To obtain the subject new compound exhibiting an excellent nNOS- inhibiting activity or an excellent iNOS-inhibiting activity and useful as a medicine for treating cerebrovascular diseases, head wounds, spinal injuries, headache, Parkinson's disease, Alzheimer's disease, etc.
A compound of formula I [R1, R2 are each H, a (substituted) lower alkyl, an acryl, etc., R3, R4 are each H, a (substituted) lower alkyl, etc.; R5 is H, a lower alkyl, an acyl, etc.; X1-X4 are each H, a halogen, nitro, etc.; A is a (substituted) benzene ring or a (substituted) aromatic heterocyclic ring; (n), (m) are each 0, 1]. For example, 2-(3-(di-(t-butoxycarbonyl)aminomethyl) phenylamino)-3-nitropyridine. The compound of formula I is obtained by reacting a a substituted aniline of formula II [R5 is H, a (substituted) lower alkyl] with a compound of the formula: A-L (L is a releasing group) in the presence of a base and, if necessary, further a metal catalyst and a ligand in a proper solvent at a temperature of from room temperature to the boiling point of the reaction mixture.
MAKINO TOSHIHIKO
NISHIMURA SACHIKAZU
NAGAFUJI TOSHIAKI
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