Biguanidin-Derivate

1,213,119. Boron - biguanidine compounds. F. HOFFMANN - LA ROCHE & CO. A.G. 20 June, 1969 [21 June, 1968], No. 31200/69. Heading C2C. The invention comprises boron-biguanidine compounds of the general formula wherein X and Y are chlorine or bromine. They are prepared by reacting an N1-(3,4-dihal...

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Bibliographic Details
Main Authors HANS SPIEGELBERG,DR, HENRI RAMUZ,DR, WERNER BOLLAG,DR
Format Patent
LanguageGerman
Published 02.01.1970
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
CLADDING OR PLATING BY SOLDERING OR WELDING
CUTTING BY APPLYING HEAT LOCALLY, e.g. FLAME CUTTING
MACHINE TOOLS
METAL-WORKING NOT OTHERWISE PROVIDED FOR
METALLURGY
ORGANIC CHEMISTRY
PERFORMING OPERATIONS
SOLDERING OR UNSOLDERING
TRANSPORTING
WELDING
WORKING BY LASER BEAM
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Summary:1,213,119. Boron - biguanidine compounds. F. HOFFMANN - LA ROCHE & CO. A.G. 20 June, 1969 [21 June, 1968], No. 31200/69. Heading C2C. The invention comprises boron-biguanidine compounds of the general formula wherein X and Y are chlorine or bromine. They are prepared by reacting an N1-(3,4-dihalogenophenyl) - N5 - isopropylguanidine with boric acid, a boric acid ester, a boron halide or boric acid amide preferably in presence of an inert organic solvent. In preferred embodiments, (a) the reaction with boric acid takes place at elevated temperature in presence of an inert organic solvent, e.g. benzene, which distills azeotropically with water; (b) a boric acid ester is used e.g. tributyl borate in presence of toluene, (c) a boric acid amide is used e.g. tri-(N-dimethylamino)-borane, in presence of benzene, and (d) a boron halide e.g. borontrichloride, is used in presence of an inert organic solvent e.g. toluene and an acid binding agent which is soluble in the solvent e.g. pyridine. The starting N1 - (3,4 - dihalogeno - phenyl)- N5-isopropyl-guanidine compounds are prepared by reacting a 3,4-dihalogenoaniline with #-cyano -#1-isopropylguanidine. Examples 6 to 8 inclusive describe pharmaceutical compositions containing the above boronbiguanidine compounds. They may be in the form of tablets, dragÚes, ampoules, suppositories or capsules or may be in liquid form and may be taken enterally or parenterally.
Bibliography:Application Number: DE19691926210