A one-step gram-scale protocol for stereoselective domino dimerization to asperazine A analogs

Here, we present an efficient protocol for stereoselective 4N-based domino dimerization in one single step, establishing a 22-membered library of asperazine A analogs. We describe steps for performing a gram-scale 2N-monomer to access the unsymmetrical 4N-dimer. We detail the synthesis of the desired dimer 3a as a yellow solid in 78% yield. This process demonstrates the 2-(iodomethyl)cyclopropane-1,1-dicarboxylate to be an iodine cation source. The protocol is limited to unprotected aniline of 2N-monomer. For complete details on the use and execution of this protocol, please refer to Bai et al. (2022).¹