DERIVATIVES OF INDOLINE-2-ONE AND INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS Russian patent published in 1999 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to derivatives of indoline of the general formula (I) where R₁ - halogen, lower alkyl, lower-alkoxy-group, OH-group, NO₂, alkoxycarbonyl-group, COOH-group; R₂ - H, free or substituted lower alkenyl, free or substituted alkyl, free or substituted cycloalkyl, free or substituted aryl; R₃- - free or substituted lower alkyl, free or substituted aryl, R₄ where OR₅, -NR₆R₇, can be similar or distinct and each means H, free or substituted lower alkyl, free or substituted cycloalkyl, free or substituted pyridyl, pyrimidyl, indolyl, indolinyl or lower alkoxy-group, or R₅, R₆, R₇ and R₆ taken together form R₇ or -(CH₂)_m- where each k, l, m = 1-8; -(CH₂)_lNR₈-(CH₂)_k - H, lower alkyl; X and Y can be similar or distinct and each means R₈, -NH-, -O-; n = 0-4. compounds show a selective antagonism with respect to gastrin receptors. Compounds of the formula (II) CH₂- where and n have values indicated above; R₁, R₃ is a group of R₉ in the formula (III) where -CH₂CH(OR₁₀)(OR₁₁) and R₁₀ - each free or substituted lower alkyl; R₁₁ - lower alkyl, aralkyl that are used as intermediated compounds for synthesis of derivatives of indole of the formula (I) R_a. EFFECT: improved method of synthesis. 12 cl, 8 dwg, 13 tbl, 219 ex