Downstream synthetic route of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

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

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO278,mainly used in chemical industry, its synthesis route is as follows.,763111-47-3

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.

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; KUDOS PHARMACEUTICALS LIMITED; MAYBRIDGE LIMITED; WO2004/80976; (2004); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

The important role of 763111-47-3

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

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

The important role of 763111-47-3

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

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

The important role of 763111-47-3

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

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

The important role of 763111-47-3

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

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

The important role of 763111-47-3

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

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

Share a compound : 763111-47-3

763111-47-3 is used more and more widely, we look forward to future research findings about 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

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

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%.

763111-47-3 is used more and more widely, 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

Simple exploration of 763111-47-3

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.

763111-47-3,763111-47-3, 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

To a solution of compound 1.3.2a dispersed in 200 mu of acetonitrile was added HBTU (500 mug, 131 mmol) and 1.4.2 (500 mug , 137 mmol). The reaction was kept at 32 C in a shaker for 3 hours at 700 rpm. The final product was isolated by HPLC employing a C18 Atlantis T3 column (4.6 x 250 mm, 5 muiotaeta) with the following eluents: water as solvent A and acetonitrile as solvent B, going from 5 % of B to 100% of B in 15 minutes and then 100% of B from 15.01 minutes to 25 minutes. The fractions containing the radioligand were dried in vacuum, obtaining a white solid as product.

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; 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

The important role of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

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

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

Analyzing the synthesis route of 763111-47-3

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

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