Intermediates in the synthesis of 5-alkylamino-7-phenyl or substituted phenyl-2,3-dihydro-1H-1,4-diazepines

摘要

Compounds of the formula WHEREIN R is alkyl of 1 to 6 carbon atoms, EACH X is independently alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo, and M IS 0, 1 OR 2, AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, ARE USEFUL AS ANTI-OBESITY AND ANTI-DIABETIC AGENTS. They are synthesized by reacting a 2-alkyl-5-arylisoxazolium salt with ethylene diamine to obtain a compound of the formula OH ¦ H2N-CH2CH2-NH-C-CH=C PARALLEL N ¦, R or a tautomer thereof, wherein R, X and m are as defined above, which is then cyclized with a strong acid.