首页> 外国专利> PROCESS FOR THE PREPARATION OF CIS-1-amino-2-indanol from trans-1-AMIDO-2-HALOINDAANVERBINDING, TRANS-1-AMINO-2-HALOINDAANVERBINDINGEN AND PROCESS FOR THE PREPARATION OF TRANS-1-AMIDO-2-HALOINDAANVERBINDINGEN .

PROCESS FOR THE PREPARATION OF CIS-1-amino-2-indanol from trans-1-AMIDO-2-HALOINDAANVERBINDING, TRANS-1-AMINO-2-HALOINDAANVERBINDINGEN AND PROCESS FOR THE PREPARATION OF TRANS-1-AMIDO-2-HALOINDAANVERBINDINGEN .

机译:由反式1-氨基2-卤代吲哚结合,反式1-氨基2-卤代吲哚丁烯制备CIS-1-氨基-2-茚满醇的工艺及反式1-氨基-2-卤代吲哚丁烯的制备工艺。

摘要

The invention relates to a process for the preparation of cis-1-amino-2-indanol, wherein first a trans-1-amido-2-haloindane according to formula 1, wherein X is a halogen, in particular Br, and R an alkyl alkenyl or aryl group, preferably methyl, is cyclized under acidic conditions and optionally then subjected to a, preferably acidic, hydrolysis. The invention also relates to trans-1-amido-2-haloindane compounds of the formula 1, in particular trans-1-acetamido-2-bromoindane, and processes for the preparation of a trans-1-amido-2-haloindane of the formula 1 wherein the corresponding trans-2-halo-1-indanol is contacted with a nitrile of formula RC = N or in which indene is contacted with a donor of a positive halogen and a nitrile of formula RC = N, both in the presence of an acid, for example sulfuric acid. A particularly attractive process for the preparation of cis-1-amino-2-indanol is to obtain indanol without intermediate isolation of the intermediately formed products. Cis-1-amino-2-indanol, in particular optical active cis- (2R, 1S ..
机译:本发明涉及一种制备顺式-1-氨基-2-茚满醇的方法,其中首先是根据式1的反式-1-酰胺基-2-卤代茚满,其中X是卤素,特别是Br,R是烷基烯基或芳基,优选甲基,在酸性条件下被环化,然后任选进行优选为酸性的水解。本发明还涉及式1的反式-1-酰胺基-2-卤代茚满化合物,特别是反式-1-乙酰氨基-2-溴代茚满,以及制备该化合物的反式-1-酰胺基-2-卤代茚满的方法。式1,其中相应的反式-2-卤-1-茚满醇与式RC = N的腈接触,或其中茚与正卤素供体和式RC = N的腈接触,都在存在下酸,例如硫酸。制备顺式-1-氨基-2-茚满醇的一种特别有吸引力的方法是获得茚满醇,而无需中间分离中间形成的产物。顺式-1-氨基-2-茚满醇,尤其是旋光性顺式(2R,1S ..

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