CAS: 519059-09-7; 5-(Cyanomethyl)-2-Fluorobenzonitrile

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CAS号7677-24-9 三甲基氰硅烷 | CAS号180302-35-6 2-氟-5-(溴甲基)苯腈

📜三甲基氰硅烷,3-氰基-4-氟苄溴置于四丁基氟化铵体系中,用 乙腈 作为反应溶剂,化学反应 2.0H,反应生成 3-氰基-4-氟苯乙腈
参考文献:Development Of Substituted 6-[4-Fluoro-3-(Piperazin-1-Ylcarbonyl)Benzyl]-4,5-Dimethylpyridazin-3(2H)-Ones As Potent Poly(Adp-ribose) Polymerase-1 (Parp-1) Inhibitors Active In Brca Deficient Cells
标题:Development Of Substituted 6-[4-Fluoro-3-(Piperazin-1-Ylcarbonyl)Benzyl]-4,5-Dimethylpyridazin-3(2H)-Ones As Potent Poly(Adp-ribose) Polymerase-1 (Parp-1) Inhibitors Active In Brca Deficient Cells
摘要:We Describe An Extensive Sar Study In The 6-[4-Fluoro-3-(Substituted)Benzyl]-4,5-Dimethylpyridazin-3(2H)-One Series Which Led To The Identification Of Potent Parp-1 Inhibitors,Capable Of Inhibiting The Proliferation Of Brca-1 Deficient Cancer Cells In The Low Nanomolar Range,And Displaying >100-Fold Selectivity Over The Brca Wild Type Counterparts. The Series Of Compounds Was Devoid Of Herg Channel Activity,And Cyp Inhibition And Induction Liabilities. Several Analogs Were Stable In Rat And Human Liver Microsomes And Displayed Moderate Rat Clearance,With Urinary Excretion Of Parent As The Major Route Of Elimination. (C) 2009 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2009.11.087