公开(公告)号：EP2581375A2

公开(公告)日：2013-04-17

申请号：EP11791980.3

申请日：2011-06-13

申请人： Medichem, S.A.

发明人： SOLDEVILLA MADRID, Nuria ,  VÁZQUEZ MARTÍNEZ, Manel

IPC分类号： C07D471/08

CPC分类号： A61K31/504 ,  C07D471/08

摘要： The present invention provides an improved method for preparing a compound of formula (IIIA), which is a varenicline synthesis intermediate. Furthermore, the present invention provides an improved method for preparing varenicline, or a salt or a solvate thereof. Moreover, the present invention provides a process for decolouring varenicline, or a salt or a solvate thereof. Moreover, the present invention provides a process for preparing varenicline L-tartrate, with an improved yield. Moreover, the present invention relates to the use of a compound of formula (V), or a salt or a solvate thereof, as reference marker and reference standard for evaluating the purity of varenicline, or a salt or a solvate thereof.

摘要翻译： 本发明提供了制备式（IIIA）化合物的改进方法，其为伐伦尼克合成中间体。 此外，本发明提供了制备伐伦尼克或其盐或溶剂合物的改进方法。 此外，本发明提供一种脱色伐伦碱或其盐或溶剂合物的方法。 此外，本发明提供了一种以提高的产率制备L-酒石酸伐伦碱的方法。 此外，本发明涉及式（V）化合物或其盐或溶剂合物作为评价伐伦尼克或其盐或溶剂化物的纯度的参考标准和参考标准的用途。