Diphenoxyacetic acid derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 57/00 (2006.01) C07C 51/08 (2006.01) C07C 59/68 (2006.01) C07C 59/70 (2006.01) C07C 69/76 (2006.01) C07D 215/06 (2006.01) C07D 215/14 (2006.01) C07D 215/233 (2006.01) C07D 295/096 (2006.01) C07D 295/14 (2006.01) C07D 311/58 (2006.01) C07D 335/06 (2006.01)

Patent

CA 1049529

A B S T R A C T Diphenoxyacetic acid derivatives of the general formula Image wherein R1 is H or alkyl of 1-4 carbon atoms, 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-chroma- nyl, 4-thiochromanyl or 4-chlorophenoxy, and R4 is H or alkyl of 1-4 carbon atoms, and the physiologically acceptable salts thereof have been found to possess cholesterol level lowering activity. They may be prepared by react- ing a phenol of the formula Image ABSTRACT OF THE DISCLOSURE - continued 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 wherein X1 is Cl, Br, I, NH2, 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.

215506

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