| 摘要 |
FIELD: organic chemistry. SUBSTANCE: invention relates to compounds of the general formula (I) where R<SB>1</SB> - hydrogen atom or alkyl radical with 1-4 carbon atoms; R<SB>2</SB> - hydrogen atom, hydroxyl group, amino-group or alkyl radical with 1-4 carbon atoms; R<SB>3</SB> - hydrogen atom, or R<SB>2</SB> and R<SB>3</SB> form together group -CH<SB>2</SB>-CH<SB>2</SB>-. Invention relates to also a method of synthesis of compounds of the formula (I) that involves interaction of compound of the formula (II) where R<SB>1</SB> has a value indicated above with alkanol with 1-4 C-atoms in the presence of gaseous hydrogen chloride. Synthesized compound of the formula (III) where value R<SB>1</SB> is indicated above and alk means alkyl radical with 1-4 C-atoms is interacted with one of enantiomers of alpha--methylbenzylamine. Synthesized 2-hydroxy-3-[1-(1H-imidazole- -4-yl)-alkyl] -N--alpha-methylbenzylbenzene carboximideamide of the formula (IV) where R<SB>1</SB> has the above indicated value is interacted with compound of the formula R<SB>2</SB>NH<SB>2</SB> (V) where R<SB>2</SB> means hydrogen atom, hydroxyl group, amino-group or alkyl radical with 1-4 C-atoms if R<SB>3</SB> means hydrogen, or with ethylenediamine if R<SB>2</SB> and R<SB>3</SB> mean together -CH<SB>2</SB>-CH<SB>2</SB>-group. For synthesis of compound of the formula (I) as an optic isomer N--alpha--methyl- -benzylated diastereomers of the formula (IV) where R<SB>1</SB> means alkyl radical with 1-4 C-atoms are separated. For synthesis of compound of the formula (I) where R<SB>2</SB> and R<SB>3</SB> mean hydrogen alpha-methylbenzyl-group in separated diastereomers is removed by hydrolysis with concentrated hydrochloric acid at 80-110 C and if necessary the end product is converted to acid additive salt. Invention proposes also a pharmaceutical composition for intraocular pressure decrease that contains an active component as one or some 2-hydroxy-3-[1-(1H-imidazole-4-yl)-alkyl] -benzene carboxyimideamides of the formula (I) or their nontoxic ophth
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