Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

Abstract: The present invention relates to a Variovorax sp. which produces an acylase having an asymmetric hydrolysis activity on an N-acetyl ?-amino acid to selectively produce an R-?-amino acid, and a Burkholderia sp. which produces both an acylase having an asymmetric hydrolysis activity on an N-acetyl ?-amino acid to selectively produce an S-?-amino acid and an acylase having an asymmetric hydrolysis activity of an N-acetyl ?-amino acid to selectively produce an R-?-amino acid, and a process for the selective production of an S-, or R-?-amino acid using the above strains.

Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

Abstract: The present invention relates to a Variovorax sp. which produces an acylase having an asymmetric hydrolysis activity on an N-acetyl ?-amino acid to selectively produce an R-?-amino acid, and a Burkholderia sp. which produces both an acylase having an asymmetric hydrolysis activity on an N-acetyl ?-amino acid to selectively produce an S-?-amino acid and an acylase having an asymmetric hydrolysis activity of an N-acetyl ?-amino acid to selectively produce an R-?-amino acid, and a process for the selective production of an S-, or R-?-amino acid using the above strains.

Abstract: Aminopyrimidine compounds represented by formula (3) may be efficiently prepared by reacting an azlactone compound represented by formula (1) with an amidine compound represented by formula (2) or a salt thereof: wherein R1, R2 and M are as defined in the specification.

Abstract: The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.

Abstract: The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.

Abstract: Aminopyrimidine compounds represented by formula (3) may be efficiently prepared by reacting an azlactone compound represented by formula (1) with an amidine compound represented by formula (2) or a salt thereof: wherein R1, R2 and M are as defined in the specification.

Abstract: The present invention relates to a novel production method of a diaminopyrimidine compound useful as an intermediate for various compounds having a pharmacological activity, a novel intermediate useful for producing said compound, and a production method of the intermediate. The present invention provides a novel 5-aminopyrimidine compound represented by the following formula (2) and a novel 4,5-diaminopyrimidine compound represented by the formula (3), as well as production methods of the compounds of the following formulas (2) to (6). wherein each symbol is as defined in the specification.

Abstract: The present invention relates to a production method of a compound represented by the formula (3), which includes reacting a compound represented by the formula (2) with a diphenylmethyl halide compound represented by the formula (1) in the presence of alkali metal alkoxide. According to the method of the present invention, compound (3) can be produced at a high purity and in a high yield. wherein each symbol is as defined in the specification, *1 and *2 each show an asymmetric carbon atom, and the configuration of the asymmetric carbon atom of *1 and *2 is (S,S) or (R,R).

Abstract: Compounds represented by formula (II): wherein M is a hydrogen atom, sodium, potassium, or lithium; P is a hydrogen atom, an alkyl group, and the like; and the wavy line indicates a cis form, a trans form, or a mixture thereof for the double bond to which it is attached, may be prepared by hydrolyzing a compound represented by formula (I), or a salt thereof: wherein R1 and R2 are the same or different and each is an alkyl group, or R1 and R2 together with the adjacent nitrogen atom may form an aliphatic heterocycle, and P and the wavy line are as defined above, in the presence of alkali metal hydroxide.

Abstract: The present invention relates to a production method of optically active 2-[(N-benzylprolyl)amino]-5-chlorobenzophenone (3) or a salt thereof, which includes reacting optically active N-benzylproline (1) with 2-amino-5-chlorobenzophenone (2) in acetonitrile and in the presence of an amide compound and thionyl chloride. According to the method of the present invention, optically active 2-[(N-benzylprolyl)amino]-5-chlorobenzophenone (3) or a salt thereof can be conveniently produced at a high purity and in a high yield: wherein * shows an asymmetric carbon atom and the configuration of the asymmetric carbon atom is S or R.

Abstract: Compounds represented by formula (II): wherein M is a hydrogen atom, sodium, potassium, or lithium; P is a hydrogen atom, an alkyl group, and the like; and the wavy line indicates a cis form, a trans form, or a mixture thereof for the double bond to which it is attached, may be prepared by hydrolyzing a compound represented by formula (I), or a salt thereof: wherein R1 and R2 are the same or different and each is an alkyl group, or R1 and R2 together with the adjacent nitrogen atom may form an aliphatic heterocycle, and P and the wavy line are as defined above, in the presence of alkali metal hydroxide.

Abstract: The present invention relates to a Variovorax sp. which produces an acylase having an asymmetric hydrolysis activity on an N-acetyl ?-amino acid to selectively produce an R-?-amino acid, and a Burkholderia sp. which produces both an acylase having an asymmetric hydrolysis activity on an N-acetyl ?-amino acid to selectively produce an S-?-amino acid and an acylase having an asymmetric hydrolysis activity of an N-acetyl ?-amino acid to selectively produce an R-?-amino acid, and a process for the selective production of an S-, or R-?-amino acid using the above strains.

Abstract: A production method for conveniently producing a 5?-acyloxynucleoside compound shown by the formula [A] in a good yield while suppressing formation of by-products, including subjecting a 2?,3?,5?-triacyloxynucleoside compound represented by the formula [I] to selective deacylation in an alcohol represented by the formula [II] using a base selected from the group consisting of alkali metal hydroxide, alkali metal alkoxide and alkali metal carbonate: wherein each symbol in the formula is as defined in the specification.

Abstract: Compound (II) is reacted with formate in the presence of an alkali metal alkoxide and the like to give compound (III); then this is reacted with compound (IVa) or compound (IVb) to give compound (V); then this is reacted with compound (VI) to give compound (VII); and then this is deprotected to give compound (I). The present invention provides an industrially advantageous production method of a 4-acetylpyrimidine compound useful as a synthetic intermediate for a pharmaceutical product: wherein X is a methylthio group and the like, R1 is a lower alkyl group and the like, R2 is a lower alkyl group optionally having substituent(s) and the like, M is an alkali metal and X1 is a halogen atom.

Abstract: Compound (II) and compound (III) are reacted to give compound (IVa) and/or compound (IVb); which are/is then reacted with compound (V) to give compound (I). wherein X is a methylthio group and the like, R1 and R2 are each a lower alkyl group optionally having substituent(s), an aryl group optionally having substituent(s) and the like, R3 is a lower alkyl group, R4 is a hydrogen atom, a lower alkyl group optionally having substituent(s) and the like, and Q is a carboxylate group and the like.

Abstract: Purine nucleosides which are fluorinated at the 3?-position (preferably the ?-position), may be economically and efficiently produced by fluorinating a novel purine nucleoside derivative (1) in which the hydroxyl group at the 5?-position is protected to obtain a novel purine nucleoside derivative (2) in a high yield. The derivative (2) is subjected to desulfurization, deprotection of R1 and, as necessary protection, deprotection, or modification of nucleic acid base moiety, to obtain the desired purine nucleoside (3). wherein each symbol is as defined in the specification.