GB2502624A — Phosphoramide and phosphoramide-based catalysts and their use in intermolecular aziridination
Assigned to University of East Anglia · Expires 2013-12-04 · 12y expired
What this patent protects
A method of synthesising aziridines of formula (III) or a salt thereof including isotopically labelled aziridines, the method comprising contacting an imine (I), or one or more precursors thereof, with a diazo compound (II) or a salt thereof in the presence of a phosphoramide or …
USPTO Abstract
A method of synthesising aziridines of formula (III) or a salt thereof including isotopically labelled aziridines, the method comprising contacting an imine (I), or one or more precursors thereof, with a diazo compound (II) or a salt thereof in the presence of a phosphoramide or a phosphoramide-derived catalyst of formulae (IV) or (V): wherein R1-R9 are any atom or group; and X is O, S or NR9. Preferred diazo compounds include tert-butyl diazoacetate, deuterated tert-butyl diazoacetate, deuterated allyl diazoacetate and ethyl diazoacetate. Preferred catalysts are chiral 1,1-bi-2-naphthol (BINOL) based phosphoramides with (S)-3,3-bis(9-anthracenyl)-[1,1]-binaphthalen-2,2-yl-N-triflyl-phosphoramide being particularly preferred. Certain phosphoramide or phosphoramide-derived catalysts of formulae (IV) and (V) are also claimed.
Drugs covered by this patent
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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