EP4023644A1 — Process for the preparation of a pharmaceutical agent
Assigned to Zaklady Farmaceutyczne Polpharma SA · Expires 2022-07-06 · 4y expired
What this patent protects
This invention relates to a process for the preparation of empagliflozin comprising lithiation of (3S)-3-[4-(5-bromo-2-chlorobenzyl)phenoxy]tetrahydrofuran using lithium reagent, coupling the lithiated anion species with (3R,4S,5R,6R)-3,4,5-tris[(trimethylsilyl)oxy]-6-{[(trimethy…
USPTO Abstract
This invention relates to a process for the preparation of empagliflozin comprising lithiation of (3S)-3-[4-(5-bromo-2-chlorobenzyl)phenoxy]tetrahydrofuran using lithium reagent, coupling the lithiated anion species with (3R,4S,5R,6R)-3,4,5-tris[(trimethylsilyl)oxy]-6-{[(trimethylsilyl)oxy]methyl}tetrahydro-2H-pyran-2-one and reducing the product methyl 1-C-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl)-α-D-glucopyranoside] using triethylsilane and boron trifluoride diethyl etherate and optionally purifying the crude product, wherein the reduction is conducted in the presence of molecular sieves.
Drugs covered by this patent
- Jardiance (empagliflozin) · Boehringer Ingelheim
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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