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61. 发明公开

EP1697313A2 PROCESSES FOR THE PREPARATION OF AMINOALKYL PHENYLCARBAMATES 有权转让
标题翻译：制备氨基烷基苯基氨基甲酸酯的方法
公开(公告)号：EP1697313A2
公开(公告)日：2006-09-06
申请号：EP04806260.8
申请日：2004-12-17
申请人： Generics (UK) Limited
发明人： GAITONDE, Abhay , MANGLE, Mangesh , PAWAR, Sanjay, R.
IPC分类号： C07C269/02 , C07C269/04 , C07C269/06 , C07C269/08 , C07C271/44 , A61K31/27
CPC分类号： C07C269/06 , C07C269/00 , C07C271/44
摘要： The present invention relates to a process for preparing an aminoalkyl phenylcarbamate (4), comprising the steps of converting a hydroxy phenyl ketone (2) to a phenylcarbamate ketone (3), and converting the phenylcarbamate ketone (3) to the desired aminoalkyl phenylcarbamate (4). Optionally the aminoalkyl phenylcarbamate (4) may be resolved into its enantiomers and/or converted into a pharmaceutically acceptable acid addition salt. The invention further relates to aminoalkyl phenylcarbamates (4) and pharmaceutically acceptable salts prepared by the above process, in particular, to rivastigmine (1) and rivastigmine hydrogen tartrate (9). The aminoalkyl phenylcarbamates (4) may be comprised in pharmaceutical compositions. The invention further relates to a method of inhibiting acetylcholine esterase or treating dementia, senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesias, hyperkinesia, a confusion disorder, ataxia, Friedrich's ataxia, Down's syndrome, mania or an acute confusion disorder, using the aminoalkyl phenylcarbamates (4) of the present invention.
摘要翻译：本发明涉及制备氨基烷基苯基氨基甲酸酯（4）的方法，包括将羟基苯基酮（2）转化为苯基氨基甲酸酯酮（3），并将苯基氨基甲酸酯酮（3）转化为所需的氨基烷基苯基氨基甲酸酯 4）。任选地，可将氨基烷基苯基氨基甲酸酯（4）拆分成其对映异构体和/或转化成药学上可接受的酸加成盐。本发明还涉及氨基烷基苯基氨基甲酸酯（4）及通过上述方法制备的药学上可接受的盐，特别是卡巴拉汀（1）和利凡斯的明酒石酸氢盐（9）。氨基烷基苯基氨基甲酸酯（4）可以包含在药物组合物中。本发明进一步涉及抑制乙酰胆碱酯酶或治疗痴呆，老年性痴呆，阿尔茨海默病，亨廷顿氏舞蹈症，迟发性运动障碍，运动过度，混乱障碍，共济失调，弗里德里希共济失调，唐氏综合征，躁狂或急性混乱障碍的方法，氨基烷基苯基氨基甲酸酯（4）。

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