Catalytic Enantioselective Formal Synthesis of MDM2 Antagonist RG7388 and Its Analogues.

Summary of main observation and conclusion: The catalytic asymmetric 1,3‐dipolar [3 + 2] cycloaddition of azomethine ylides with stilbenes has been established, affording structurally diverse pyrrolidines bearing four contiguous stereocenters with stereo‐diversity in generally high yields and good to excellent stereoselectivities (up to 98% yield, 99 : 1 dr, >99% ee). Meanwhile, this strategy allowed the formal synthesis of antitumor drug RG7388 (Phase III clinical study) and its analogues in high efficiency. [ABSTRACT FROM AUTHOR]