GB2422149A — Process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide
Assigned to Bial Portela and Cia SA · Expires 2006-07-19 · 20y expired
What this patent protects
A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide (1) by epoxide ring opening of 11a, 10b-dihydro-6H-dibenz[b,f]azepine-5-carboxamide (5) at elevated pressure. <EMI ID=1.1 HE=40 WI=98 LX=569 LY=918 TI=CF> Preferred conditions incl…
USPTO Abstract
A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide (1) by epoxide ring opening of 11a, 10b-dihydro-6H-dibenz[b,f]azepine-5-carboxamide (5) at elevated pressure. <EMI ID=1.1 HE=40 WI=98 LX=569 LY=918 TI=CF> Preferred conditions include performing the epoxide opening utilising hydrogenation (hydrogenolysis) with gaseous hydrogen at a pressure of 200 kPa-4 MPa and optionally elevated temperatures, in the presence of a catalyst, preferably palladium on charcoal (Pd on C). A base such as a trialkylamine may also be added to the reaction mixture. Suitable solvents include methanol/water. Subsequent derivatisation of alcohol (1) to form the corresponding ketone by oxidation, or ester groups etc by reaction with a suitable carbonyl compound is also outlined.
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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