Method of producing aroyl-benzfurane- or aroylbenzthiophenacetic acid or its pharmaceutically accept

专利摘要:
Novel aroyl-substituted benzofuran and benzothiophene acetic and propionic acids of the formula: or a pharmaceutically acceptable salt wherein: R, is hydrogen, hydroxy, C1-6 alkoxy, or methyl; R. is hydrogen or methyl; R3 is hydrogen, C1-12 alkyl, phenyl, phenyl Ci-6 alkyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, wherein the R groups are the same and are C1-6 alkyl; X, is oxygen or is sulfur if R, is hydrogen; X2 is oxygen or sulfur; Ar is phenyl unsubstituted or independently substituted with one or more substituents which are C1-6 alkyl, C1-6 alkoxy, halo, C1-6 alkyl sulfinyl, Ci-6 alkyl sulfonyl, C1-6 alkyl thio, or 2-furyl, 3-furyl, 2-thienyl, or 3-thienyl; and the dotted line represents a single or double bond. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
公开号:SU1614762A3
申请号:SU864024097
申请日:1986-02-07
公开日:1990-12-15
发明作者:Патрик ДАНН Джеймс
申请人:Синтекс (Ю.С.А.) Инк. (Фирма)；
IPC主号:

专利说明:

table 2

权利要求:
Claims (1)
[1]
Claim
The method of obtaining aroylbenzofuran - or aroylbenzothiopheneacetic acid of General formula
7
1614762
eight
where Ar is unsubstituted phenyl or phenyl, substituted by halogen, lower-C ₆ -alkyl, lower C ^ -Cb-thioalkyl;
X - O or 5,
or its pharmaceutically acceptable salts, characterized in that the compound of General formula
where X has the specified value;
To - lower C, -C ₆ -alkyl, is subjected to interaction with haloan
^e hydride AGS acids of general formula (G) HA1, wherein Ar is as defined above, in an organic stretched at reflux the reaction voritelya
ΙΦ mixture in the presence of Lewis acids as a catalyst, followed by conversion of the resulting product to the corresponding acid or pharmaceutically acceptable salt.
Table 1
Compounds of General Formula (I) Anti-inflammatory activity (Phenilbutazone = 1) ^Ag _________! Phenyl 0 one 4-CH3 5-Phenyl 0 1.5 4-C1-phenyl 0 0.5 4-C1-phenyl five 1.5
table 2
The compound of formula (I)
Analgesic (Aspirin =
activity
one)
Phenyl 0 25 4-CH * 5-Phenyl 0 95 4-C1-Phenyl 0 32 4-C 1-Phenyl 5 7 4-CH * 5-Phenyl * 0 95
* Compound as sodium salt.

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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US51354583A| true| 1983-07-14|1983-07-14|

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