method for preparing a preparation with a cytotoxic and / or ganglioplegische force, formed preparations obtained by applying this method.and method for the preparation of heterocyclic nitrogen containing spiroverbindingen, suitable for use in this method.

摘要

1408147 Sila-spirane compounds GESCHICKTER FUND OF MEDICAL RESEARCH Inc 8 Sept 1972 [8 Sept 1971] 41888/72 Heading C3S [Also in Division C2] Compounds of the general formula and acid addition and quaternary ammonium salts thereof wherein RSP1/SP and RSP2/SP are C 1-4 alkyl, X is Si, A and ASP1/SP are the same and are either CH 2 or C=O, n is 0 or 1, B is CH 2 when n is 1 and the same as A when n is 0, RSP3/SP is C 2-6 alkylene or C 3-4 alkenylene, and RSP4/SP and RSP5/SP are C 1-4 alkyl or C 3-4 alkenyl or together form a heterocyclic group which may contain at least one further N atom and which may be substituted are prepared by reacting a compound of formula with a compound H 2 N-RSP3/SP-N(RSP4/SP) (RSP5/SP) to give an azaspirodione of Formula I which can be reduced to give an azaspirane of this general formula, and optionally converting the compound into salt form, particularly a salt of formula where Q is H, C 1-4 alkyl or C 3-4 alkenyl and Z is a non-toxic, pharmaceutically acceptable anion such as Cl, Br, I,SO 4 , acetate, perchlorate, mucate, pamsate, succinate citrate or phosphate. When n is 1 and A is CO, the reactant of Formula II is prepared by dehydration of the corresponding diacid which is prepared by reacting the 4-(dialkylsila) - cyclohexanone with a compound (E) 2 P(O)-CH 2 D, where D is COOE or CN and E is C 1-4 alkoxy to form a compound which is reacted with an alkyl cyanoacetate to give which is hydrolysed to form the diacid. The compounds are pharmacologically active.