摘要 |
Diphenoxyacetic acid derivatives of the general formula <IMAGE> wherein R1 is H or alkyl of 1-4 carbon atoms, R2 is H or Cl, R2 is H or Cl, R3 is piperidino, 4-piperidinophenyl, 1,2,3,4-tetrahydroquinolino, 1-R4-1,2,3,4-tetrahydro-4-quinolyl, 4-oxo-1,2,3,4-tetrahydroquinolino, 4-chromanyl, 4-thiochromanyl or 4-chlorophenoxy, and R4 is H or alkyl of 1-4 carbon atoms, and the physiologically acceptable salts thereof, possess cholesterol level lowering activity and can be prepared by reacting a phenol of the formula <IMAGE> with a compound of the formula <IMAGE> wherein X is OH, esterified OH, Cl, Br or I, one R is R2 and the other is R3; or by cyclizing a compound of the formula <IMAGE> +tr <IMAGE> wherein X1 is Cl, Br, I, NH2+L, OH or an esterified or etherified OH-group and n is 0 or 1; or by treating a compound of the formula <IMAGE> wherein Z is a functionally modified carboxyl group different from COOR1, with a solvolyzing agent, R1, R2 and R3 in each instance having the values given above.
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申请人 |
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG |
发明人 |
SCHACHT, ERICH;MEHRHOF, WERNER;SIMANE, ZDENEK;KAYSER, DETLEV;NOWAK, HERBERT |