发明名称 Isoxazoles, useful as antiviral agents, and preparation thereof.
摘要 <p>Compounds of the Formulas I or II (herein) wherein R is alkyl, X is 0 or CH&lt;Sub&gt;2&lt;/Sub&gt;, n is an integer from 4 to 8, and Ar is phenyl or substituted phenyl, useful as antiviral agents especially against picornaviruses. Said compounds are prepared by: &lt;UnorderedLists id="ula01" listStyle="none"&gt;&lt;ListItem&gt;a) reacting an alkali metal derivative of 3-R-5-methylisoxazole with a compound of the formula Hal-(CH&lt;Sub&gt;2&lt;/Sub&gt;)&lt;Sub&gt;n&lt;/Sub&gt;-X-AR' where Hal is bromine or iodine, and Ar' is phenyl or phenyl substituted by one or two halogen, lower-alkyl, lower-alkoxy, nitro or cyano substituents to produce a compound of the Formula (I) wherein Ar is phenyl or phenyl substituted by one or two substituents which are halogen, lower-alkyl, lower-alkoxy, cyano or tertiary-butyloxy-carbonyl; or&lt;/ListItem&gt;&lt;ListItem&gt;b) reacting a compound of the formula &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="14" wi="105" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;where Hal is bromine or iodine, with an alkali metal salt of a compound of the formula &lt;Chemistry id="chema02" num="0002"&gt;&lt;Image id="ia02" he="7" wi="32" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;where Ar' has the meaning given above, followed by optimal conversions of the phenyl substituents of Ar.&lt;/ListItem&gt;&lt;/UnorderedLists&gt;</p>
申请公布号 EP0111345(A2) 申请公布日期 1984.06.20
申请号 EP19830112541 申请日期 1983.12.13
申请人 STERLING DRUG INC. 发明人 DIANA, GUY DOMINIC
分类号 C07D261/08;(IPC1-7):07D261/08;61K31/41 主分类号 C07D261/08
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