Nam Seonghyeon, Lee Sunhee, Kim Woojin, Kim Ikyon
College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 85 Songdogwahak-ro, Yeonsu-gu, Incheon, 21983, Republic of Korea.
Org Biomol Chem. 2023 May 10;21(18):3881-3895. doi: 10.1039/d3ob00471f.
Herein we describe the divergent synthesis of two types of indolizines construction of the pyrrole moiety from pyridine-2-acetonitriles, arylglyoxals, and TMSCN. While one-pot three-component coupling provided 2-aryl-3-aminoindolizines an unusual fragmentation process, a sequential two-step assembly protocol with these starting materials allowed efficient access to a wide range of new 2-acyl-3-aminoindolizines through an aldol condensation-Michael addition-cycloisomerization process. The subsequent manipulation of 2-acyl-3-aminoindolizines enabled direct access to novel polycyclic -fused heteroaromatic skeletons.
在此，我们描述了两类中氮茚的发散合成——由吡啶 -2- 乙腈、芳基乙二醛和 TMSCN 构建吡咯部分。虽然一锅三组分偶联通过一个不寻常的碎片化过程得到 2- 芳基 -3- 氨基中氮茚，但使用这些起始原料的顺序两步组装方案通过羟醛缩合 - 迈克尔加成 - 环异构化过程能够高效地获得多种新型 2- 酰基 -3- 氨基中氮茚。对 2- 酰基 -3- 氨基中氮茚的后续操作能够直接得到新型多环稠合杂芳族骨架。
