DERIVATIVES OF 1-PHENOXY-3-AMINOPROPAN-2-01 AND PROCESSES FOR THEIR PREPARATION

摘要

DERIVATIVES OF 1-PHENOXY-3-AMINO-PROPAN-2-OL AND PROCESS FOR THEIR PRODUCTION The present invention relates to now pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula wherein X denotes A denotes -CH2-alkoxy, -O-alkoxyalkyl, -O-hydroxyalkyl or , R1 denotes hydrogen or methyl, denotes an aromatic or quasi -aromatic, 5- membered or 6-membered, monocyclic ring which is linked through a C atom which has one or 2 nitrogen, oxygen and/or sulphur hetero -atoms and which can be substituted additionally by one or more methyl groups, and R2 and R3 denote hydrogen, alkyl, alkenyl or cycloalkyl or, conjointly with the N atom to which they are linked and,optionally,with a further oxygen or sulphur hetero-atom, denote a saturated, 5 membered or 6-membered, monocyclic, heterocyclic structure, and alkyl radicals contain 1 to 4 carbon atoms, alkoxy radicals contain 1 to 4 carbon atoms, alkenyl radicals contain 3 or 4 carbon atoms and cycloalkyl radicals contain 5 to 7 carbon atoms; and aldehyde condensation products and acid addition salts thereof and to the production thereof by a method selected from (A) reacting a compound having the formula with a compound of the general formula Y - X wherein X has the meanings indicated above and Y represents halogen and, ii X denotes also represents -OH, OK and -ONa;(B) reacting a compound having the formula with a compound of the formula H2N-X wherein X has the meanings indicator above and Z represents or , and Hal denotes halogen; (C) reacting a phenol of the formula with a compound of the formula Z-CH2NH-X wherein X has the meanings indicator above and Z denotes or wherein Hal represents a halogen atom; and that the resulting compound is optionally reacted with an aldehyde of the formula R4-CHO , wherein R4 denotes hydrogen or a lower alkyl radical having up to 4 C atoms, to form an oxyzolidine of the formula or is optionally reacted with an acid to form an acid addition salt. 1a