Naturally occurring diaryl ethers exhibit significant potential for pharmaceutical
and agricultural applications owing to their diverse biological activities. Previous
synthetic approaches to these bioactive molecules have predominantly focused on developing
novel aryl–O–aryl bond formation methodologies. In this study, a two-phase synthetic strategy
is presented, comprising a coupling phase establishing the ethereal linkage through
SNAr reaction between simple aryl substrates, followed by a functionalization phase
enabling precise introduction of diverse substituents through C–H activation and subsequent
cross-coupling transformations. This modular approach has enabled the efficient synthesis
of four natural products: ethericin A, ethericin B, C10-deoxygerfelin, and diorcinol.
Key words
diaryl ether - two-phase synthesis - ethericin A - ethericin B - C10-deoxygerfelin
- diorcinol