发明名称 PROCESS FOR THE PREPARATION OF AN N-(2-BROMOALKYL)-AMIDE DERIVATE_______________________________________________________________
摘要 <p>The invention relates to a method for the preparation of an N-(2-bromoalkyl)-amido derivative according to formula (1), wherein an alkenically unsaturated compound (alkene) is brought into contact with a donor of a positive bromine ion and a nitrile in the presence of water or an acid, preferably sulphuric acid. The invention also relates to the use of an N-(2-bromoalkyl)-amido derivative thus obtained in the preparation of 1,2-aminoalcohols, β-amido-α-hydroxycarboxylic acids, β-amino acids, β-amido acids, β-aminonitriles, β-amidonnitriles, β-amido-α-hydroxynitriles, β-aminoamides, β-amidoamides or β-amido-α-hydroxyamides, in particular a method for the preparation of a 1,2-aminoalcohol, an N-(2-bromoalkyl)-amido derivative first being subjected to a ring closure, preferably under acidic conditions, and optionally subsequently being subjected to a preferably acidic hydrolysis. Such 1,2-aminoalcohols can suitably be used in the preparation of known pharmaceuticals. A particularly attractive method for the preparation of a 1,2-aminoalcohol is obtained if the total route from the alkene is carried out without the products formed intermediately being isolated in between.</p>
申请公布号 WO1997000237(A1) 申请公布日期 1997.01.03
申请号 NL1996000237 申请日期 1996.06.13
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