摘要:
A modified lithium aluminium hydride type reducing agent is useful for reducing organic compounds having a carbonyl group-(ketone group of aldehyde group) in their structure to the corresponding alcohols. It is obtained by reacting one equivalent of lithium aluminium hydride with one equivalent of an optically active N-substituted ephedrine of the formula, (wherein R, is a C i -C 4 alkyl group or benzyl group and Ph is phenyl group) and two equivalents of an N-substituted aniline of the formula, (wherein R 2 is a C 1 -C 4 alkyl group or phenyl group, and Ph is phenyl group). The reducing agent is particularly useful for reducing 2-acetyl-5, 8-dimethoxy-3, 4-dihydronaphthalene to the corresponding 2-(1'-hydroxy)ethyl compound, and, by selecting a particular modified aluminium hydride the unsymmetrical ketone can be reduced to selectively produce either an alcohol in which the asymmetric carbon atom bonded to the hydroxy group is in R-configuration or an alcohol in which said asymmetric carbon atom is in S-configuration.
摘要:
An aminonaphthacene derivative of the formula: wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a hydrogen atom or a hydroxyl group, R 3 is a hydrogen atom or a lower alkanoyl group and R 4 and R 5 are, same or different, each a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or a group of the formula: wherein A is an alkylene group which may have one or more lower alkyl substituent(s) and R 6 and R 7 are, same or different, each a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or a lower aminoalkyl group, and an acid addition salt thereof, which is useful as anti-tumor agent.
摘要:
Sodium 6- D (―)[-α-(4-hydroxy-1,5-naphtthydridine-3-carboxyamido) phenylacetamido] penicillanate or the derivative thereof bearing alydroxylgroup at the p-position of the phenyl group in a crude state can be purified efficiently through the reaction with dimethyl-sulfoxide in a liquid medium and decomposition of the obtained adducts in a water-containing liquid medium.
摘要:
9-Aminonaphthacene derivative having the formula: wherein R 1 and R 2 are both hydrogen atoms or either one of them is a hydrogen atom and the other is hydroxy group or methoxy group; R 3 is acetyl group or 1-hydroxyethyl group; R 4 is a hydrogen atom or halogen-substituted lower alkanoyl group; R 5 is a hydrogen atom, hydroxy group, lower alkanoyloxy group, amino group, halogen-substituted lower alkanoylamino group or morpholino group; R 6 is a hydrogen atom, hydroxy group, lower alkanoyloxy group or tetrahdropyranyl- oxy group; R' is a hydrogen atom, methyl group, hydroxymethyl group or lower alkanoyloxymethyl group; R is a hydrogen atom, hydroxy group or lower alkanoyloxy group, and n is zero or one, which is useful as anti-cancer chemical agents with lower toxicity.
摘要:
Aminonaphthacene derivatives of the formula: wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a hydrogen atom or a hydroxyl group, R 3 and R 4 are each a lower alkyl group or, when taken together, represent an ethylenedioxy group or an oxo group and R 6 and R 8 are each a hydrogen atom, a lower alkyl group or a group of the formula: -A-Q (in which A is an alkylene group optionally bearing at least one lower alkyl and Q is a hydrogen atom, a hydroxyl group, a lower alkoxy group or a group of the formula: wherein R 7 and R 8 are each a hydrogen atom, a lower alkyl group, a benzyl group, a hydroxy (lower) alkyl group or an amino (lower) alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a 5 to 7-membered nitrogen-containing ring optionally having an additional nitrogen or oxygen atom in the ring and optionally bearing any substituent on the ring) or, R 5 and R 6 when taken together with the adjacent nitrogen atom to which they are attached, represent a 5 to 7-membered nitrogen-containing ring optionally having an additional nitrogen or oxygen atom in the ring and optionally bearing any substituent on the ring, and their acid addition salts, which are useful as anti-tumor agents.