INDUSTRIAL PROCESS FOR PREPARATION OF 1,2-DIHYDROQUINOLINE DERIVATIVE OR A SALT THEREOF, AND INTERMEDIATE FOR PREPARATION THEREOF
申请人:SANTEN PHARMACEUTICAL CO., LTD.
公开号:US20140371459A1
公开(公告)日:2014-12-18
Provided is a method for producing a compound represented by formula (7) or a salt thereof:
the method comprising the steps of:
removing a R
1
group and a R
2
group from a compound represented by formula (5) or a salt thereof:
and
reacting the compound (in which R1 and R2 in formula (5) are hydrogen atoms) obtained in the removing step or a salt thereof with a compound represented by formula (d):
or a salt thereof in the presence of a base. The method is a method for producing a 1,2-dihydroquinoline derivative having glucocorticoid receptor binding activity or a salt thereof. This method does not require a purification step by column chromatography and is suitable for industrial production.
提供了一种生产由式(7)或其盐所表示的化合物的方法:该方法包括以下步骤:从由式(5)或其盐所表示的化合物中去除R1基团和R2基团;并在碱的存在下,将在去除步骤中获得的化合物(其中式(5)中的R1和R2为氢原子)或其盐与由式(d)或其盐所表示的化合物反应。该方法是一种生产具有糖皮质激素受体结合活性的1,2-二氢喹啉衍生物或其盐的方法。该方法不需要经过柱层析纯化步骤,适用于工业生产。