Work

Synthesis of belumosudil

Year: 2025

Type: article

Abstract: We developed a novel synthetic route to belumosudil featuring an oxidative cyclization of anthranilamide with meta ‐substituted benzaldehyde as the key step for constructing the quinazolinone scaffold. Alkylation of 3‐hydroxybenzaldehyde with 2‐chloroacetamide furnished a benzaldehyde derivative bearing the desired meta ‐substituent. Subsequent metal‐free aerobic oxidative cyclization of anthranilamide and the aldehyde in DMSO afforded the desired quinazolinone. Treatment with POCl 3 converted the quinazolinone intermediate into the corresponding quinazolinyl chloride, which was then coupled with 5‐aminoindazole to complete the synthesis of belumosudil.

Source: Bulletin of the Korean Chemical Society

DOI: 10.1002/bkcs.70079

Authors: Sangjun Park, Jinjae Park, Tae Lyn Kim, Cheol‐Hong Cheon

Institution: Korea University

Language: English

Topic: Quinazolinone synthesis and applications

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: bronze

Funders: National Research Foundation, National Research Foundation of Korea