C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
260/602.2, 260/4
C07C 69/76 (2006.01) A01N 33/02 (2006.01) A01N 37/30 (2006.01) A61K 31/13 (2006.01) A61K 31/135 (2006.01) A61K 31/165 (2006.01) A61K 31/215 (2006.01) A61K 31/24 (2006.01) C07C 69/14 (2006.01)
Patent
CA 1052387
ABSTRACT OF THE DISCLOSURE This invention relates to a process for the preparation of new amines of the formula Image wherein R is selected from the group consisting of cycloalkyl having at most 6 carbon atoms or Image wherein R2 is selected from the group consisting of hydrogen and hydroxy, whereby R4 is selected from the group consisting of Image ; Image ; when R2 is hydrogen, and whereby R4 is selected from the group consisting of Image ; or Image when R2 is hydroxy, and R3 is selected from the group consisting of hydrogen and methyl, R is selected from the group consisting of hydrogen and benzyl, and R6 is selected from the group consisting of hydrogen, and halogen, chara- cterized in that a) a compound of the formula II Image wherein R and R have the meanings given above X1 is a hydroxy group and Z is a reactive, esterified hydroxy group, or X1 and Z together form an epoxy group is reacted with an amine of the formula NH2-R, wherein R has the same meanings as given above, or b) a compound of the formula III Image wherein R1 and R6 have the meanings given above is reacted with a compound of the formula Z-R, wherein R and Z have the same meanings as given above, except for the case when R3 is methyl c) a compound of the formula IV Image (IV) wherein R1 and R6 have the same meanings as given above is reacted with a compound of formula V Image (V) wherein Z, X1 and R have the same meanings as given above, or d) a compound of the formula IV Image (IV) wherein R1 and R6 have the same meanings as given above is reacted with a compound of the formula VI Image (VI) wherein R has the same meaning as given above, e) from a compound of the formula Image wherein R, R1 and R6 have the meanings given above and R10 is a protecting group of the group consisting of benzyl, acyl, arylsulphonyl, cyano, silyl, substituted methylene, substituted carbonyl, carbamoyl, the protecting group - 2 - being split off by means of solvolysis, reduction, pyrolysis or fermentation, of f) a Schiffs' base of the formula VIII or IX Image (VIII) Image (IX) or a cyclic tautomer of formula X corresponding to the compound of formula IX Image (X) wherein R1 and R6 have the same meanings as above except for the case when R3 is methyl and R'H is the same as R, and whereby the compounds IX and X may be present simultaneously, is reduced, or g) in a compound of the formula XI Image (XI) wherein R, R1 and R6 have the same meanings as above, the oxo group is reduced to a hydroxy group, or h) reducing a compound of formula XIII Image (XIII) wherein R1, R6 and R have the meanings given above, by means of a complex metalhydride, if desired, isomer mixtures obtained are separated into pure isomeres, and/or racemates obtained are separated into optical antipodes and/or free bases obtained are transformed into their therapeutically acceptable salt or salts obtained are transformed into their free bases. The substances of this invention constitute such agents according to the results obtained in animal experiments. The positively acting effect of these substances depends - 3 - on the activation of the adrenergic receptors which control the contractility of the heart. - 4 -
220014
Carlsson Enar I.
Persson Nils H.a.
Samuelsson Gustav B. R.
Wetterlin Kjell I. L.
Ab Hassle
Na
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