| 摘要 |
<p>884,760. Phenthiazines. OLIN MATHIESON CHEMICAL CORPORATION. May 6, 1958, No. 14468/58. Class 2 (3). The invention comprises compounds of the general formula wherein A is a lower alkylene radical, B is a hydroxy-lower alkyl, hydroxy-(lower alkoxy)- lower alkyl, an ester of these or a carbalkoxy radical; R is a hydrogen atom or a lower alkyl radical; and n is 0, 1 or 2; their non-toxic acid addition salts; and the preparation thereof by reacting a phenthiazine of the formula in which Y represents hydrogen, -(lower alkanoyl) halide or -(lower alkylene) halide, with a compound' of the formula in which Z represents -(lower alkanoyl halide or -(lower alkylene) halide when Y represents hydrogen or in which Z represents hydrogen when Y represents -(lower alkanoyl) halide or -(lower alkylene) halide, reducing any resulting lower alkanoyl derivative; and, if desired, treating the base with an acid to form the acid addition salt. The terms 'lower alkyl', 'lower alkoxy' and lower alkylene' include straight and branched chain radicals of less than 8 carbon atoms. The products of the invention may be converted into the S-monoxides by reaction with an oxidising agent or the S,S-dioxides may be prepared by reacting an appropriate N-acylphenthiazine with an oxidising agent to form the S,S-dioxide, hydrolysing off the acyl group and carrying out the process of the invention. The phenthiazines of the second general formula above are prepared either by reacting an appropriate 10-unsubstituted phenthiazine with a halo-acyl halide and, if desired, reducing the keto group or with a di-halo-alkane, or (where Y is lower alkylene halide only) by condensing an appropriate phenthiazine with a (2-tetrahydropyranyloxy) alkyl halide, hydrolysing the product to the alcohol and halogenating. N-Hydroxyethoxyethylpiperazine is prepared from N-hydroxyethylpiperazine and 2-chloroethanol.</p> |
