Diphenoxyacetic acid derivatives

Details Diphenoxyacetic acid derivatives Diphenoxyacetic acid derivatives

1974-12-11

1977-09-27

Killos, Paul J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

260287R, 26029382, 26029383, 260327R, 2603455, 260520C, 2605017, 2605012, 424258, 424267, 424289, C07G 6976

Patent

active

040511707

ABSTRACT:
Diphenoxyacetic acid derivatives of the general formula ##STR1## wherein R.sub.1 is H or alkyl of 1-4 carbon atoms, R.sub.2 is H or Cl, R.sub.2 is H or Cl, R.sub.3 is piperidino, 4-piperidinophenyl, 1,2,3,4-tetrahydroquinolino, 1-R.sub.4 -1,2,3,4-tetrahydro-4-quinolyl, 4-oxo-1,2,3,4-tetrahydroquinolino, 4-chromanyl, 4-thiochromanyl or 4-chlorophenoxy, and R.sub.4 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 ##STR2## with a compound of the formula ##STR3## wherein X is OH, esterified OH, Cl, Br or I, one R is R.sub.2 and the other is R.sub.3 ; or by cyclizing a compound of the formula ##STR4## wherein X.sub.1 is Cl, Br, I, NH.sub.2 OH or an esterified or etherified OH-group and n is 0 or 1; or by treating a compound of the formula ##STR5## wherein Z is a functionally modified carboxyl group different from COOR.sub.1, with a solvolyzing agent, R.sub.1, R.sub.2 and R.sub.3 in each instance having the values given above.

REFERENCES:
patent: 3454581 (1969-07-01), Groit
patent: 3474128 (1969-10-01), Griot
patent: 3517051 (1970-06-01), Bolhofer
patent: 3526632 (1970-09-01), Griot
patent: 3546229 (1970-12-01), Groit
patent: 3681365 (1972-08-01), Griot
patent: 3707549 (1972-12-01), Mills

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