Asymmetric Iodoaminocyclization for the Synthesis of Chiral 2-Heteroaryl Pyrrolidines

An asymmetric iodoaminocyclization strategy catalyzed by (DHQD)2PHAL has been developed for the synthesis of chiral 2-heteroaryl pyrrolidines, including 2-purinyl and 2-indolyl analogues. This method proceeds under mild conditions and affords the target products in high yields (up to 98%) with excellent diastereoselectivity (trans only) and enantioselectivity (up to 98% ee). The approach provides efficient access to azanucleoside-like scaffolds and demonstrates broad functional group tolerance, highlighting its potential for the synthesis of biologically active pyrrolidine derivatives.