NEW MATERIAL:A compound of formula I [R1 is lower alkyl; R2, R3 are H, lower alkyl or combining together shows -(CH2)4- or -CH=CH-CH=CH-; R4 is aromatic heterocyclic 5- to 6-membered ring containing N, O, S or other hetero atoms (wherein isthiazole, pyridine, 1,3,5-triazine are excluded), pyrazine- N-oxide, pyridazine-N-oxide, pyrimidine-N-oxide].
EXAMPLE: 2,6-Di-t-butyl-4-[(5-hydroxymethyl-2-pyrazynyl)amino]phenol.
USE: Anti-inflammatory, therapeutic agent for asthma, bronchitis or psoriasis.
PREPARATION: Thermal dehydrative condensation reaction between a benzoquinone derivative of formula II and an aromatic heterocyclic amine of formula III is conducted in the presence of a solid dehydrative condensation agent such as silica gel to give a compound of formula IV, then the product is allowed to react with a compound of formula V reductively to give the compound of formula I.
TAFUSA FUJIO
NAMIKAWA JUNICHI
MANABE YOSHIAKI