NEW MATERIAL:An indazole derivative of formula I (n is an integer 1W6; R1 and R2 are H, 1W6C alkyl or heterocyclic ring having up to 5C atoms with the N atom in which the H atoms linked to one C atom on the heterocyclic ring may be substituted by an alkyl) and an acid addition salt thereof.
EXAMPLE: 1-(2-Dimethylaminoethyl)-3-aminoindazole.
USE: Useful as a nonsteroid remedy having a high anti-inflammatory activity and improved analgesic action, and a remedy for suppressing the side effects, e.g. ulceration in digestive tracts, of acidic nonsteroid anti-inflammatory agnets.
PROCESS: A 3-aminoindazole is reacted with phthalic anhydride to give 3-phthalimidoindazole, which is then reacted with an ω-halogenoalkylamine of formula II (X is halogen) to afford a 1-(aminoalkyl)-3-phthalimidoindazole. The protecting group of the amino group at the 3-position in the resultant compound is then removed with hydrazine hydrate to give the compound of formula I.
SUGIHARA TASUKE
SONE TAKANORI
KAWAKUBO HIROSHI