Anthelmintic 2-(5-nitro-2-thienyl)-4-(substituted amino)quinazolines.
Anthelmintic 2-(5-nitro-2-thienyl)-4-(substituted amino)quinazolines.
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DOI：
10.1021/jm00271a036
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发表时间：
1972
影响因子：
7.3
通讯作者：
R. Alaimo
中科院分区：
文献类型：
--
作者：
R. Alaimo
The general method for the preparation of the amino compounds 6-24 involves displacement of the activated 4-C1 atom in 4-chloro-2-(5-nitro-2-thienyl) quinazolines 5a or 5b by a variety of amines in DMF solution. Thesynthesis of 5a and 5b involves the reaction of 5-nitro-2-thiophenecarboxaldehyde (1) with an anthranilamide (2a or 2b) in acidic EtOH. The resulting dihydroquinazolinone (3a or 3b) is oxidized to the correspondingquinazolinone (4a or 4b) with p-benzoquinone. Chlorination of the quinazoli-nones with PC1S in POCl3 results in the formation of 5a or 5b in moderate yield. Thesyntheses of 5a and 5b and 6-24 are outlined in Scheme I.
