Derivatives of 2-amino-1-phenyl-cyclopentanol

Details Derivatives of 2-amino-1-phenyl-cyclopentanol Derivatives of 2-amino-1-phenyl-cyclopentanol

C - Chemistry, Metallurgy

07

D

260/476.1, 260/4

C07D 303/22 (2006.01) C07D 203/26 (2006.01) C07D 209/52 (2006.01) C07D 295/096 (2006.01)

Patent

CA 1126283

A B S T R A C T Compounds are disclosed of general formula (I) Image (I) in which R1 represents a hydrogen atom, a halogen atom or a group OR2, in which R2 re- presents a hydrogen atom, an alkyl group or an acyl group, R3 represents hydrogen or an alkyl, alkenyl or aryl group, R4 and R5 which may be the same or different, each represents a hydrogen atom or an alkyl, alkenyl or alkynyl group optionally substituted by an aryl or cycloalkyl group: or R4 and R5 together with the nitrogen atom may form a saturated four to seven membered ring, with the provisos that, when R4 and R5 simultaneously represent hydrogen atoms then (i) when R1 is hydrogen then R3 is not methyl and (ii) the compounds are the B-isomers; and their physiologically acceptable salts. Compounds of formula (I) may be prepared from the corresponding a- or B-configuration alcohols, from an aziridine intermediate or by a variety of alkylation procedures whereby the group R4 and/or R5 is introduced. The compounds (I) and their salts have analgesic activity and may be formulated as pharmaceutical compositions in conventional manner.

338378

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