Table 1. Structures and summary of biophysical, permeability and lipophilicity results for VHL inhibitors.

*Reaction conditions:1/LiHMDS/2/[Pd(η³-C₃H₅)Cl]₂/S-IPr·HCl=200/200/100/2.5/5; 0.1 M of ketone 1; T=30^oC; B/L and dr was determined by ¹H NMR, dr is the ratio of (±)-(syn,anti)-3/other diastereoisomers; Isolated yield. †T=50 ^oC. ‡Solvent=THF. §OBoc of 2 was replaced with OP(OEt)₂. ||The yield was determined by ¹H NMR.