Category: 763111-47-3

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

(c) 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one (A)To a stirred suspension of compound B (1290 g) in CH2CI2 (15480 ml) under nitrogen was added a pre-mixed solution of triethylamine (470 ml) and cyclopropane carbonyl chloride (306 ml) in CH2CI2 (1290 ml) dropwise with the temperature kept below 2O0C. The solution was then stirred at 10-15C for 15 minutes and sampled for completion. The reaction mixture was found to contain only 1.18% of starting material B and so the reaction was deemed complete and the batch was then worked-up.The reaction mixture was washed with water (7595 ml), 5% citric acid solution (7595 ml), 5% sodium carbonate solution (7595 ml) and water (7595 ml). The organic layer was then dried over magnesium sulfate (50Og).The CH2CI2 containing product layer was then isolated, filtered through Celite and charged to a 25I vessel. CH2CI2 (8445 ml) was then distilled out at atmospheric pressure and ethanol (10000 ml) added. Distillation was then continued with every 4000 ml of distillate that was removed being replaced with ethanol (4000 ml) until the head temperature reached 73.70C. The reaction volume was then reduced (to 7730 ml) by which time the head temperature had reached 78.90C and the solution was allowed to cool to 8C overnight. The solid was then filtered off, washed with ethanol (1290 ml) and dried at 700C overnight.Yield = 1377.3 g (90%). HPLC purity (99.34% [area %]). Contained 4.93% ethanol and 0.45% CH2CI2 by GC.

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; KUDOS PHARMACEUTICALS LIMITED; WO2008/47082; (2008); A2;,
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.

General procedure: Compound 4 (400 mg, 1.09 mmol, 1 eq) was dissolved in acetonitrile(10 ml), and then 5a-c (1 eq) and DIEA (2 eq) were added.The mixture was stirred at room temperature for 2 h, and then theprecipitate was filtered, washed with water, acetonitrile and ethylether, and dried to give products 6a-c.4.1.2.1. Methyl (E)-3-(4-((4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl) benzoyl)piperazin-1-yl)methyl)phenyl)acrylate(6a). White powder; yield 64%; mp 160-162 C; 1H NMR(400 MHz, DMSO-d6) d 12.60 (s, 1H), 8.26 (dd, J = 7.7, 1.5 Hz, 1H),7.96 (d, J = 7.7 Hz, 1H), 7.91-7.85 (m, 1H), 7.85-7.78 (m, 1H),7.72-7.60 (m, 3H), 7.46-7.40 (m, 1H), 7.36 (d, J = 8.0 Hz, 2H),7.31 (dd, J = 6.5, 2.3 Hz, 1H), 7.26-7.17 (m, 1H), 6.63 (d,J = 16.1 Hz, 1H), 4.32 (s, 2H), 3.73 (s, 3H), 3.67-3.56 (m, 2H), 3.51(s, 2H), 3.23-3.10 (m, 2H), 2.45-2.34 (m, 2H), 2.32-2.18 (m, 2H).19F NMR (376 MHz, DMSO-d6) d-119.83. 13C NMR (101 MHz,DMSO-d6) d 166.6, 163.63, 159.2, 156.2 (d, J = 245.4 Hz), 144.7,144.2, 140.4, 134.7 (d, J = 3.2 Hz), 133.3, 132.8, 131.4,, 129.2,129.0, 128.6 (d, J = 3.9 Hz), 128.2, 127.8, 126.0, 125.3, 123.7 (d,J = 18.3 Hz), 117.4, 115.9, 115.7, 61.2, 52.6, 52.0, 51.3, 46.5, 41.3,36.3. HRMS (ESI) m/z calculated for [M+H]+ 541.2251, found541.2227.

The synthetic route of 763111-47-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yuan, Zigao; Chen, Shaopeng; Sun, Qinsheng; Wang, Ning; Li, Dan; Miao, Shuangshuang; Gao, Chunmei; Chen, Yuzong; Tan, Chunyan; Jiang, Yuyang; Bioorganic and Medicinal Chemistry; vol. 25; 15; (2017); p. 4100 – 4109;,
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.

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).

The synthetic route of 763111-47-3 has been constantly updated, and we look forward to future research findings.

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

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.

The appropriate acid chloride (0.24 mmol) was added to a solution of 4- [4-Fluoro-3- (piperazine-1-carbonyl) benzyl]-2H-phthalazin-l-one (2) (0.2 mmol) in dichloromethane (2 ml). Hunigs base (0.4 mmol) was then added and the reaction was stirred at room temperature for 16 hours.

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; KUDOS PHARMACEUTICALS LIMITED; MAYBRIDGE LIMITED; WO2004/80976; (2004); 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 20 mg (54.5 muiotaetaomicronIota) of 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one dissolved in 1 mL of MeCN, 9.2 mg (65.5 muiotaetaomicronIota) 4-fluorobenzoic acid was added followed by 24.8 mg (65.5 muiotaetaomicronIota) of HBTU and 18 mu (131 muiotaetaomicronIota) of Et3N. The reaction mixture was stirred for 5 minutes and purified by H PLC to yield the compound as an orange solid (11.5 mg, 23.5 muiotaetaomicronIota, 43%). 1H-NM R (500 M Hz, CDC delta = 10.74 (s, 1H), 8.51-8.49 (d, 1H), 7.83-7.76 (m, 2H), 7.82 (s, 1H), 7.45-7.44 (m, 2H), 7.38-7.36 (m, 2H), 7.14-7.08 (m, 3H), 4.33 (s, 2H), 3.75-3.39 (m, 8H). MS-ES m/z [M + Na]+ = 511.2. H RMS-ESi m/z calculated for [C27 H22 N4 03 F2 Naf 511.1558, found 511.1569 [M + Na]+.

The synthetic route of 763111-47-3 has been constantly updated, and we look forward to future research findings.

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

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

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

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

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

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