C07H1/00

Method for preparing oligonucleic acid compound

A method for subjecting a compound [A] having a hydroxyl group or a primary or secondary amino group and a compound [B] having a substituent containing a phosphorus atom to a condensation reaction to prepare a compound [C] represented by the following general formula [C]: ##STR00001##
wherein the condensation reaction is carried out in a mixed solvent containing a polar solvent and a halogen solvent as a reaction solvent.

Method for preparing trifluridine

The present application relates to a method for preparing trifluridine, comprising reacting a compound of formula III with a compound of formula IV in a first solvent in the presence of an acid to obtain a compound of formula II, and performing further reaction to obtain trifluridine.

SYNTHESIS OF REVERSIBLE NUCLEOTIDE TERMINATORS BY IN-SITU THIO-ALKYL GROUP TRANSFER FOR USE IN DNA SEQUENCING BY SYNTHESIS

The invention is directed to a method for production of a deoxynucleotide triphosphate according to general formula (7)

##STR00001## wherein B is a nucleobase and R is an alkyl group having 1 to 4 carbon atoms and n is an integer from 1 to 10 by reaction of reaction precursor of compound 6

##STR00002## wherein R.sub.1, R.sub.2 and R.sub.3 are independently H, O-Alkyl with alkyl residues having 1 to 4 carbon atoms or halogen and n is an integer from 1 to 10 with dialkyl(alkylthio)sulfonium salt (8B)

##STR00003## wherein R.sub.4, R.sub.5 R.sub.6 are independently alkyl residues having 1 to 4 carbon atoms and X is selected from the group consisting of BF.sub.4.sup.−, F.sup.−, Cl.sup.−, Br.sup.−, I.sup.−, SO.sub.4.sup.2−, SO.sub.3.sup.2− in aqueous solution having a pH between 3 and 7.

SYNTHESIS OF REVERSIBLE NUCLEOTIDE TERMINATORS BY IN-SITU THIO-ALKYL GROUP TRANSFER FOR USE IN DNA SEQUENCING BY SYNTHESIS

The invention is directed to a method for production of a deoxynucleotide triphosphate according to general formula (7)

##STR00001## wherein B is a nucleobase and R is an alkyl group having 1 to 4 carbon atoms and n is an integer from 1 to 10 by reaction of reaction precursor of compound 6

##STR00002## wherein R.sub.1, R.sub.2 and R.sub.3 are independently H, O-Alkyl with alkyl residues having 1 to 4 carbon atoms or halogen and n is an integer from 1 to 10 with dialkyl(alkylthio)sulfonium salt (8B)

##STR00003## wherein R.sub.4, R.sub.5 R.sub.6 are independently alkyl residues having 1 to 4 carbon atoms and X is selected from the group consisting of BF.sub.4.sup.−, F.sup.−, Cl.sup.−, Br.sup.−, I.sup.−, SO.sub.4.sup.2−, SO.sub.3.sup.2− in aqueous solution having a pH between 3 and 7.

NOVEL MIMETICS OF HEPARIN OLIGOSACCHARIDES
20230012702 · 2023-01-19 ·

The present disclosure relates to disaccharides with defined sulfation patterns, and oligosaccharide mimetics comprising the disaccharides as repeating units linked in a head to tail fashion. The present disclosure further relates to methods of making the same, and to methods of using the same to mediate cell proliferation, cell differentiation, amyloid plaque formation, anti-coagulation, and neuronal growth.

NOVEL MIMETICS OF HEPARIN OLIGOSACCHARIDES
20230012702 · 2023-01-19 ·

The present disclosure relates to disaccharides with defined sulfation patterns, and oligosaccharide mimetics comprising the disaccharides as repeating units linked in a head to tail fashion. The present disclosure further relates to methods of making the same, and to methods of using the same to mediate cell proliferation, cell differentiation, amyloid plaque formation, anti-coagulation, and neuronal growth.

METHOD FOR PRODUCING OLIGONUCLEIC ACID COMPOUND
20230018780 · 2023-01-19 · ·

The present invention relates to a method for producing a compound [C] of the general formula [C] by subjecting a compound [A] having a hydroxyl group or a primary or secondary amino group and a compound [B] having a phosphorous atom-containing substituent group of the general formula [1] to a condensation reaction, characterized in that the method is carried out in the presence of at least one reaction accelerator selected from the group consisting of a quaternary ammonium salt, a quaternary imidazolium salt, a quaternary morpholinium salt, a quaternary phosphonium salt, a quaternary piperidinium salt, a quaternary pyridinium salt, a quaternary pyrrolidinium salt and a quaternary sulfonium salt.

METHOD FOR PRODUCING OLIGONUCLEIC ACID COMPOUND
20230018780 · 2023-01-19 · ·

The present invention relates to a method for producing a compound [C] of the general formula [C] by subjecting a compound [A] having a hydroxyl group or a primary or secondary amino group and a compound [B] having a phosphorous atom-containing substituent group of the general formula [1] to a condensation reaction, characterized in that the method is carried out in the presence of at least one reaction accelerator selected from the group consisting of a quaternary ammonium salt, a quaternary imidazolium salt, a quaternary morpholinium salt, a quaternary phosphonium salt, a quaternary piperidinium salt, a quaternary pyridinium salt, a quaternary pyrrolidinium salt and a quaternary sulfonium salt.

TRITERPENE SAPONIN ANALOGUES

The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases.

TRITERPENE SAPONIN ANALOGUES

The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases.