📜6,7-二甲氧基喹唑啉-4-酮置于吡啶,4-二甲氨基吡啶,甲烷磺酸,L-蛋氨酸,三氯氧磷体系中,用 异丙醇 作为反应溶剂,化学反应 28.0H,反应生成 4-((3-氯-2-氟苯基)氨基)-7-甲氧基喹唑啉-6-基乙酸酯
参考文献:The First Radiosynthesis Of [11 C]Azd8931 As A New Potential Pet Agent For Imaging Of Egfr,Her2 And Her3 Signaling
标题:The First Radiosynthesis Of [11 C]Azd8931 As A New Potential Pet Agent For Imaging Of Egfr,Her2 And Her3 Signaling
摘要:The Reference Standard Azd8931{2-(4-((4-((3-Chloro-2-Fluorophenyl) Amino)-7-Methoxyquinazolin-6-yl)Oxy) Piperidin-1-yl)-N-Methylacetamide} (11A) Was Synthesized From Methyl 4,5-Dimethoxy-2-Nitrobenzoate Or Ethyl 4,5-Dimethoxy-2-Nitrobenzoate And 2-Chloro-N-Methylacetamide In 11 Steps With 2-5% Overall Chemical Yield. The Precursor N-Desmethyl-Azd8931{2-(4-((4-((3-Chloro-2-Fluorophenyl)Amino)-7-Methoxyquinazolin-6-yl)Oxy)Piperidin-1-yl) Acetamide} (11B) Was Synthesized From Methyl 4,5-Dimethoxy-2-Nitrobenzoate Or Ethyl 4,5-Dimethoxy-2-Nitrobenzoate And 2-Bromoacetamide In 11 Steps With 2-4% Overall Chemical Yield. The Target Tracer [c-11] Azd8931 {2-(4-((4-((3-Chloro-2-Fluorophenyl) Amino)-7-Methoxyquinazolin-6-yl) Oxy) Piperidin-1-yl)-N-[c-11] Methylacetamide} ([c-11]11A) Was Prepared From N-Desmethyl-Azd8931 (11B) With [c-11]Ch3Otf Under Basic Condition (Nah) Through N-[11C] Methylation And Isolated By HPLC Combined With Solid-Phase Extraction (Spe) In 40-50% Radiochemical Yield Based On [c-11]Co2 And Decay Corrected To End Of Bombardment (Eob) With 370-1110 Gbq/mu Mol Specific Activity At Eob. (C) 2014 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2014.07.092