Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.

Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.

Abstract: An efficient method for producing cytidine derivatives that took away the previous drawbacks by efficiently synthesizing cytidine derivatives by utilizing a tertiary amine can be provided.

Abstract: A quinoline derivative represented by the following formula (1): 1

Abstract: An efficient method for producing cytidine derivatives that took away the previous drawbacks by efficiently synthesizing cytidine derivatives by utilizing a tertiary amine can be provided.

Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.

Abstract: 5-trifluoromethyl-2,4-bis(trimethylsilyloxy)pyrimidine is reacted with a 2-deoxy-&agr;-D-erythro-pentofuranosyl chloride derivative reacted in the absence or presence of a small amount of solvent to give a &bgr;-form of 1-(2′-deoxy-&bgr;-D-erythro-pentofuranosyl)-5-trifluoromethyl uracil derivative with a high selectivity.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: Heterocyclic compounds useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells are disclosed, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

Abstract: Therapeutic agents for degressive diseases in the central nervous system, which contain amide derivatives of dihydrocaffeic acid of the general formula (I) ##STR1## wherein, R.sub.1 and R.sub.2 and A are defined in the specification; the compounds exert a nerve growth factor inducing action and thus are effective for the prevention of the progression of degenerative diseases in the central nervous system and the therapeutic treatment thereof.

Abstract: Dihydrocaffeic acid derivatives are here disclosed which are applicable as medicines having excellent absorbency in the case of oral administration and good concentration retention in blood.The disclosed compounds have the function to induce the production and secretion of a nerve growth factor (NGF) in the brain tissue, and therefore they are effective as medicines for the progression inhibition and therapy of regressive disorders of the central nervous system.

Abstract: 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.

Abstract: 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.

Abstract: Dihydrocaffeic acid derivatives are here disclosed which are applicable as medicines having excellent absorbency in the case of oral administration and good concentration retention in blood.The disclosed compounds have the function to induce the production and secretion of a nerve growth factor (NGF) in the brain tissue, and therefore they are effective as medicines for the progression inhibition and therapy of regressive disorders of the central nervous system.

Abstract: 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.

Abstract: 2-Methoxycarbonyl-4-(4-pyridyl)cyclohexanone of the present invention is an important intermediate for preparing isoquinoline derivatives which are useful as medicines, particularly as heart medicines.

Abstract: This invention relates to pyridazinone derivatives of the general formula: ##STR1## [wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group; R.sup.2 for a hydrogen atom or a lower alkyl group; and A for (i) a ring selected from a benzene ring, a furan ring, a thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present), or (ii) a grouping of the formula: ##STR2## (wherein R.sup.3 stands for a hydrogen atom, a lower alkyl group, a phenyl(lower)alkyl, a hydroxyphenyl(lower)alkyl group, a lower alkylmercapto(lower)alkyl group, a benzylmercapto(lower)alkyl group, a guanidino(lower)alkyl group, a nitroguanidino(lower)alkyl group, an indolyl(lower)alkyl group, a carbamoyl(lower)alkyl group or a carboxy(lower)alkyl group, R.sup.4 for a hydrogen atom or a lower alkyl group, R.sup.

Abstract: This invention relates to a novel process for preparing 4-acetyl-1-methyl-7-pyridyl-5,6,7,8-tetrahydro-3(2H)-isoquinolinone characterized by condensing 2-acetyl-4-pyridyl cyclohexanone with acetoacetamide. This compound is useful as pharmaceuticals, particularly cardiotonics.