Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Spofa United Pharmaceutical Works

Spojene Podniky Prozdravotnickou Vyrobu (spofa)

Ludmila Fisnerova

Jaroslava Grimova

Oldrich Nemecek

Zdenek Roubal

Bohumila Brunova

Eva Maturova

An etheric derivative of 4(3H)-quinazolinone which is a fluorinated 3-[2-(4-biphenylyloxy)ethyl]-4(3H)-quinazolinone, produced by reacting said 4(3H)-quinazolinone with the corresponding fluorinated 4-(2-chloroethoxy)biphenyl, and its acid addition salts, especially the hydrochloride. This compound possesses substantially higher analgesic activity and lower acute toxicity than aminophenazone, ibuprofen, acetylosalicyclic acid and paracetamol.

Etheric derivative of 4(3H)-quinazolinone and a process for preparation

This invention relates to the compound 3-[2-(2-Benzimidazolyl) Benzoyloxyethyl]-4(3H)-Quinazolinone of Formula I, and a process for the preparation thereof. The compound exhibits strong analgesic activity and almost zero toxicity in laboratory mice. ##STR1## The compound of Formula I is prepared by acylation of the compound 3-(2-hydroxyethyl)-4(3H)-quinazolinone with a reactive derivative of 2-(2-benzimidazolyl)benzoic acid, preferably its imidazolide, formed by treatment of the acid of Formula III with 1,1'-carbonyldiimidazole. The compounds of Formula II and Formula III are reacted in situ, at room temperature, and in the presence of an inert organic solvent. The product compound is isolated and purified by common techniques.

3-(2-(2-benzimidazolyl) benzolyloxyethyl)-4(3H)-quinazolinone

A technique is described for the preparation of a novel anti-inflammatory agent comprising 2-phenyl-2-carboxyethyl 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetate. The preparative technique involves reacting indomethacin with tropic acid.

2-Phenyl-2-carboxyethyl

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Prague, Czechia

Ludmila Fisnerova