摘要:
A readily available and inexpensive natural α-amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula (3), which is then treated with an acid to provide an optically active aminoketone represented by formula (4). The product is then converted into an optically active aminoalcohol represented by formula (5) or (6) by, for example reduction.
摘要:
A novel polyamine derivative, or polyol derivative, having a piperidylaminotriazine skeleton; salts of such compounds; a process for producing them; an organic material stabilizer comprising any of such compounds; a method of stabilizing an organic material; and a stabilized organinc material. Compounds of the general formula: (1) (wherein X is N(R4) or an oxygen atom; R1 is an n-valent hydrocarbon group; R2 is an hydrogen atom or an alkyl; R3 is a hydrogen atom, an alkyl, an alkoxy or an acyl; R4 is a hydrogen atom or an alkyl; and n is an integer of 3 to 16) are effective in the stabilization of an organic material against deterioration by light, heat, oxygen, ozone and electromagnetic waves, such as X-rays and γ-rays.
摘要:
A novel polyamine derivative, or polyol derivative, having a piperidylaminotriazine skeleton; salts of such compounds; a process for producing them; an organic material stabilizer comprising any of such compounds; a method of stabilizing an organic material; and a stabilized organinc material. Compounds of the general formula: (1) (wherein X is N(R4) or an oxygen atom; R1 is an n-valent hydrocarbon group; R2 is an hydrogen atom or an alkyl; R3 is a hydrogen atom, an alkyl, an alkoxy or an acyl; R4 is a hydrogen atom or an alkyl; and n is an integer of 3 to 16) are effective in the stabilization of an organic material against deterioration by light, heat, oxygen, ozone and electromagnetic waves, such as X-rays and γ-rays.
摘要:
A process for producing 1-(2'-deoxy-B-D-erythropentofuranosyl)-5-trifluoromethyluracil derivatives having the formula as shown below: ##STR1## wherein X.sup.1 and X.sup.2 are independently hydrogen or halogen, comprising:(a) reacting 5-trifluoromethyl-5,6-dihydrouracil with alkylsulfoxide in the presence of a halogen and and acid to obtain 5-trifluoromethyluracil;(b) reacting the obtained 5-trifluoromethyluracil with a silylating agent to obtain 5-trifluoromethyl-2,4 -bis(trimethylsilyloxy)uracil; and(c) reacting the obtained 5-trifluoromethyl-2,4-bis(trimethylsilyloxy)uracil with a protected 2-deoxyalpha-D-erthro-pentofuranosyl)halide derivative in chloroform solvent in the presence of fluoride ion and in the presence of a copper compound as a catalyst.The resulting, deblocked nucleosides are useful as antiviral and antitumor agents.
摘要:
Compounds having an activity to stimulate the carcinostatic effect of carcinostatic agents, which can be expressed by the following general formula (1): ##STR1## in which A is ##STR2## (in which R.sub.1, R.sub.2 and R.sub.3 are each independent and represent a hydrogen atom or a phenyl group) are made into fumarates so as to improve their oral absorbability and solubility in water without interfering with their effects.
摘要:
A glycide derivative represented by the following general formula (I) is produced by reacting a hydroxyaryl or heteroaryl represented by A-OH with glycidyl tosylate in the presence of a cesium base as a base. Thereby, an aryl glycidyl ether derivative, which is an important intermediate for drug production, can be produced easily and reliably. Particularly when optically active glycidyl tosylate is used, said compound can be obtained at a high optical purity. ##STR1## wherein A represents an aryl group or a heteroaryl group.
摘要:
Catechol derivatives which produce nerve growth factor in particular tissues of the brain are disclosed. These derivatives provide preventive and therapeutic effects for regressive disorders of the central nervous system including senile dementia of the Alzheimer type.
摘要:
Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.
摘要:
Isoquinoline derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 denotes a hydrogen or halogen atom, or a nitro or acetyl group, and R.sub.2 denotes a hydrogen atom, or a methyl, methoxy, phenyl, 4-pyridyl or 2-pyridyl group, and therapeutically acceptable salts thereof have high cardiotonic activity and low toxicity.
摘要:
A novel polyamine derivative, or polyol derivative, having a piperidylaminotriazine skeleton; salts of such compounds; a process for producing them; an organic material stabilizer comprising any of such compounds; a method of stabilizing an organic material; and a stabilized organic material. Compounds of the general formula: (1) (wherein X is N(R4) or an oxygen atom; R1 is an n-valent hydrocarbon group; R2 is a hydrogen atom or an alkyl; R3 is a hydrogen atom, an alkyl, an alkoxy or an acyl; R4 is a hydrogen atom or an alkyl; and n is an integer of 3 to 16) are effective in the stabilization of an organic material against deterioration by light, heat, oxygen, ozone and electromagnetic waves, such as X-rays and γ-rays.