Herein we describe a compelling sequential methodology for obtaining optically active α‐arylmethanols‐1,2,3‐triazoles. The approach is based on the enantioselective alkynylation of aldehydes followed by a one‐pot two‐step desilylation/CuI‐catalyzed azide‐alkyne 1,3‐dipolar cycloaddition (CuAAC), providing the corresponding products with excellent yields and high levels of enantioselectivity. Furthermore, the click chemistry can be performed without affecting the enantiomeric excess. The application of the reaction has been demonstrated in the synthesis of a 1,2,3‐triazole analog of antihistaminic and anticholinergic drug (R)‐orphenadrine.

Herein, we describe the preparation and thorough characterization of a novel magnetically recoverable copper(I)-exchanged β-zeolite and its use as an efficient catalyst for the synthesis of 1,2,3-triazoles via the one-pot...

Compound (IIIb) shows potential as an antioxidative agent.

No abstract

The Front Cover shows a chiral arylmethanols bearing the 1,2,3‐triazole moiety, with a variety of di(hetero)arylmethanols, which do not contain any N‐heteroatom. Such molecules can be obtained by using a straightforward sequential approach based on the enantioselective alkynylation of aldehydes followed by a one‐pot two‐step desilylation/CuAAC, providing the products with excellent yields and high levels of enantioselectivity. More information can be found in the https://doi.org/10.1002/ejoc.201800751