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.
EXAMPLE A.4. Compound c-3 (127l): 4-(4-fluoro-3-(4-(2-(3-iodophenyl)acetyl)piperazine-l-carbonyl)- benzyl)phthalazin-l(2H)-one. A solution of 3-iodophenyl acetic acid (6.5 mg, 0.048 mmol), l-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) (10.5 mg, 0.055 mmol), N-hydroxy succinimide (NHS) and 600 mu DM F was stirred for 30 min at room temperature. Then, 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)- phthalazin-l(2H)-one (10 mg, 0.0275 mmol) was added to the solution and the mixture was stirred at room temperature overnight. The reaction was washed with 500 mu of H20 and extracted with 500 mu dichloromethane (DCM). The resulting organic solution was purified on silica gel, using a gradient elution from neat DCM to DCM/hexane 5:1 to obtain the desired product as a white solid (3 mg, 20% yield). 1H NMR (CDCI3) delta = 9,82 (s, 1H), 8.40-8.38 (m, 1H), 7.71-7.69 (m, 2H), 7.55-7.53 (m, 1H), 7.51-7.50 (m, 2H), 7.25-7.24 (m, 2H), 7.09-6.90 (m, 3H), 4.20 (s, 2H), 3.64-3.31 (m, 8H), 2.84 (s, 2H). LC-ESI-MS (+) m/z = 633.1 [M+Na+]+. HRMS-ESI [M+H+]+ m/z calculated for [C28H24FIN403]+ 611.0955, found 611.0948.
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.
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