-bromo-6-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-benzyl ester (3.21 g, 45%). 1H NMR (300 MHz, CDCl3): delta 8.17 (d, J=2.7 Hz, 1H), 7.71 (t, J=4.8 Hz, 1H), 7.50-7.45 (m, 2H), 7.36 (s, 1H), 7.34 (d, J=0.9 Hz, 1H), 5.17 (s, 2H), 1.94 (s, 3H), 1.42 (s, 9H). LC-MS calcd for C21H20BrFN2O3 (m/e) 446.06, obsd 447 and 449 [M+1]+., 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; 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