PROCESS FOR PREPARATION OF HETEROCYCLIC SPIROLINKED AMIDINES

    公开(公告)号:KR840000498B1

    公开(公告)日:1984-04-16

    申请号:KR790002987

    申请日:1979-08-31

    Applicant: HOECHST AG

    Abstract: Antidepressant amidines (I; n=1, 2; R1, R2=H, alkyl; R3=H, Me; R4=C1-4 alkyl, alkxy,methylenedioxy, hydroxy, halo, CN, NO2, MeF3, amino, C2-5 acylamino, C1-4 alkylamino, Ph, thiophene) and their 5,6,-dihydro derivs. were prepd. Thus, 3-(2-methoxyphenyl)-2-nitrobicyclo[2.2.1 hept-5-ene was treated with CH2:CHCO2Me and the resulting propionate reduced and cyclized to the ketone(III) which was thiolated, S-methylated, and aminated to give the 5,6-dihydro deriv. of I (R1R2=pyrrolidino; R3=H; R4=2-MeOC6H4).

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