EP Patent

EP4487910A1 — Process for the preparation of dapagliflozin

Assigned to Zaklady Farmaceutyczne Polpharma SA · Expires 2025-01-08 · 1y expired

What this patent protects

The present invention relates to a process for the preparation of dapagliflozin, comprising the reaction of 4-(5-bromo-2-chlorobenzyl)phenyl ethyl ether starting material with an alkyl-lithium compound (step a); subsequent reaction of the obtained product with a trimethylsilyl-pr…

USPTO Abstract

The present invention relates to a process for the preparation of dapagliflozin, comprising the reaction of 4-(5-bromo-2-chlorobenzyl)phenyl ethyl ether starting material with an alkyl-lithium compound (step a); subsequent reaction of the obtained product with a trimethylsilyl-protected gluconolactone (step b); subsequent reaction of the obtained product with an acid in methanol to obtain the methyl C-aryl glycoside (V) (step c); and a last step, wherein the obtained product is converted to dapagliflozin, or a pharmaceutically acceptable salt or solvate thereof (step d). The selection of specific ratios and/or amounts of solvents in steps a) and c) provides an improved process, with improved overall purity with less purification steps.

Drugs covered by this patent

Patent Metadata

Patent number
EP4487910A1
Jurisdiction
EP
Classification
—
Expires
2025-01-08
Drug substance claim
No
Drug product claim
No
Assignee
Zaklady Farmaceutyczne Polpharma SA
Source
FDA Orange Book + USPTO grounding via Google Patents

Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.

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