DERIVATIVES OF 1,2,3,4-TETRAHYDROBENZOFURO[3,2-C]-PYRIDINE, METHODS OF THEIR SYNTHESIS AND COMPOSITIONS BASED ON THEREOF Russian patent published in 2003 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes derivatives of 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine of the general formula: , its N-oxide form, pharmaceutically acceptable addition salt or stereochemically isomeric form where each of R¹ means independently hydrogen, halogen atom, C_1-6-alkyl, nitro-group or C_1-4-alkoxy-group; Alk means C_1-6-alkanediyl; n = 1 or 2; D means 1- or 2-benzimidazolyl, 2(3H)-benzoxazolone-3-yl or radical of formulas: (a) , (b) , (c) , (d) , (e) , (f) , (g) where each X means S;R²meansC_1-6-alkyl,aryloraryl-C_1-6-alkyl;R³meansC_1-6-alkylthio-group; each of R⁴, R⁵, R⁶, R⁷, R⁸, R¹⁰, R¹¹ means independently hydrogen atom or C_1-6-alkyl; R⁹ means aryl; or R³ and R⁴ taken in common form bivalent radical -R³-R⁴- of formulas (a-2) or (a-5) -CH=CH-CH= CH- where one or two hydrogen atoms of indicated radicals can be replaced independently for halogen atom, C_1-6-alkyl, aryl-C_1-6-alkyl, trifluoromethyl, amino-group, hydroxy-group or C_1-6-alkoxy-group; or where possible two heminal hydrogen atoms can be replaced for aryl-C_1-6-alkylidene; or -R³-R⁴- can mean formula (a-6) , (a-7) , (a-8) -S-CH= CH-, (a-11) -NH-CH=CH- or (a-14) -CH=CH-O also where from one to three hydrogen atoms of indicated radicals can be replaced each independently for C_1-6-alkyl; and aryl means phenyl or phenyl substituted with C_1-6-alkyl. Invention describes also methods of synthesis of compounds of the formula (I), composition eliciting antagonistic activity with respect to central α-adrenoceptors and composition useful for treatment of sickness associated with norepinephrine deficiency in central and peripheral nervous system. Invention provides synthesis of new compounds with useful biological properties. EFFECT: improved methods of synthesis. 12 cl, 6 tbl, 16 ex