Derivatives of trans-3-hydroxy-4-amino-chromans

C - Chemistry – Metallurgy – 07 – D

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C07D 309/30 (2006.01) C07D 311/22 (2006.01) C07D 311/58 (2006.01) C07D 311/68 (2006.01) C07D 493/04 (2006.01)

Patent

CA 1119180

ABSTRACT OF THE DISCLOSURE Compounds of the formula (1) are disclosed Image (I) wherein R1 is a hydrogen atom or an alkyl group of up to 4 carbon atoms optionally substituted by a chlorine or bromine atom or by a hydroxyl group or by an alkoxyl group of up to 4 carbon atoms or by an acyloxy group or up to 4 carbon atoms and R2 is a hydrogen atom or an alkyl group of up to 4 carbon atoms or R1 is joined to R2 so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7- membered heteroalicyclic ring which is optionally substituted by methyl; Y is a group CO.R3, CO2R3, SO.R3, SO2.R3, SO.OR3, SO2.OR3, CH(OH)R3, C(R3)NOH, C(R3)NNH2, CO.NH2, CO.NR4R5, SO.NR4R5 or SO2NR4R5 where R3 and R4 are independently a hydrocarbon group of up to 8 carbon atoms or such a group inertly substituted by a chlorine or bromine atom or by a hydroxyl group or by an alkoxyl group of 1 - 4 carbon atoms or by acyloxy group of up to 4 carbon atoms or by 3 fluorine atoms attached to the same carbon atom and R5 is a hydrogen atom or an alkyl group of up to 4 carbon atoms; and salts thereof and O-acyl derivatives thereof wherein the O-acyl moiety contains up to 18 carbon atoms. These compounds have useful anti-hypertensive activity. Methods of preparation are also disclosed.

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