Aliphatic three-and four-membered rings including cyclopropanes, cyclobutanes, oxetanes,
azetidines and bicyclo [1.1. 1] pentanes have been increasingly exploited in medicinal …

The oxetane ring is an emergent, underexplored motif in drug discovery that shows attractive
properties such as low molecular weight, high polarity, and marked three-dimensionality …

Bioisosteres provide valuable design elements that medicinal chemists can use to adjust the
structural and pharmacokinetic characteristics of bioactive compounds towards viable drug …

The use of flow technology as an enabling tool for accessing 1-azabicyclo [1.1. 0] butanes
bearing strained 3-, 4-, and 5-membered O-heterocycles with C3 (N-het)–C2 (O-het) …

Four-membered heterocycles offer exciting potential as small polar motifs in medicinal
chemistry but require further methods for incorporation. Photoredox catalysis is a powerful …

Oxetanes and azetidines continue to draw significant interest in medicinal chemistry, as
small, polar and non-planar motifs. Oxetanes also represent interesting surrogates for …

Annulations that combine diacceptors with bis-nucleophiles are uncommon. Here, we report
the synthesis of 1, 4-dioxanes from 3-aryloxetan-3-ols, as 1, 2-bis-electrophiles and 1, 2 …

This work describes the 6-endo-dig cyclization of S-aryl propargyl sulfides to afford 2 H-
thiochromenes. The substitution at the propargylic position plays a crucial role in allowing …

A facile and sustainable protocol for the thiolation of hydrazones with sodium sulfinates has
been developed in the presence of CuBr2 and DBU in DMF to afford diverse benzylic …

Oxetanes have received increasing interest in medicinal chemistry as attractive polar and
low molecular weight motifs. The application of oxetanes as replacements for methylene …