Optically active 1,4-benzodiazepines and process for use as a tranquilizer
OwnerFranjo Kajfez, Nikola Blazevic +1inventors
InventorsFranjo Kajfez, Nikola Blazevic, Vitomir Sunjic
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OwnerFranjo Kajfez, Nikola Blazevic +1inventors
InventorsFranjo Kajfez, Nikola Blazevic, Vitomir Sunjic
Estimating the term…
Compositions, useful as tranquilizers containing, as active ingredient, an optically active compound having the formula: ##STR1## having an asymmetric carbon atom in position 3 having the S configuration and wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, nitro, and trifluoromethyl groups, R.sub.2 is selected from the group consisting of hydrogen and C.sub.1-4 lower alkyl groups and R.sub.3 is selected from the group consisting of C.sub.1-4 lower alkyl, hydroxy C.sub.1-4 lower alkyl, phenyl, hydroxyphenyl, benzyl, hydroxybenzyl, and 3'-methyleneindolyl groups, is described. They are obtained by reaction of a compound having the formula ##STR2## with a compound of the formula wherein A is a protective group. The compounds of formula I have sedative and tranquilizing properties.
A method for tranquilizing a patient which comprises administering to the patient an effective amount of an optically active compound of the formula ##STR20## having an asymmetric carbon atom in position 3, said asymmetric carbon atom having the S configuration wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, nitro, and trifluoromethyl, R.sub.2 is selected from the group consisting of hydrogen and C.sub.1-4 lower alkyl and R.sub.3 is selected from the group consisting of C.sub.1-4 lower alkyl, hydroxy C.sub.1-4 lower alkyl, phenyl, hydroxyphenyl, benzyl, hydroxybenzyl, and 3'-methyleneindolyl.
Dependencies are inferred from the claim text.