Increased building block access through collaboration. Issue 8 (August 2018)

• Record Type: Journal Article
• Authors: Helal, Christopher J.; Bartolozzi, Alessandra; Goble, Steven D.; Mani, Neelakanda S.; Guzman-Perez, Angel; Ohri, Ajay K.; Shi, Zhi-Cai; Subramanyam, Chakrapani
• Is Part Of: Drug discovery today. Volume 23:Issue 8(2018)
• Page Start: 1458
• Page End: 1462
• Publication Date: 2018-08
• Subjects: Drugs -- Design -- Periodicals; Drugs -- Research -- Periodicals; 615.1
• DOI: 10.1016/j.drudis.2018.03.001
• Languages: English
• ISSNs: 1359-6446

Abstract

Graphical abstract: Highlights: Fluorine can impact potency, selectivity and ADME of medicinal chemistry analogs. Fluorinated building blocks (FBB) greatly enable fluorinated analog preparation. Some vendor-listed FBB are expensive because many have not been synthesized. A vendor–pharma Buying Group was created to share costs and reduce FBB prices. The details of the Buying Group formation, FBB usage and conclusions are presented. We detail the formation of a pilot multipharmaceutical-company–chemical-vendor Buying Group that successfully facilitated access to fluorinated building blocks of high interest to medicinal chemists for analog synthesis at significantly reduced prices. This exercise showed significant overlap in building block interests among the participants and suggests that creative approaches to access building blocks is of common interest to medicinal chemists and will be valuable as the challenges of drug discovery continue to call for more-highly-tuned drug candidates that can be synthesized quickly.