公开(公告)号：US08143400B2

公开(公告)日：2012-03-27

申请号：US12007394

申请日：2008-01-10

申请人： Svetoslav S. Bratovanov ,  Elena Bejan ,  David A. Stradiotto ,  Abbulu Kante ,  Zhi-Xian Wang ,  Stephen E. Horne

发明人： Svetoslav S. Bratovanov ,  Elena Bejan ,  David A. Stradiotto ,  Abbulu Kante ,  Zhi-Xian Wang ,  Stephen E. Horne

IPC分类号： C07D401/14

CPC分类号： C07D497/20

摘要： An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine from a cis/trans mixture of isomers. Treatment of the mixture with an organic sulfonic acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.

摘要翻译： 从异构体的顺/反混合物制备和纯化顺式-2-甲基螺（1,3-氧硫杂环戊烷-5,3'）奎宁啶的工业上可接受的方法。 用有机磺酸处理混合物产生富含顺式异构体的较不溶性的酸加成盐。 使用各种有机溶剂的重结晶或制浆允许通过过滤富集顺式异构体。 根据本发明制备的2-甲基螺旋（1,3-氧硫杂环戊烷-5,3'）奎宁啶的顺式异构体的这些新的磺酸盐可以通过任何已知的方法进一步转化成盐酸盐，例如用 碱，然后与盐酸形成盐酸盐或与盐酸交换磺酸盐。

公开(公告)号：US20090182146A1

公开(公告)日：2009-07-16

申请号：US12007394

申请日：2008-01-10

申请人： Svetoslav S. Bratovanov ,  Elena Bejan ,  David A. Stradiotto ,  Abbulu Kante ,  Zhi-Xian Wang ,  Stephen E. Horne

发明人： Svetoslav S. Bratovanov ,  Elena Bejan ,  David A. Stradiotto ,  Abbulu Kante ,  Zhi-Xian Wang ,  Stephen E. Horne

IPC分类号： C07D497/20

CPC分类号： C07D497/20

摘要： An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine from a cisitrans mixture of isomers. Treatment of the mixture with an organic sulfonice acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.

摘要翻译： 从异构体的顺式异构体混合物制备和纯化顺式-2-甲基螺（1,3-氧硫杂环戊烷-5,3'）奎宁啶的工业上可接受的方法。 用有机磺酸处理混合物产生富含顺式异构体的较不溶性的酸加成盐。 使用各种有机溶剂的重结晶或制浆允许通过过滤富集顺式异构体。 根据本发明制备的2-甲基螺旋（1,3-氧硫杂环戊烷-5,3'）奎宁啶的顺式异构体的这些新的磺酸盐可以通过任何已知的方法进一步转化成盐酸盐，例如用 碱，然后与盐酸形成盐酸盐或与盐酸交换磺酸盐。