He Bin, Song Hao, Du Yu, Qin Yong
Department of Chemistry of Medicinal Natural Products, Key Laboratory of Drug Targeting and Novel Delivery System of Ministry of Education, West China School of Pharmacy, Chengdu 610041, PR China.
J Org Chem. 2009 Jan 2;74(1):298-304. doi: 10.1021/jo802216z.
Total synthesis of potent anti-MDR indole alkaloids (-)-ardeemin and its N-acyl analogues has been accomplished from L-tryptophan with about 2% overall yield in 20 steps. The key step depended on the newly developed three-step one-pot cascade reaction of 7 with diazoester 8 via intermolecular cyclopropanation, ring opening, and ring closure to assemble the chiral 3-substituted hexahydropyrrolo[2,3-b]indole 4a.
已从L-色氨酸完成了强效抗多药耐药吲哚生物碱（-）-ardeemin及其N-酰基类似物的全合成，总收率约为2%，共20步。关键步骤依赖于新开发的7与重氮酯8通过分子间环丙烷化、开环和闭环的三步一锅串联反应，以组装手性3-取代六氢吡咯并[2,3-b]吲哚4a。
