公开(公告)号：US20080167500A1

公开(公告)日：2008-07-10

申请号：US11632699

申请日：2005-07-20

申请人： Quirinus Bernardus Broxterman ,  Ben De Lange ,  Henrius Leonardus Marie Elsenberg ,  Matthias Weber

发明人： Quirinus Bernardus Broxterman ,  Ben De Lange ,  Henrius Leonardus Marie Elsenberg ,  Matthias Weber

IPC分类号： C07C211/01

CPC分类号： C07C209/28 ,  C07C2601/02 ,  C07C211/17 ,  C07C211/27 ,  C07C211/29

摘要： 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 cycloalkyl group whereby R1 # R2, R2=a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenyl group, aryl group, cyclic or acyclic heteroalkyl group or heteroaryl group, 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.

摘要翻译： 本发明涉及一种制备非对映体富集的化合物的方法，其中根据式（I）的第一化合物与式（II）的第二化合物接触，以形成式（III）的第三化合物 ），由此将式（III）化合物随后还原，从而转化成式（Ⅳ）化合物，其中R 1 =环烷基，其中R 1 （环）烷基，（环）烯基，芳基，环状或无环杂烷基的取代或未取代的 或杂芳基，R 3 =烷基，R 4 =取代或未取代的：苯基或萘基，* =手性中心。 本发明还涉及根据式（IV）的非对映异构体富集的化合物及其在制备药物和农业化学活性化合物中的用途。 本发明还涉及通过氢解非对映体富集的式（Ⅳ）化合物来制备对映体富集的式（Ⅴ）化合物的方法，其中R 1和R 2， SUB>具有上述含义。