发明名称 METHOD OF OBTAINING 2-AMINO-6-ALKYL-AMINO-4,5,6,7-TETRAHYDROBENZOTHIAZOLES
摘要 <p>The invention relates to a method of preparing 2-amino-6-alkyl-amino-4,5,6,7-tetrahydrobenzothiazoles having formula (I), wherein the asterisk (*) represents an asymmetrical carbon and R&lt;SUP&gt;1&lt;/SUP&gt; is alkyl C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;, the enantiomers or mixtures thereof, the pharmaceutically-acceptable solvates, hydrates or salts of same. The inventive method comprises the following steps consisting in: (a) reacting a compound (II) with a secondary amine, optionally in the presence of an acid and a solvent 1, in order to form an enamine; (b) optionally removing the acid and solvent 1 and, subsequently, reacting the enamine with sulphur in the presence of a solvent 2; and (c) reacting the previously obtained compound with cyanamide in order to obtain compound (I). Compounds having formula (I) include pramipexol which is a compound with dopamine D2 agonist activity that can be used for the treatment of Parkinson's disease and schizophrenia.</p>
申请公布号 WO2006003220(A1) 申请公布日期 2006.01.12
申请号 WO2005ES00362 申请日期 2005.06.24
申请人 RAGACTIVES, S.L.;PASCUAL COCA, GUSTAVO;MARTIN JUAREZ, JORGE 发明人 PASCUAL COCA, GUSTAVO;MARTIN JUAREZ, JORGE
分类号 (IPC1-7):C07D277/82;C07C211/40;A61K31/429;A61P25/18;A61P25/28;C07C225/20;C07C321/22 主分类号 (IPC1-7):C07D277/82
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