HALOID-CONTAINING 3'-AMIDODERIVATIVES OF (1'R,5'R)-3' -AZA-1'-(2-AMINO -1,6-DIHYDRO -6-OXOPURINYL-9) -3'-DEOXYPYRANOSIDE AS SPECIFIC IRREVERSIBLE FLUORESCENT INHIBITORS OF RNA-POLYMERASE Russian patent published in 1995 - IPC

Abstract RU 2039065 C1

FIELD: organic chemistry. SUBSTANCE: product: (1′R, 5′R)-3′-aza-1′-(2-amino-1,6-dihydro -6-oxopurinyl-9)-3′-deoxy-3′-[5-(dimethylamino) naphthalene-1-sulfamido] hexopyranosyl-6′- [4-fluorosulfonyl)benzoate] yield is 42% empirical formula is C29H29FN8O8S2, m. p. is 170-172 C (with decomposition). Product: (1′R, 5′R)-3′-aza-1′- (2-amino-1,6- dihydro-6-oxopurinyl -9)-3′-deoxy-3′- [5-(dimethylamino) naphthalene-1-sulfamido] hexopyranosyl-6′- [4-bromomethyl)benzoate] yield is 51% empirical formula is C30H31BrN8O8S, m. p. is 176-178 C (with decomposition). Product: (1′R, 5′R)-3′-aza-1′- (2-amino-1,6-dihydro -6-oxopurinyl-9)-3′ -deoxy-3′- (2-hydroxybenzamido)hexopyranozyl -6′-[4-(fluorosulfonyl)benzoate] yield is 38% empirical formula is C24H22FN7O10S, m. p. is 160 C (with decomposition). Product: (1′R, 5′R)-3′-aza-1′- (2-amino-1,6-dihydro -6′-oxopurinyl -9-3′-deoxy-3′- (2-hydroxybenzamido)hexopyranosyl -6′-[4-(bromomethyl)benzoate] yield is 43% empirical formula is C25H24BrN7O8, m. p. is 168-170 C (with decomposition). Synthesized compounds were used as specific irreversible fluorescent inhibitors of RNA-polymerase. EFFECT: improved method of synthesis. 1 tbl

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RU 2 039 065 C1

Authors

Khropov Ju.V.

Baranova L.A.

Tunitskaja V.L.

Kochetkov S.N.

Dates

1995-07-09Published

1991-01-24Filed