摘要 |
<p>The present invention discloses a new process for producing ioversol (marketed as OPTIRAY3) comprising: (a) reacting 5-amino-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide with chloroacetyl chloride in a polar aprotic solvent, or combinations thereof, to produce N,N'-bis[2,3-di(2-chloroacetoxy)propyl]-5-(2-chloroacetamido)-2,4,6-triiodoisophthalamide; (b) reacting the product of (a) with sodium hydroxide to produce N,N'-bis(2,3-dihydroxypropyl)-5-(2-chloroacetamido)-2,4,6-triiodoisophthalamide; (c) reacting the product of (b) in water and sodium acetate to produce N,N'-bis(2,3-dihydroxypropyl)-5-glycolamido-2,4,6-triiodoisophthalamide; and (d) reacting the product of (c) with an alkylating agent capable of producing hydroxylhylated product in the presence of a base and water to produce ioversol.</p> |
申请人 |
MALLINCKRODT MEDICAL, INC. |
发明人 |
DUNN, THOMAS, JEFFREY;WHITE, DAVID, H.;KNELLER, MILLS, THOMAS;JONES, MICHELLE, M.;DORAN, NARCISO, OCAMPO, III |