C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 305/14 (2006.01) C07D 407/12 (2006.01)
Patent
CA 2214993
An antitumor compound of formula (5), in which R = Ac or H, and R1 = R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R3 = H; R1 = R2 = R3 = H; R1 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R2 = R3 = H; R1 = R3 = H, R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R1 = H, R2 = R3 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R1 = R2 = R3 = an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t- Bu is tert-butyl. Also provided by the invention is a one-step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.
Composé antitumoral de formule (5), dans laquelle R = Ac ou H, et R¿1? = R¿2? = un groupe alkyle tel que Me, Et, Pr, i-Pr, n-Bu ou t-Bu, R¿3? = H; R¿1? = R¿2? = R¿3? = H; R¿1? = un groupe alkyle tel que Me, Et, Pr, i-Pr, n-Bu ou t-Bu, R¿2? = R¿3? = H; R¿1? = R¿3? = H, R¿2? = un groupe alkyle tel que Me, Et, Pr, i-Pr, n-Bu ou t-Bu; R¿1? = H, R¿2? = R¿3? = un groupe alkyle tel que Me, Et, Pr, i-Pr, n-Bu ou t-Bu; R¿1? = R¿2? = R¿3? = un groupe alkyle Me, Et, Pr, i-Pr, n-Bu ou t-Bu. Me est une abréviation pour méthyle, Et représente éthyle, Pr représente propyle, i-Pr représente isopropyle, n-Bu représente n-butyle, et t-Bu représente tert-butyle. L'invention concerne également un procédé en une étape de préparation d'un composé de la formule (5), selon lequel un taxane présenant un groupe tiglate fixé à la chaîne latérale est mis en contact avec un réactif oxydant ayant pour résultat la formation d'un époxyde présentant une activité antitumorale.
Daughenbaugh Randall J.
Murray Christopher K.
Zheng Qun Y.
Hauser Inc.
Hauser Chemical Research Inc.
Smart & Biggar
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