Optically active 1,4-benzodiazepines intermediates
OwnerFranjo Kajfez, Nikola Blazevic +1inventors
InventorsFranjo Kajfez, Nikola Blazevic, Vitomir Sunjic
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Abstract
Optically active intermediates of the formula: ##STR1## in the S optical 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, or 3'-methyleneindolyl, and A is a protective group, and their preparation is described. These compounds are useful in the preparation of corresponding optically active 1,4-benzodiazepines.
Claims3
A compound having the formula:
- ##STR19## in the S optical 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, and A is a protective group selected from the group consisting of tertiarybutoxy carbonyl and carbobenzoxy.
A compound having the formula:
- ##STR20## in the S optical 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, and hydroxybenzyl, and A is a protective group selected from the group consisting of tertiary-butoxy carbonyl, and carbobenzoxy.
Dependencies are inferred from the claim text.