# Enantioselective Synthesis of 3‑Alkyl-1,5-Functionalized 1,4-Diynes via Isoxazol-5(4H)‑ones

## TL;DR

This paper presents a new method to create chiral 1,4-diynes with high enantioselectivity using isoxazol-5(4H)-ones.

## Contribution

A novel enantioselective synthesis of 3-alkyl-1,5-functionalized 1,4-diynes using isoxazol-5(4H)-ones as a platform.

## Key findings

- The method achieves good overall yields and excellent enantioselectivities.
- It demonstrates the synthetic versatility of isoxazol-5(4H)-ones as a scaffold.
- The process combines conjugate addition and Zard-type transformation in one pot.

## Abstract

An enantioselective
strategy for the synthesis of chiral 3-alkyl-1,5-functionalized
1,4-diynes is reported. The method involves a highly enantioselective
organocatalytic conjugate addition of isoxazol-5­(4H)-ones to nitroenynes followed by a Zard-type transformation under
one-pot conditions yielding chiral skipped diynes in good overall
yields and with excellent enantioselectivities. This study highlights
the synthetic versatility of the isoxazol-5­(4H)-one
scaffold and its value as a platform for accessing structurally diverse
and synthetically relevant building blocks.