Method for producing single enantiomer epoxides by the adh...

C - Chemistry – Metallurgy – 07 – D

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C07D 303/08 (2006.01)

Patent

CA 2612407

The invention relates to a method for producing single enantiomer epoxides by reducing a-leaving group-substituted ketones with (R)- or (S)-selective alcohol dehydrogenases in the presence of a cofactor and optionally a suitable system for regenerating the oxidised cofactor, to produce the corresponding single enantiomer alcohols and subsequently, by means of cyclisation induced by a base, the corresponding single enantiomer epoxides (EQUATION 1 ), wherein in EQUATION 1 LG may stand for F, CI, Br, I, OSO2Ar, OSO2CH3, OSO2R or OP(O)OR2, and R1, R2 and R3, independently of one another, stand for hydrogen, a branched or unbranched, optionally substituted C1-C2O- alkyl radical, symbolise an optionally randomly substituted C3-C10- cycloalkyl or alkenyl radical or a randomly substituted carbo- or heterocyclic aryl radical, or corresponds to a radical from the group CO2R, CONR2, COSR, CS2R, C(NH)NR2, CN, CHaI3, ArO, ArS, RO, RS, CHO, OH, NHR, NR2, Cl, F, Br, I or SiR3.

Procédé de production d'époxydes exempts d'énantiomères par réduction de cétones à substitution d'.alpha.-nucléofuges à l'aide d'alcool déshydrogénases à sélection (R) ou (S) en présence d'un cofacteur et éventuellement d'un système approprié pour la régénération du cofacteur oxydé, pour obtenir les alcools exempts d'énantiomères correspondants, puis par cyclisation subséquente induite par une base pour obtenir les époxydes exempts d'énantiomères correspondants (EQUATION 1) dans laquelle LG peut signifier F, Cl, Br, I, OSO2Ar, OSO2CH3, OSO2R ou OP(O)OR2 et R1, R2 et R3 représentent indépendamment les uns des autres hydrogène, un radical alkyle C1-C20 ramifié ou non ramifié, éventuellement substitué, symbolisent un radical cycloalkyle C3-C10, éventuellement substitué d'une manière quelconque, un radical alcényle ou un radical aryle carbocyclique ou hétérocyclique substitué d'une manière quelconque, ou correspondent à un radical du groupe CO2R, CONR2, COSR, CS2R, C(NH)NR2, CN, CHal3, ArO, ArS, RO, RS, CHO, OH, NHR, NR2, Cl, F, Br, I ou SiR3.

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