Methods for the site-selective introduction of halogen into natural products
US9944967B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 20, 2014 |
| Grant date | Apr 17, 2018 |
| Priority date | — |
| Expiry date | Aug 20, 2034 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12P7/62
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Organohalides (e.g., organofluorides) represent a rapidly expanding proportion of molecules used in pharmaceuticals, diagnostics, agrochemicals, and materials. The present invention exploits the naturally occurring acetate condensation pathway as a means of introducing halogenated building blocks into natural product scaffolds. In an exemplary embodiment, the invention provides a pathway involving at least one polyketide synthase system and utilizes haloacetate or a haloacetate synthon (e.g., halomalonate) to incorporate an organohalide into the polyketide backbone in vitro. In an exemplary embodiment, the invention provides an analogous method for site-selective introduction of haloacetate or a synthon into polyketide products in vivo. The present invention expands the scope of existing chemical methods for producing halogenated natural product scaffolds such as complex halogenated natural products.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.