VERFAHREN ZUR HERSTELLUNG VON DIBENZOTHIEPIN-DERIVATEN.

摘要

Prepn. of a propionic acid derivs. of formula (I) comprises: (a) reacting a propiophenone deriv. of formula (II) with a halogenating agent to give an acid of formula (III); (b) reacting with an alcohol of formula R2OH (IV) and an orthoformate of formula HC(OR2)3 (V) to give an acetal of formula (VI); then either (1) (c) converting (VI) into a dicarboxylic ester of formula (VII) in presence of zinc halide; (d) hydrolysing (VII) to give an acid of formula (VIII); and (e) treating (VIII) with a condensing agent to give (I); (2) (c1) reacting (VI) with zinc halide to form (VII); (d1) treating (VII) with a condensing agent to form an ester of formula (IX); and (e1) hydrolysing (IX) to form (I); or (3) (c2) treating (VI) with a base in a proton-donating medium to form (VIII); and (d2) treating (VIII) with a condensing agent to form (I). R1 = H or lower alkyl; R2 = lower alkyl; R'1 = lower alkyl (and is the same as R2 when R1 = H); X = halo. (VI) are new when R'1 = H or 1-6C alkyl; and R2 = 1-6C alkyl.