New process for the preparation of oxabispidines

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 498/08 (2006.01) A61K 31/5386 (2006.01) A61P 9/06 (2006.01)

Patent

CA 2443475

There is provided a process for the preparation of a compound of formula (I): which process comprises reaction of a compound of formula (II): with either a compound of formula (III): or acrylamide, followed, in the latter case, by reaction of the resulting intermediate of formula (IV): with an alcohol of formula R2-OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R2- OH, and wherein R1, R2 and R16 have meanings given in the description.

Cette invention concerne un procédé de préparation d'un composé de formule (I). Ce procédé consiste à faire réagir un composé représenté par la formule (II) avec soit un composé de formule (III) : ou un acrylamide, opération suivie dans ce dernier cas d'une réaction de l'intermédiaire de formule (IV) qui en résulte avec un alcool de formule R?2¿-OH et un agent qui favorise ou des agents qui, en combinaison, favorisent le réarrangement et l'oxydation du compose de formule (IV) en un isocyanate intermédiaire, qui peut ensuite réagir avec un alcool de formule R?2¿-OH, R?1¿, R?2¿ et R?16¿ ayant les significations qui leur sont attribuées dans le descriptif.

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