N-phosphoryl biguanides - with hypoglycaemic activity

摘要

N-Phosphorylbiguanides of formula: (MO)2PNO)-NH-C(=NH)-NH-C(=NH)-NR1R2 (where M is a cation; R1 is H or alkyl and R2 is an aliphatic, isocyclic or heterocyclic residue contg. no ionogenic gps., or NR1R2 is a 6-membered heterocycle) are hypoglycaemics with more favourable therapeutic index than known hypoglycaemic guanidine dereivs. and are useful for treating all forms of diabetes. They may be prepd. by reacting a diaralkyl phosphite with H2N-C(=NH)-NR1R2 in the presence of CCl4 and alkali and catalytically hydrogenolysing the reaction product.