Method for producing a N- substituted glycine derivatives -n- cyclopentyl

摘要

Novel compounds possessing both angiotensin enzyme inhibitory activity and diuretic activity are disclosed. The compounds are represented by the general formulain which R¹, R₂, R₃, R₄, R_s and R₆ are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, and cycloalkyl, and may be the same or different; n is an integer from 0 to 4 inclusive; M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl, or M and R₆ taken together with the nitrogen to which M is bonded and the carbon to which R₆ is bonded from a saturated unsubstituted heterocyclic group containing 3 or 4 ring carbon atoms; Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy; Z, and Z₂ each is a chemical bond, the group X₃-(CH₂)_m, an amino acid group or the group X₃-(CH₂)_m-X₃ wherein X₃ is oxygen, sulfur or NH and m is an integer from 0 to 4 inclusive; A and B each is the same as R, or halogen, trifluoromethyl, OR₁, NO₂, NR₁R₂, SO₂NH₂, CN, SR₁, SOR₁, SO₂R₁, CONR₁R₂, COOR,; C is hydrogen alkyl, heteroallyl, amino, -CR₁=CR₂-,aminoalkyl, furfurylmethylamino, aminorayl or aminobenzyl; X, and X₂ are each S, SO, SO₂, NR₁, O, chemical bond, (CR₉R₁₀)_m, -CR₉=CR₁₀, and CHOH, with the proviso that at least one of X, and X₂ be (CR₉R₁₀)_m, wherein R₉ and R₁₀ are each hydrogen or lower alkyl, and m is an integer from 1 to 5; Ar is a divalent arylene or heteroarylene; and R, and R₈ are each hydrogen, alkyl, halo, cyano, hydroxy, alkoxy, amino, alkylamino, dialkylamino, mercapto, alkylmercapto, nitro, trifluoromethyl, carboxy, carbalkoxy, COY and NHCONHR, wherein R, and Y are as hereindefined; and pharmaceutically-acceptable salts thereof.