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Russian-american Institute for New Drug Development

Nauchno-issledovatelsky Institut Farmakologii

Arkady M Likhosherstov

Alexandr P Skoldinov

Vitaly P Peresada

James A Halikas

Natalya Veniaminovna Kaverina

Tatiana A Voronina

Galina Alexandrovna Markova

Sergey B Seredenin

Liya Semenovna Nazarova

Konstantin O Chizhov

Gennady M Molodavkin

1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine derivatives having the formula (Formula I) ##STR1## and therapeutically acceptable acid addition salts thereof (Formula I.HX), wherein: R.sup.1 =hydrogen or acyl groups; and R.sup.2 =hydrogen or substituted aminomethyl groups. Said compounds and their acid addition salts have psychotropic activity, particularly anxiolytic activity.

1,2,3,4-tetrahydropyrrolo-[1,2-a]-pyrazine derivatives

1,2,3,4-Tetrahydropyrrolo-[1,2-a]-pyrazine of the formula: ##STR1## is disclosed together with a method for preparing the same which comprises reducing 3,4-dihydropyrrolo-[1,2-a]-pyrazine, in a medium of an organic solvent, by way of hydrogenation with hydrogen or complex hydrides of metals. When using hydrogen said hydrogenation is effected in the presence of a catalyst of the group of platinum. The desired product is then isolated from the reaction mixture. The resulting 1,2,3,4-tetrahydropyrrolo-[1,2-a]-pyrazine may be used as the starting product for the synthesis of physiologically active compounds such as octahydropyrrolo-[1,2-a]-pyrazine which serves as the basis for the preparation of coronary-dilating and neuroleptic compounds. The method for preparing 1,2,3,4-tetrahydropyrrolo-[1,2-a]-pyrazine is technologically simple and may be readily implemented on a commercial scale.

1,2,3,4-Tetrahydropyrrolo-[1,2-a]-pyrazine

The novel compound according to the present invention, viz. 3,4-dihydropyrrolo-[1,2-a]-pyrazine has the formula: ##STR1## The method of preparing this compound comprises reacting dialkylacetals or dioxalane of a 2,5-dialkoxytetrahydrofurfurol with ethylenediamine in a medium of lower aliphatic acids at a temperature within the range of from 100.degree. to 150.degree. C., followed by isolation of the desired product. The novel compound according to the present invention, viz. 3,4-dihydropyrrolo-[1,2-a]-pyrazine, owing to a simple method for producing same, simplifies the process of manufacture of physiologically active compounds employed in neuroleptic or coronary dilating preparations, wherein it may be used as the starting material.

3,4-Dihydropyrrolo-[1,2-a]-pyrazine and method of preparing same

Novel compounds 10'-[.omega.-N/1,4-diazabicyclo(4,m,0)-alkanyl/-acyl] -phenothiazines having the formula: ##STR1## wherein X = H, Cl, CF.sub.3 ; n = 1, 2, 3; m = 3, 5; and their salts of acidic addition and quaternary salts. The process for producing said compounds comprises reacting .omega. -chloracyl -2-substituted phenothiazines with 1,4-diazabicyclo(4,m,0)-alkanes in an inert solvent medium at a temperature of 50-140.degree. C followed by isolation of the desired product. Said compounds are pharmacologically active. The most active compound 10'- [.beta.-N-/1,4-diazabicyclo-(4,3,0)-nonanyl/-propyonyl]-2'-chlorophenothia zine of the formula: ##STR2## is an active principle of a medicated compound possessing spasmolytic and coronary-dilatant effect.

10'-( .omega.-N)-1,4-Diazabicyclo(4,3,0)-alkanyl-lacyl) -phenothiazine

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Moscow, Russia

Arkady M Likhosherstov