METHOD OF SYNTHESIS OF 3-AMINOISOQUINOLINE DERIVATIVES Russian patent published in 1994 - IPC

FIELD: organic chemistry. SUBSTANCE: synthesis of the end products is carried out by reaction of cyclodi- or trimerization of phenylacetic acid nitriles of the general formula II or their mixture with nitriles of the general formulas III and IV R₆- C≡ N (III), R₇-C≡ N (IV) where R₆ and R₇ as indicated above by HCl following isolation of the end product where R₄ and R₅ - H or one of their is group C[=NH]-R₇ or acylation with isolation of compound where NR₄R₅ - acylamino-group, or hydrolysis and isolation of compound where NR₄R₅ - amino- or acylamino-group, or by alkylation and preparing of compound where R₄ and R₅ - a lower alkyl. Reaction is carried out preferably in the medium of aprotonic organic or inorganic solvent (dioxane, chloroform, phosphorus oxychloride). Necessary nitriles and halogen hydrogen can be prepared in situ from amides or aldoximes by action of phosphorus oxychloride. Method ensures to increase the yield of the end products from 72 to 87.5%. EFFECT: increased yield and assortment of 3-aminoisoquinoline derivatives. 3 cl, 1 tbl