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PROCESS FOR THE PREPARATION OF 4-AMINOINDANE DERIVATIVES AND RELATED AMINOINDANE AMIDES

机译:制备4-氨基茚满衍生物和相关的氨基茚满酰胺的方法

摘要

A process for preparation of 4-aminoindane compounds of a first formula, salts and enantiomers thereof including: a) hydrogenating a 1,2-dihydroquinoline of a second formula to give a corresponding tetrahydroquinoline of a third formula; b) acylating the tetrahydroquinoline of the third formula with a carboxylic acid derivative of a fourth formula to obtain a corresponding acyl derivative compound of a fifth formula; c) rearranging the acyl derivative compound of the fifth formula under acidic conditions so as to give an acyl indane compound of a sixth formula or an addition salt thereof; and d) hydrolysing the acyl group of the acyl indane compound of the sixth formula so as to obtain the 4-aminoindane derivatives of the first formula.
机译:一种第一式的4-氨基茚满化合物,其盐和对映体的制备方法,包括:a)将第二式的1,2-二氢喹啉加氢,得到相应的第三式的四氢喹啉; b)将第三式的四氢喹啉与第四式的羧酸衍生物酰化,得到相应的第五式的酰基衍生物化合物; c)在酸性条件下重新排列第五式的酰基衍生物化合物,得到第六式的酰基茚满化合物或其加成盐; d)水解第六式的酰基茚满化合物的酰基,以获得第一式的4-氨基茚满衍生物。

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