Abstract:
:The synthesis of 4-Methoxyphenyl-[5-methyl-6-(2-(4-morpholinyl)-ethyl)-6H-thieno[2,3- b]pyrrol-4-yl)phenylmethanone (1), a thiophene analogue of the analgesic Pravadoline B, is described. Starting with the acetylprotected thienylhydrazine 2b compound 7 was obtained in a Fischer-analogue cyclication in two steps. Use of the BOC-protected thienylhydrazine 2a yielded the pyrazol 5. Alkylation of 7 with N-(2-Chloroethyl)morpholine gave the target compound 1. In the acetylcholine-writhing-test in mice as well as in the acetic acid-writhing-test in rats 1 showed a significant lower antinociceptive activity than Pravadolin (B).
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Binder D,Schnait H,Rovenszky F,Enzenhofer R,Stroissnig Hdoi
10.1002/ardp.19913240406subject
Has Abstractpub_date
1991-04-01 00:00:00pages
219-21issue
4eissn
0365-6233issn
1521-4184journal_volume
324pub_type
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19913240110
更新日期:1991-01-01 00:00:00
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更新日期:2020-04-01 00:00:00
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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更新日期:1999-06-01 00:00:00
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更新日期:1996-12-01 00:00:00