The present invention is a process for the preparation of certain 5′-phosphoramidate nucleotide diastereoisomers. The phosphoramidates include those useful in the treatment of cancer such as NUC-3373 (5-fluoro-2′-deoxyuridine-5′-O-[1-naphthyl(benzyloxy-L-alaninyl)]phosphate).

The present invention is a process for the preparation of certain 5′-phosphoramidate nucleotide diastereoisomers. The phosphoramidates include those useful in the treatment of cancer such as NUC-3373 (5-fluoro-2′-deoxyuridine-5′-O-[1-naphthyl(benzyloxy-L-alaninyl)]phosphate).

Disclosed is a process for the preparation of Cangrelor in salt form by preparation and subsequent hydrolysis of an intermediate of formula (IV): ##STR00001## The process is characterized by the high yield and purity of the product, and can be used industrially.

An inorganic porous carrier including a linker of formula (1), wherein a mode diameter in a pore distribution is 0.04 μm to 1 μm, and a predetermined cumulative pore volume ratio is 30% or less [a bond * represents a linkage to the oxygen atom of a silanol group in an inorganic porous substance; n is an integer; R represents independently of each other an alkyl group containing 3 to 10 carbon atoms which may optionally have a substituent such as an alkoxy group; and L represents a single bond; an alkylene group of 1 to 20 carbon atoms; or an alkylene group containing 2 to 20 carbon atoms which contains —CH.sub.2-Q-CH.sub.2— group wherein any group Q selected from a group consisting of —O— etc. is inserted into at least one of —CH.sub.2—CH.sub.2— group constituting the alkylene group]; and a method for preparing a nucleic acid using the same.

##STR00001##

An inorganic porous carrier including a linker of formula (1), wherein a mode diameter in a pore distribution is 0.04 μm to 1 μm, and a predetermined cumulative pore volume ratio is 30% or less [a bond * represents a linkage to the oxygen atom of a silanol group in an inorganic porous substance; n is an integer; R represents independently of each other an alkyl group containing 3 to 10 carbon atoms which may optionally have a substituent such as an alkoxy group; and L represents a single bond; an alkylene group of 1 to 20 carbon atoms; or an alkylene group containing 2 to 20 carbon atoms which contains —CH.sub.2-Q-CH.sub.2— group wherein any group Q selected from a group consisting of —O— etc. is inserted into at least one of —CH.sub.2—CH.sub.2— group constituting the alkylene group]; and a method for preparing a nucleic acid using the same.

##STR00001##

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: ##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: ##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

The present invention relates to an alkoxyphenyl derivative capable of synthesizing an oligonucleotide by a quicker liquid phase synthesis method than in the prior art, a protected nucleoside and a protected nucleotide to which the alkoxyphenyl derivative is bonded, a method for producing an oligonucleotide using the same, and a method for selectively removing the alkoxyphenyl derivative moiety and the like. A compound represented by the general formula (1) or a derivative thereof:

##STR00001##

(In the formula, R each independently represents an optionally substituted alkyl group having 10 to 40 carbons. m represents an integer between 1 and 5. When m is 2 or more, a plurality of ROs may be the same or different. X represents O, S, NH, or NR.sup.N. n represents an integer from 1 to 4. R.sup.N represents an optionally substituted alkyl group having 1 to 6 carbons.)

The present invention relates to an alkoxyphenyl derivative capable of synthesizing an oligonucleotide by a quicker liquid phase synthesis method than in the prior art, a protected nucleoside and a protected nucleotide to which the alkoxyphenyl derivative is bonded, a method for producing an oligonucleotide using the same, and a method for selectively removing the alkoxyphenyl derivative moiety and the like. A compound represented by the general formula (1) or a derivative thereof:

##STR00001##

(In the formula, R each independently represents an optionally substituted alkyl group having 10 to 40 carbons. m represents an integer between 1 and 5. When m is 2 or more, a plurality of ROs may be the same or different. X represents O, S, NH, or NR.sup.N. n represents an integer from 1 to 4. R.sup.N represents an optionally substituted alkyl group having 1 to 6 carbons.)

An optically active segment for use in synthesis of a stereocontrolled oligonucleotide represented by the following formula (I), a method for producing the same, and a method for synthesizing a stereocontrolled oligonucleotide therefrom are provided. In formula, B is a protected/unprotected nucleoside base; R.sup.1 is substituted/unsubstituted aliphatic group; R.sup.2, R.sup.3 is a DMTr group or —P(R.sup.11)(NR.sup.12).sub.2; R.sup.11 is OCH.sub.2CH.sub.2CN, SCH.sub.2CH.sub.2CN, etc.; R.sup.12 is a substituted/unsubstituted aliphatic group or aromatic group; X is H, an alkyl, O-alkyl, etc.; Y is H, NHR.sup.13, a halogen, etc., or a hydroxyl group protected with an acyl, ether, or silyl, or forms an X—Y bond with X; and n is an integer of 0 or more and 4 or less.

##STR00001##