Method for preparing arylaminopropanol

Method for preparing arylaminopropanol

  • CN 1,445,224 A
  • Filed: 03/20/2003
  • Published: 10/01/2003
  • Est. Priority Date: 03/20/2002
  • Status: Active Grant
First Claim
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1. the method for the compound of the general formula (I) of preparation enantiomorph enrichmentAr-CH(OH)-CH 2-CH 2-NR 1R 2 (I) WhereinAr be replace or unsubstituted aryl andR 1And R 2Be hydrogen, C independently of one another 1-C 20-alkyl, C 4-C 14Aryl or C 5-C 15-aralkyl, perhaps two R 1And R 2Group is C together 3-C 12-alkylidene group, It is characterized in that:

  • A) compound of general formula (II) compound that is converted into the compound of enantiomorph enrichment of general formula (III) or general formula (IV) is converted into the compound of the enantiomorph enrichment of logical formula VAr-CO-CH 2-COOR 3 (II) Ar-CH(OH)-CH 2-COOR 3 (III) Ar-CO-CH 2-CONR 1R 2 (IV) Ar-CH(OH)-CH 2-CONR 1R 2 (V) Wherein, in each case,Ar as the definition under general formula (I) andR 1And R 2Each freely the definition under general formula (I) and R 3Be hydrogen, C 1-C 20-alkyl, C 4-C 14-aryl or C 5-C 15-aralkyl and Wherein this reaction is following carries out-in the presence of transition-metal catalyst-use hydrogen or hydrogen transference compound or its mixture andB) compound at general formula (II) is used under the situation of step a), the amine reaction of the compound of the enantiomorph enrichment of general formula (III) and general formula (VI)HNR 1R 2 (VI) R wherein 1And R 2Each definition under general formula (I) freely, obtain above-mentioned definition logical formula V the enantiomorph enrichment compound and C) compound of the enantiomorph enrichment of logical formula V changes into the compound of enantiomorph enrichment of the general formula (I) of above-mentioned definition by reduction.

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