Dihydroxypyrrolidines constitute an important group of biologically active molecules that are found in nature. In this paper, we report the development of a selective method for the synthesis of 1,2‐disubstituted‐cis‐3,4‐dihydroxypyrrolidines from Ugi four‐component‐reaction/propargylamine adducts through a 5‐endo‐dig cycloisomerization and subsequent cis‐dihydroxylation process.
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