METHOD OF OBTAINING 5-( α -HALOGEN ACETYL)-8-(SUBSTITUTED OXY)-(1H)-QUINOLINE-2-ONS Russian patent published in 2008 - IPC C07D215/26 

FIELD: chemistry.

SUBSTANCE: obtaining 5-(α-halogen acetyl)-8-oxy-(1H)-quinoline-2-ons or their protected forms includes: (a) interaction of (i) 8-hydroxy-(1H)-quinoline-2-on with acidifying agent and Lewis acid obtaining as the result 5-acetyl-8-hydroxyl-(1H)-quinoline-2-on; or (ii) 8-hydroxy-(1H)-quinoline-2-on with acidifying agent obtaining as a result 8-acetoxy-(1H)-quinoline-2-on, and processing, in situ (at the moment of obtaining) 8-acetoxy-(1H)-quinoline-2-on with Lewis acid, obtaining as the result 5-acetyl-8-hydroxy-(1H)-quinoline-2-on; (b) interaction of 5-acetyl-8-hydroxy-(1H)-quinoline-2-on, obtained at stage (a), with compound of formula RL in presence of base and solvent obtaining as the result 5-acetyl-8-oxy-(1H)-quinoline-2-on or its protected form, where R stands for protecting group, and L stands for released group; and (c) interaction of 5-acetyl-8-oxy-(1H)-quinoline-2-on or its protected form with halogenating agent in presence of solvent obtaining as the result 5-(α-halogenacetyl)-8-oxy-(1H)-quinoline-2-on or its protected form. In invention also described is method of obtaining salts of 5-[(R)-2-(5,6-diethyl-indane-2-ylamino)-1-hydroxyethyl]-8-hydroxy-(1H)-quinolinon-2-on. Claimed method is alternative to used at present industrial method of production of salts of 5-[(R)-2-(5,6-diethyl-indane-2-ylamino)-1-hydroxyethyl]-8-hydroxy-(1H)-quinolinon-2-on.

EFFECT: improved method of said product production.

12 cl, 1 tbl, 11 ex