公开(公告)号：EP2274292A1

公开(公告)日：2011-01-19

申请号：EP09718942.7

申请日：2009-03-13

申请人： Bial-Portela & CA, S.A.

发明人： BELIAEV, Alexander ,  LEARMONTH, David, Alexander ,  ALMENA PEREA, Juan José ,  GEIß, Gerhard ,  HITZEL, Patrick ,  KADYROV, Renat ,  VOIGTLAENDER, David

IPC分类号： C07D311/04

CPC分类号： C07D311/04

摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein: X is CH
2 , oxygen or sulphur; R
1 , R
2 and R
3 are the same or different and signify hydrogen, halogen, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R
4 is alkyl or aryl, the transition metal catalyst comprising a chiral ligand having the formula wherein each R and R' independently represents alkyl, aryl, aralkyl, alkenyl, alkynyl, alkoxy, aryloxy, alkylthio, arylthio, unsubstituted or substituted cyclic moiety selected from a group consisting of monocyclic or polycyclic saturated or partially saturated carbocyclic or heterocyclic, aromatic or heteroaromatic rings said rings comprising from 4 to 8 atoms and comprising from 0 to 3 heteroatoms, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means an aromatic or heteraromatic group, optionally substituted one or more times by alkyl, alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.