| 摘要 |
Amidines (I; R1 = lower alkylthio-substituted ph; R2 = ester; ficated or amidified 1-carboxy-lower alkyl; ph = substd. 1,2-phenylene; alk = C1-3 aliphatic hydrocarbon radical; R1' = lower alkanesulphinyl or lower alkanesulphonyl-substituted ph) were prepd. by the reduction of II in the presence of reductant. Thus, 172 g 2-((p- methanesulphinylbenzoylamino)-ethyl)-5-fluoro-indole3-acetic acid ethylester was refluxed with PCl3 for 3 hrs. to give 7-fluoro-1-(p- methanesulfinyl-phenyl)-3,4-dihydro-pyrimido(1,6-a)indole-5-acetic acid ethylesterhydrochloride, which was refluxed in the presence of activated nickel-contained ethylacetate to give 7-fluoro-1-(p- methylthio-phenyl)-3,4-dihydro-pyrimido (1,6-a)indole-5-acetic acid ethylester.
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