A stereospecific process for the preparation of a pharmaceutically active compound in at least 70% by weight S-configuration of the formula
or a pharmaceutically acceptable salt or ester thereof, wherein R1 represents an optionally substituted aryl group such as a phenyl or naphthyl group, or R1 represents a heterocyclic ring system, which is optionally . substituted, or R1 represents a heteroaromatic ring system optionally containing in addition to carbon atoms one or more atoms of nitrogen, sulphur or oxygen atoms, this ring system being optionally substituted, comprises subjecting a compound of the formula
wherein R2 is an alkyl group containing at least 3 carbon atoms, to the action of a micro-organism or substances derived therefrom capable of stereoselective oxidation of compound (II) into compound (I), having at least 70% by weight S-configuration.
一种制备式中至少 70%(重量)为 S-构型的药用活性化合物或其药用盐或酯的立体定向工艺
或其药学上可接受的盐或酯,其中 R1 代表任选被取代的芳基,如苯基或
萘基,或 R1 代表任选被.取代的杂环环系,或 R1 代表除碳原子外还任选含有一个或多个氮、
硫或氧原子的杂芳环环系,该环系任选被取代,该工艺包括将式的化合物
其中 R2 是含有至少 3 个碳原子的烷基,在微
生物或由微
生物衍生的物质的作用下,能将化合物 (II) 立体选择性地氧化成化合物 (I),其 S-构型的重量比至少为 70%。