Although there is an abundance of methods for the enantioselective synthesis of 2-isoxazolines and 2-isoxazolin-5-ones, relatively few of these approaches have been reported when these heterocycles bear fully substituted stereocenters. In this review, we will detail the methods that have been used to successfully accomplish these challenging asymmetric trans-formations and give insights into their importance, such as allowing access to unique three-dimensional chemical space. The limitations of the currently known reactions will be discussed, as well as highlighting the future developments needed to advance the research field.

Chemical concepts such as isosteres and scaffold hopping have proven to be powerful tools in agrochemical innovation processes. They offer opportunities to modify known molecular lead structures with the aim to improve a range of parameters, including biological efficacy and spectrum, physicochemical properties, stability, and toxicity. While recent biochemical insights into plant-specific receptors and signaling pathways trigger the discovery of the first lead structures, the disclosure of such a new chemical structure sparks a broad range of synthesis activities giving rise to diverse chemical innovation and often a considerable boost in biological activity. Herein, recent examples of isostere concepts in plant-hormone chemistry will be discussed, outlining how synthetic creativity can broaden the scope of natural product chemistry and giving rise to new opportunities in research fields such as abiotic stress tolerance and growth promotion.

Although there is an abundance of methods for the enantioselective synthesis of 2-isoxazolines and 2-isoxazolin-5-ones, relatively few of these approaches have been reported when these heterocycles bear fully substituted stereocenters. In this minireview, we will detail the methods that have been used to successfully accomplish these challenging asymmetric transformations and give insights into their importance, such as allowing access to unique three-dimensional chemical space. The limitations of the currently known reactions will be discussed, as well as highlighting the future developments needed to advance the research field.

Although there is an abundance of methods for the enantioselective synthesis of 2-isoxazolines and 2-isoxazolin-5-ones, relatively few of these approaches have been reported when these heterocycles bear fully substituted stereocenters. In this minireview, we will detail the methods that have been used to successfully accomplish these challenging asymmetric transformations and give insights into their importance, such as allowing access to unique three-dimensional chemical space. The limitations of the currently known reactions will be discussed, as well as highlighting the future developments needed to advance the research field.