NYE AZETIDIN-DERIVATER.

摘要

1388861 Aminopropanol derivatives TEIKOKU HORMONE MFG CO Ltd 3 May 1972 [7 May 1971] 20638/72 Heading C2C The invention comprises a process for the preparation of aminopropanol derivatives of the Formula III wherein Ar is a substituted or unsubstituted phenylene or naphthylene group, Ac is an organic acyl group or a triphenylmethyl group, Y is H, a monovalent hydrocarbon group having up to 12 carbon atoms, or an organic acyl group, or Y and Ac together with the nitrogen atom to which they are attached for a cyclic dicarboximido group, Z is H or a protecting group bonded to the oxygen atom by an aliphatic ether linkage, and R is alkyl or aralkyl group and non-toxic acid addition salts thereof, the compounds being novel when Z is a protecting groups as defined above, by reacting compounds of the formula or non-toxic acid addition salts thereof with compounds of the formula and, if desired, converting the compounds of Formula III so obtained to non-toxic acid addition salts. 4-Acetamido-2,3-xylenol is obtained by acetylating 4-amino-2,3-xylenol. 1 - Isopropyl - 3 - azetidinol and 1 - tert.- butyl-3-azetidinol are prepared by the hydrogenolysis of 3-benzyloxy-1-isopropylazetidine and 3- benzyloxy - 1 - tert. - butylazetidine respectively, which are obtained by reacting 2-benzyloxy-1,3- dichloropropene with isopropylamine and tert.- butylamine respectively. Pharmaceutical compositions contain the above novel compounds or non-toxic acid addition salts thereof and pharmaceutically acceptable carriers or diluents. The compounds are used as antiulcerative agents. Reference has been directed by the Comptroller to Specifications 1,078,852, 1,185,044, 1,185,045, 1,185,046, 1,199,037 and 1,270,723.