Work

Continuous-flow synthesis of 1,4,6,7-tetrahydro-5 H -[1,2,3]triazolo[4,5- c ]pyridines towards key intermediates of clinical candidates JNJ-54175446 and zanvipixant (JNJ-55308942) with antidepressant activity

Year: 2025

Type: article

Abstract: temperature-controlled regioselectivity. Applying the optimized conditions, yields of 48% (58% regioselectivity) and 45% (91% regioselectivity) were achieved, respectively. The method ensures safe utilization of azide in the cycloaddition, and uses a safer oxidant for the elimination, offering a scalable and affordable alternative synthetic route.

Source: RSC Advances

DOI: 10.1039/d5ra03780h

Authors: Zsolt Fülöp, Péter Bana, István Greiner, János Éles

Institutions: Gedeon Richter (Hungary), Budapest University of Technology and Economics

Language: English

Topic: Innovative Microfluidic and Catalytic Techniques Innovation

Subfield: Biomedical Engineering

Field: Engineering

Domain: Physical Sciences

Open Access status: gold

Estimated APC paid: $1,042

Funders: Gedeon Richter, Nemzeti Kutatási, Fejlesztési és Innovaciós Alap