title: Synthesis and Biological Evaluation of Cremastrine and an Unnatural Analogue.
abstract: In this Letter, we describe the first total synthesis of cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata, with anticholinergic activity as well as an unnatural analogue. The streamlined synthesis proceeds in 9 steps, 7 steps longest linear sequence, in 25.2% overall yield, and features novel methodology to construct the pyrrolizidine core. Biological evaluation of cremastrine and the unnatural analogue indicated that both are pan-mAChR functional antagonists.
authors: Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA.
authors: Kristopher N
authors: KN
authors: Hahn
authors: Olugbeminiyi O
authors: OO
authors: Fadeyi
authors: Hyekyung P
authors: HP
authors: Cho
authors: Craig W
authors: CW
authors: Lindsley