Universitaet Hamburg

Universitat Hamburg

Chris Meier

Viktoria Caroline Tonn

Saskia Wolf

Tristan Gollnest

Tobias Nack

Svenja Warnecke

Lina Weinschenk

Jens O Thomann

Viktoria Tonn

Jens Thomann

Compounds which can be used as prodrugs, in particular nucleoside diphosphate and triphosphate prodrugs, and a method for producing these compounds. The aim is to provide improved di- and/or triphosphate prodrugs, in particular nucleotide or nucleotide analog prodrugs. This is achieved in one aspect by providing bioreversibly and asymmetrically masked di- and triphosphate compounds, in particular nucleoside diphosphate and nucleoside triphosphate compounds or the analogs thereof. The masking only occurs at the terminal phosphate, i.e. at the &#x3b2;- or &#x3b3;-phosphate, whereas the masking of the internal phosphate is omitted.

Di- and triphosphate prodrugs

The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method, a cyclosaligenyl nucleotide is produced first, to which a linker is added, which is used to perform the immobilization on a solid phase. A subsequent reaction with corresponding nucleophiles results in the desired phosphate-bridged nucleoside conjugates, which can then again be cleaved from the solid phase-bound linker.

Method for the solid phase-based production of phosphate-bridged nucleoside conjugates

The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method a nucleophile is first dissolved in a non-aqueous solvent and dried, and a cyclosaligenyl phosphate compound is subsequently added to the solution.

Method for producing phosphate-bridged nucleoside conjugates

The present invention relates to a method for stereoselective synthesis of phosphorus compounds, whereby in the first reaction step a chiral auxiliary on the phosphorus atom of phosphoryl chloride, thiophosphoryl chloride or phosphorus trichloride is covalently bonded, the product from the first reaction step is reacted in the following step with an alcohol, thiol, or amine as the nucleophile in the presence of a base, and in the last step the chiral auxiliary is displaced from the product of the following step by a nucleophile.

Method for the stereoselective synthesis of phosphorus compounds

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Jork, Germany

Chris Meier