[EN] PROCESS FOR THE PREPARATION OF A DIASTEREOMERICALLY ENRICHED COMPOUND<br/>[FR] PROCEDE POUR LA PREPARATION D'UN COMPOSE ENRICHI EN DIASTEREOMERE
申请人:DSM IP ASSETS BV
公开号:WO2006008171A1
公开(公告)日:2006-01-26
The present invention relates to a process for the preparation of a diastereomerically enriched compound, wherein a first compound according to formula (I), is contacted with a second compound according to formula (II), to form a third compound according to formula (III), whereby the compound according to formula (III) is subsequently reduced and thereby converted into a compound according to formula (IV), in which formulas: R1= a cycloalkylgroup whereby R1 # R2, R2= a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenylgroup, aryl group, cyclic or acyclic heteroalkylgroup or heteroarylgroup, R3= an alkyl group, R4= a substituted or unsubstituted: phenyl- or naphthyl-group, *= a chiral center. The invention furthermore relates to a diastereomerically enriched compound according to formula (IV) and its use in the preparation of pharmaceutical and agrochemically active compounds. The invention further relates to a process for the preparation of enantiomerically enriched compounds of formula (V), through hydrogenolysis of diastereomerically enriched compounds of formula (IV), wherein R1 and R2 have the meanings given above.
本发明涉及一种制备对映异构体富集化合物的过程,其中将式(I)的第一化合物与式(II)的第二化合物接触,形成式(III)的第三化合物,随后将式(III)的化合物还原,从而转化为式(IV)的化合物,其中式中:R1 = 环烷基,其中R1 ≠ R2,R2 = 取代或未取代的:(环)烷基,(环)烯基基团,芳基基团,环状或非环状杂基基团或杂环基团,R3 = 烷基,R4 = 取代或未取代的苯基或萘基,* = 手性中心。此外,本发明还涉及一种对映异构体富集化合物,其符合式(IV),以及其在制备制药和农业化学活性化合物中的应用。本发明还涉及一种制备式(V)的对映异构体富集化合物的过程,通过对式(IV)的对映异构体进行氢解,其中R1和R2具有上述含义。