发明名称 PROCESS FOR THE PREPARATION OF A THIOPRECURSOR FOR STATINS
摘要 The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.
申请公布号 US2014343292(A1) 申请公布日期 2014.11.20
申请号 US201214363986 申请日期 2012.12.06
申请人 DSM Sinochem Pharmaceuticals Netherlands B.V. 发明人 De Lange Ben;Heemskerk Dennis;Bessembinder Karin Henderika Maria
分类号 C07D417/12;C07D405/12 主分类号 C07D417/12
代理机构 代理人
主权项 1. A method for the preparation of a compound of general formula (2)wherein R2 and R3 each independently stand for an alkyl with 1 to 12 carbon atoms, an alkenyl with 1 to 12 carbon atoms, a cycloalkyl with 3 to 7 carbon atoms, a cycloalkenyl with 3 to 7 carbon atoms, an aryl with 6 to 10 carbon atoms or an aralkyl with 7 to 12 carbon atoms, wherein each of R2 and R3 may be substituted and wherein R2 and R3 may form a ring together with the carbon atom to which they are bound and wherein R4 is an alkyl or alkenyl group with 1 to 6 carbon atoms and wherein R5 is an aryl group, comprising the steps of: (a) mixing a compound of general formula R5—SH with a base; (b) adding to the mixture obtained in step (a) water and a compound of general formula (4) wherein X is halogen; (c) adding during and/or following step (b) an alcohol of general formula R4—OH; (d) adding an acetal or an alkoxy-alkene or a ketone and removing water prior to, during or after said adding (e) adding an acid to the mixture obtained in step (c) and/or step (d)
地址 Delft NL