Optimizing the CHF6523 Isocoumarin Core Scaffold: From the Preclinical Stage to Large-Scale Production
| Title: | Optimizing the CHF6523 Isocoumarin Core Scaffold: From the Preclinical Stage to Large-Scale Production |
|---|---|
| Authors: | Rocco Bussolati; Paolo Ronchi; Fausto Pivetti; Claudio Fiorelli; Emanuele Ferrari; Diego Copelli; Massimiliano Mari; Paolo Bruno; Matteo Biagetti; Piotr Malysa; Xiaoping Tang; Jonathan Simmons; Max Espensen; Benjamin Rowley; Peter Mullens; Huihua Lu; Junqiang Wang; Huajun Ge; Zhongwei Zhang |
| Publication Year: | 2025 |
| Collection: | The University of Auckland: Figshare |
| Subject Terms: | Biochemistry; Medicine; Cell Biology; Genetics; Biotechnology; Developmental Biology; Infectious Diseases; Plant Biology; pi3kδ inhibitor chf6523; multikilogram synthesis route; isocoumarin core scaffold; described molecule bears; api candidate ’; provide large quantities; api process development; process research; development work; successful establishment; scale production; product required; preclinical stage; clinical studies |
| Description: | The structure of the new active pharmaceutical ingredient (API) PI3Kδ inhibitor CHF6523.02, identified for the treatment of exacerbating chronic obstructive pulmonary disease (COPD) in patients, is reported. The described molecule bears an isocoumarin core scaffold, whose synthetic route scalability is critical for API process development and the successful establishment of a multikilogram synthesis route. In this paper, we describe the process research and development work for the isocoumarin scaffold synthetic procedure, exploiting a novel and efficient electrophilic cyclization step, to provide large quantities of the product required to support the API candidate’s clinical studies. |
| Document Type: | article in journal/newspaper |
| Language: | unknown |
| DOI: | 10.1021/acs.oprd.5c00133.s001 |
| Availability: | https://doi.org/10.1021/acs.oprd.5c00133.s001; https://figshare.com/articles/journal_contribution/Optimizing_the_CHF6523_Isocoumarin_Core_Scaffold_From_the_Preclinical_Stage_to_Large-Scale_Production/29437060 |
| Rights: | CC BY-NC 4.0 |
| Accession Number: | edsbas.B7AF9510 |
| Database: | BASE |