发明名称 Convenient Process for the Preparation of Statins
摘要 Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.
申请公布号 US2015344439(A1) 申请公布日期 2015.12.03
申请号 US201414395703 申请日期 2014.02.11
申请人 F.IS.- FABBRICA ITALIANA SINTETICI S.P.A. 发明人 DE LUCCHI Ottorino;TARTAGGIA Stefano;FERRARI Clark;GALVAGNI Marco;PONTINI Marta;FOGAL Stefano;MOTTERLE Riccardo;MORENO Rosa Maria;COMELY Alex
分类号 C07D239/42;C07D209/24;C07D215/14;C07F7/18;C07D317/30 主分类号 C07D239/42
代理机构 代理人
主权项 1. A process for preparing a compound of formula (I): wherein Z is chosen from OH, O−, OR, SR, O(CO)OR, NH2, NHR, and NR2, wherein R is chosen from linear or branched C1-7 alkyl, linear or branched C1-7 alkenyl or alkynyl, C3-7 cycloalkyl, and aryl-C0-4 alkyl, andwherein in NR2 the two R groups are optionally joined, forming a C2-10 alkyl or alkenyl ring; PG is a hydroxyl protecting group chosen from tetrahydropyranyl (THP), camphanoyl, bornyl, menthyl, R, (CO)R, CH2OR, CH2SR, and SiR3, wherein R in SiR3 is the same or different, and is chosen from linear or branched C1-7 alkyl, linear or branched C1-7 alkenyl or alkynyl, C3-7 cycloalkyl, and aryl-C0-4 alkyl; and Q is chosen from the following radicals: wherein the symbol * specifies the bonding position; R1 is hydrogen or methyl; and R2 is chosen from hydrogen, methyl, hydroxyl, hydroxymethyl, and O-PG wherein, PG is as defined above; the process comprising reacting a compound of formula (II): wherein PG and Z are as defined for the compound of formula (I), with a compound of formula (III): wherein Q is as defined for the compound of formula (I).
地址 Montecchio Maggiore IT