Stereoselective method for the preparation of nucleosides

Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system

Reexamination Certificate

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C544S212000, C544S223000, C544S262000, C544S280000, C544S314000, C544S317000, C546S117000, C546S118000, C546S280400

Reexamination Certificate

active

11399502

ABSTRACT:
A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A):wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).

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