公开(公告)号：US20060122227A1

公开(公告)日：2006-06-08

申请号：US11235105

申请日：2005-09-27

申请人： Lior Zelikovitch ,  Oded Arad ,  Mohammed Alnabari ,  Yana Sery ,  Orna Kurlat ,  Moshe Bentolila ,  Aric Abadayev ,  Hanit Marom ,  Hila Isenberg ,  Joseph Kaspi

发明人： Lior Zelikovitch ,  Oded Arad ,  Mohammed Alnabari ,  Yana Sery ,  Orna Kurlat ,  Moshe Bentolila ,  Aric Abadayev ,  Hanit Marom ,  Hila Isenberg ,  Joseph Kaspi

IPC分类号： C07D211/06 ,  A61K31/445

CPC分类号： C07D211/34

摘要： The present invention relates to an improved process of alkylating secondary amines, more particularly of alkylating compounds having amino piperidinic group, which are useful as donepezil intermediates, wherein an alcohol serves as reaction facilitator thus enabling to obtain donepezil and salts thereof in high quality and yield. The present invention also relates to the prevention of unwanted alkylation of donepezil precursors, having amino piperidinic group, by using suitable reaction conditions.

摘要翻译： 本发明涉及一种改进的仲胺烷基化方法，更特别是烷基化化合物，具有氨基哌啶基，其可用作多奈哌齐中间体，其中醇用作反应促进剂，从而能够以高质量和产率获得多奈哌齐和其盐 。 本发明还涉及通过使用合适的反应条件来防止具有氨基哌啶基的多奈哌齐前体的不需要的烷基化。