FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to chemical-pharmaceutical industry and medicine, and concerns compounds that can be used to develop agents for cardiovascular disease. What is presented is the use of 2-[2-[5-(hydroxymethyl)-3-methyl-1,3-oxazolidin-2-ylidene]-2-cyanoethylidene]indolin-3-one of formula
as a biologically active compound exhibiting the properties of an exogenous nitric oxide donor, an activator of the enzyme soluble guanylate cyclase, a blood platelet aggregation inhibitor with antihypertensive activity for preparing cardiovascular diseases. The invention refers to a method for preparing 2-[2-[5-(hydroxymethyl)-3-methyl-1,3-oxazolidin-2-ylidene]-2-cyanoethylidene]indolin-3-one of formula I which is prepared by the reaction of α-cyano-β-(3-acetoxyindolyl-2)acrylic acid nitrile of formula 
with N-methylaminopropane-2,3-diol (MeHN-CH2CH(OH)CH2OH (formula IIIa)) in a polar solvent on boiling. Also, the invention refers to a version of the method for preparing 2-[2-[5-(hydroxymethyl)-3-methyl-1,3-oxazolidin-2-ylidene]-2-cyanoethylidene]indolin-3-one of formula I characterised by the fact that N-acetylindoxyl and ethoxymethylene malondinitrile are reacted to form N-acetyl-3-hydroxy-2-dicyanovinylindole, then acetylated by acetic anhydride to N-acetyl-3-acetoxy-2-dicyanovinylindole, further reacted with an equimolecular amount of N-methylaminopropane-2,3-diol (IIIa) to form 1-acetyl-2-[2'-cyano-2'-(3"-methyl-5"-oxymethyloxazolidin-2"-ilidene)-ethylidene]indolinone-3 of formula
;
thereafter an acetyl group is removed in a methanol medium by the reaction of triton B representing 40% benzyl trimethylammonium hydroxide in methanol; the precipitation is washed, dried and purified by re-crystallisation from the mixture of dimethyl formamide and water to prepare the end product.
EFFECT: preparing the indolinone derivatives for preparing the agents for cardiovascular diseases.
3 cl, 4 tbl, 3 dwg, 11 ex
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