1,3‐Oxazolidines, derived from widely available enantiomerically pure 1,2‐aminoalcohols, are versatile chiral auxiliaries for several key transformations, often serving as a platform for inquiries into new and complex reactivity. This Review focuses on the chemistry of N‐acyl‐1,3‐oxazolidines in which the stereoselective transformation is carried out on the N‐acyl attached side chain of the molecule, covering reports from late 1980s to 2020 across several fields of asymmetric synthesis of bioactive molecules, and in particular of natural products.
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