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A new two-step approach toward the synthesis of aplysinopsin analogues 5-(1-R-1H-indol-3-ylmethylene)-2-aryl-3,5-dihydroimidazol-4-ones consisting in obtaining and reaction of 4-(1-R-1H-indol-3-ylmethilene)-2-Ar-4H-oxazol-5-ones with amines was developed. The configuration of starting compounds and final products was determined by 13С and 1H-nmr spectroscopy.

Opening of the oxirane ring in 1-oxiranylmethylindoles yielded new indole derivatives containing 1,2-amino alcohol residues at the nitrogen atom. Compounds were studied in vitro in relation to various types of pharmacological activity typical of this class of compounds, including receptor (5-HT2, 5-HT3, P2Y1-ergic, κ-opioid), antiaggregant, hemorheological, antiarrhythmic, and antioxidant activities.

Opening of the five-member ring of indolylmethyleneoxazolones with aliphatic amines was used to synthesize a series of amides of 2-amino-3-indolylacrylic acid. These compounds were studied in vitro in relation to the various types of pharmacological activity typical of this class, including receptor (5-HT2-, 5-HT3-, and P2Y1-ergic, K-opioid), antiaggregant, hemorheological, antiarrhythmic, and antioxidant activities.

A new two-step approach toward the synthesis of aplysinopsin analogues 5-(1-R-1H-indol-3-ylmethylene)-2-aryl-3,5-dihydroimidazol-4-ones consisting in obtaining and reaction of 4-(1-R-1H-indol-3-ylmethilene)-2-Ar-4H-oxazol-5-ones with amines was developed. The configuration of starting compounds and final products was determined by 13С and 1H-nmr spectroscopy.

The use of the tert-amino effect in cyclization of reaction products from 2-(azepan-1-yl)-1-methyl-1H-indole-3-carbaldehyde and active methylene compounds afforded spirocyclic fused α-carbolines.

Indole derivatives with a 2,3-epoxypropyl substituent attached to nitrogen were synthesized. In reactions with primary and secondary amines these compounds afforded the corresponding 1,2-aminoalcohols.