Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, New Mexico 87801, USA.
Org Lett. 2011 Mar 4;13(5):1118-21. doi: 10.1021/ol103149b. Epub 2011 Jan 26.
Privileged medicinal scaffolds based on the structures of tetra- and pentasubstituted 2-aminopyrroles were prepared via one-pot multicomponent reactions of structurally diverse aldehydes and N-(aryl-, hetaryl-, alkylsulfonamido)acetophenones with activated methylene compounds. This methodology was used in a four-step synthesis of alkaloids rigidins A, B, C, and D in overall yields of 61%, 58%, 60%, and 53%, respectively. Of these, rigidins B, C, and D were synthesized for the first time.
基于四取代和五取代 2-氨基吡咯结构的特权药物支架，通过结构多样的醛和 N-(芳基、杂芳基、烷基磺酰胺基)苯乙酮与活性亚甲基化合物的一锅多组分反应来制备。该方法用于四步合成生物碱 rigidins A、B、C 和 D，总收率分别为 61%、58%、60%和 53%。其中，rigidins B、C 和 D 是首次合成的。
