CAS: 2169-44-0; (S)-1,2,10-Trimethoxy-6-Methyl-5,6,6A,7-Tetrahydro-4H-Dibenzo[de,G]Quinolin-9-Ol

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(-)-roemerialinone methanol boldine

📜波尔定碱置于偶氮二甲酸二异丙酯,四丁基氟化铵,三苯基膦体系中,用 四氢呋喃 用作溶剂,化学反应 2.17H,反应生成波尔定碱 2-甲醚
参考文献:Semisynthetic Studies On And Biological Evaluation Of N-Methyllaurotetanine Analogues As Ligands For 5-Ht Receptors
标题:Semisynthetic Studies On And Biological Evaluation Of N-Methyllaurotetanine Analogues As Ligands For 5-Ht Receptors
摘要:N-Methyllaurotetanine (1) Has Been Reported To Display Good Affinity For The 5-Ht1A Receptor,But No Structureaffinity Studies Have Been Performed To Date. The Commercially Available Alkaloid Boldine (2) Was Used As The Starting Material For Synthesis Of Various C-9 Alkoxy Analogues Of N-Methyllaurotetanine In Order To Gauge The Effect Of C-9 Alkylation On Affinity And Selectivity At 5-Ht1A,5-Ht2A,And 5-Ht7 Receptors. Mitsunobu Reactions Were Implemented In The Alkylation Steps Leading To The Analogues. Modest Improvement In 5-Ht1A Affinity Was Observed Upon Alkylation For Most Analogues. Thus,The C-9 Hydroxy Group Of 1 Is Not Critical For Affinity To The 5-Ht1A Receptor. Some Analogues Displayed High Affinity For The 5-Ht7 Receptor,Comparable To N-Methyllaurotetanine,With Moderate Selectivity Vs 5-Ht1A And 5-Ht2A Receptors.
Doi:10.1021/np500893H