Borinic and borinothiolic acid derivs

摘要

Borinic and borinothiolic acid derivs Title compds. (I) useful as antibacterials esp. against Gram negative pathogens R'R2B-XR3 (I) (where R' and R2 are th ienyl or furyl opt. substd. by halogen, alkyl, alkoxy, alkylthio, hydroxy alkyl or alkenyl (all up to 6C) or ketalised or thioketalised alkanol (up to 4C) or phenyl or thio phenyl opt. subtsd. by halogen, alkyl or alkoxy (up to 6C) or dialkylamino (each alkyl up to 6C) provided that R' and R2 do not carry more than 4 substituents; X is O or S; R3 is H or an organic residue contg. O or N having a free pair of electrons sepd. from X by 2 - 4 atoms and coordinately bonded to B provided that that when R' and R2 are unsubstd. thienyl R3 is not H or 8-quinolyl. (R3 is pref. 8-quinolyl but may also be amino-aliphatic or contain a keto group opt. with other substituents)) are prepd. by reacting R3XH with either R'R2BR6, R'R2BOH. (R')2BR2 or R'B(R2)2 where R6 is iodine or alkoxy.