Tetrahedron ( IF 2.1 ) Pub Date : 2017-08-24 , DOI: 10.1016/j.tet.2017.08.042 Misayo Sera , Hideya Mizufune , Tsuyoshi Ueda , Masahiro Mineno , Atsuhiko Zanka
Efficient synthetic strategies for furnishing α-carbolines have been developed by integrating various Pd-catalyzed reactions. The methods involve 1) regioselective 5- or 6- halogenation of α-carbolines which were synthesized through intramolecular Pd-catalyzed direct C-H arylation, and subsequent Pd-catalyzed cross coupling, 2) 8-triflation of α-carbolines constructed by Pd-catalyzed cyclization, followed by Pd-catalyzed cross-coupling reaction, 3) Pd-catalyzed cyclization to tetrahydro-α-carbolines and subsequent Suzuki reaction via the corresponding α-carboline 5-triflates.
中文翻译:
集成Pd催化的交叉偶联策略,用于制备α-咔啉
通过整合各种Pd催化的反应,已经开发出用于合成α-咔啉的有效合成策略。该方法包括:1)通过分子内Pd催化的直接CH芳基化反应合成的α-咔啉的区域选择性5-或6-卤代,然后进行Pd催化的交叉偶联; 2)通过Pd催化的α-咔啉的8-三氟甲磺酸酯化。环化,然后进行Pd催化的交叉偶联反应,3)Pd催化的环化反应生成四氢-α-咔啉,随后通过相应的α-咔啉5-三氟甲磺酸酯进行Suzuki反应。