发明名称 Process for the preparation of ranitidine or acid addition salts thereof, and intermediates for this preparation.
摘要 <p>Ranitidine, which has the formula &lt;CHEM&gt; is prepared by reaction of N-[2-[[[5-(hydroxymethyl)-2-furanyl]methyl]thio]ethyl]-N'-methyl-2-nit ro-1,1-eth enediamine, which has the formula &lt;CHEM&gt; in an organic solvent, e.g. dimethylformamide, with dimethylamine and an N,N-(dimethylamino)-triphosphoniumhalide having the formula (C6H5)3 @NMe2, Hal&lt;-&gt; wherein Hal denotes bromo or chloro. The starting material (V) can be prepared in good yield and few reaction steps from known and readily available materials, and the overall synthesis of ranitidine therefore can take place from readily available raw materils in technically simple reaction steps and it gives a good yield of ranitidine in high purity without using complicated purification methods. The invention also relates to the compound (V), which is novel, and the direct starting compound for the preparation of (V), viz. N-[2-[[[5-(hydroxymethyl)-2-furanyl]methyl]thio]ethyl]-1-methylthio-2- nitroethen eamine having the formula (IV) &lt;CHEM&gt; s</p>
申请公布号 EP0219225(A1) 申请公布日期 1987.04.22
申请号 EP19860306998 申请日期 1986.09.10
申请人 A/S GEA FARMACEUTISK FABRIK 发明人 ALHEDE, BORGE;CLAUSEN, FINN PRIESS
分类号 C07D307/42;C07D307/52;(IPC1-7):C07D307/42 主分类号 C07D307/42
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