发明名称 |
METHOD FOR PREPARATION OF COMPOUNDS USEFUL FOR PREVENTION AND TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS |
摘要 |
Patients susceptible to or suffering from central nervous system are treated by administering an effective amount of an aryl substituted olefinic amine compound, such as (E)-metanicotine. (E)-metanicotine is provided from nicotine. Nicotine is reacted with ethyl chloroformate to produce ethyl. N-methyl-N-[4-chloro-4-(3-pyridyl)butyl]carbamate, which then is reacted in the presence of potassium tertbutoxide, tetrahydrofuran and dimethylformamide to produce (E)-metanicotine N-ethyl carbamate, which then is subjected to hydrolysis using hydrochloric acid to produce a reaction mixture containing (E)-metanicotine. The reaction mixture containing (E)-metanicotine is adjusted to a slightly basic pH, and then contacted with dichloromethane. The resulting water immiscible phase then is separated from the aqueous phase. The aqueous phase, then is adjusted to a very basic pH, and then contacted with methyl tert-butyl ether. (E)-metanicotine is taken up by the methyl tert-butyl ether, and after separation of the methyl tert-butyl ether from the aqueous phase, the desired product is separated from the methyl tert-butyl ether.
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申请公布号 |
WO9740013(A1) |
申请公布日期 |
1997.10.30 |
申请号 |
WO1997US06573 |
申请日期 |
1997.04.22 |
申请人 |
R.J. REYNOLDS TOBACCO COMPANY;RUECROFT, GRAHAM;WOODS, MARTIN |
发明人 |
RUECROFT, GRAHAM;WOODS, MARTIN |
分类号 |
C07D213/38;C07D213/61;(IPC1-7):C07D213/62 |
主分类号 |
C07D213/38 |
代理机构 |
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