[EN] 4 - PIPERIDINYL COMPOUNDS FOR USE AS TANKYRASE INHIBITORS<br/>[FR] COMPOSÉS DE 4-PIPÉRIDINYLE UTILES COMME INHIBITEURS DE LA TANKYRASE
申请人:NOVARTIS AG
公开号:WO2013008217A1
公开(公告)日:2013-01-17
The present invention provides for compounds of formula (I).The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
Process for producing optically active azetidine-2-carboxylic acids
申请人:Honda Tatsuya
公开号:US20050043547A1
公开(公告)日:2005-02-24
An optically active N-protected azetidine-2-carboxylic acid (5) can be produced by preparing an optically active 4-amino-2-halobutyric acid (3) by halogenating an optically active 3-hydroxy-2-pyrrolidinone (1) with inversion of configuration to prepare an optically active 3-halo-2-pyrrolidinone (2) followed by hydrolysis or by halogenating an optically active 4-amino-2-hydroxybutyric acid ester (6) with inversion of configuration to prepare an optically active 4-amino-2-halobutyric acid ester (7) followed by hydrolysis or by halogenating the compound. (6) with inversion of configuration to prepare the compound (7), cyclizing the same to prepare the compound (2) followed by hydrolysis,
further cyclizing the compound (3) followed by treating the reaction product with an amino group-protecting agent. The thus-obtained compound (5) can be improved its optical purity further by recrystallization.