公开(公告)号：EP3808737A1

公开(公告)日：2021-04-21

申请号：EP20171586.9

申请日：2014-09-12

申请人： BIAL - Portela & Ca., S.A.

发明人： RUSSO, Domenico ,  WAHON, Jorge ,  MATON, William ,  WEBER, Beat T. ,  JERÓNIMO, Paula ,  SOUSA, Luisa ,  BARROCAS, Pedro ,  PIRES, Rita ,  LIMA, Ricardo ,  VASCONCELOS, Téofilo Cardoso de

IPC分类号： C07D311/12 ,  C07D311/20

摘要： The present invention provides a process for preparing the (R)-enantiomer (R-N) or the (R)-enantiomer (S-N) of a compound of formula N, the process comprising subjecting a compound of formula M to reduction using a reductase enzyme

The present invention also provides a process for preparing a nitro chromane compound of formula N, the process comprising reacting a nitro chromene compound of formula M with a suitable reducing agent.

The present invention also provides a process for preparing the (R)-or (S)-enantiomer of a compound of formula E or a salt thereof

公开(公告)号：EP3044215A1

公开(公告)日：2016-07-20

申请号：EP14772233.4

申请日：2014-09-12

申请人： Bial-Portela & CA, S.A.

发明人： RUSSO, Domenico ,  WAHNON, Jorge ,  MATON, William ,  WEBER, Beat T. ,  JERÓNIMO, Paula ,  SOUSA, Luísa ,  BARROCAS, Pedro ,  PIRES, Rita ,  LIMA, Ricardo ,  VASCONCELOS, Teófilo

IPC分类号： C07D311/12 ,  C07D311/20

CPC分类号： C07D311/58 ,  C07C51/41 ,  C07D311/12 ,  C07D311/20 ,  C07D405/04

摘要： The present invention provides a compound of formula N wherein: X is CH
2 , oxygen or sulphur; R
1 , R
2 and R
3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine-ß-hydroxylase.