1-Cyclomexyl-carboxamido-methyl-isoquinoline derivs. mfr. - by catalytic hydrogenation of unsatd. precursors

Prepn. of 1-(cyclohexylcarboxamidomethyl) -1,2,3,4-tetrahydro- isoquinoline derivs. of formula (I) is effected by catalytic hydrogenation of isoquinoline derivs. of formula (II). R1 and R2 are H or R1+R2 is COCH2; R3, R4, R6 and R7 are H or Me; R5 is H, Me, Cl or NH2; R8 is H, OH or Me; R9 is CN nan...

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Hauptverfasser: SEUBERT,JUERGEN,DR, GOTTSCHLICH,RUDOLF,DR, KLOFT,MICHAEL,DR, POHLKE,ROLF,DR
Format: Patent
Sprache:eng ; ger
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Zusammenfassung:Prepn. of 1-(cyclohexylcarboxamidomethyl) -1,2,3,4-tetrahydro- isoquinoline derivs. of formula (I) is effected by catalytic hydrogenation of isoquinoline derivs. of formula (II). R1 and R2 are H or R1+R2 is COCH2; R3, R4, R6 and R7 are H or Me; R5 is H, Me, Cl or NH2; R8 is H, OH or Me; R9 is CN nand R10 is COR14, or R9 is CHR7-NR2-COR14 and R10 is R1; R11 and R12 are H or R11+R12 is a C-C bond; R13 is R5 or NO2; R14 is a phenyl or 1-cyclohexenyl gp. opt. substd.by OH or Me. (I; R1+R2 = COCH2) are anthelmintics useful for control of tape worms and schistosomiasis. (I; R1 = R2 = H) are intermediates for such anthelmintics. The process avoids the use of malodorous cyclohexanecarboxylic acid derivs.