Process for the preparation of nucleotides
AssigneesInstitute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
InventorsPurushortham Vemishetti, Paul R. Brodfuehrer, Henry G. Howell, Chester Sapino, Jr.
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Abstract
The present invention relates to a novel and economical process for the synthesis of HPMP-substituted nucleotide antiviral compounds. Also disclosed are novel intermediates produced in the process for the preparation of HPMPC.
Claims12
A process for preparing a compound of formula (Ia) or (Ib) ##STR5## wherein B is a purine or pyrimidine base, which comprises the steps of (a) reacting, in a reaction mixture, B' in the presence of a base with a compound of formula (IIb) to form the intermediate (IIIb) ##STR6## and, without separating intermediate (IIIb) from the reaction mixture, reacting intermediate (IIIb) with a phosphonate of formula (IV) ##STR7## to form an intermediate of formula (V) ##STR8## where B' is a purine or pyrimidine base or a suitably protected purine or pyrimidine base, R.sup.1 is a hydroxy protecting group, L is a leaving group, and R.sup.2 is a phosphonic protecting group selected from alkyl having 1-5 carbon atoms;
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- (b) replacing the R.sup.1 hydroxy protecting group, and optionally, the R.sup.2 or B' protecting groups, with hydrogen to form the product of formula (Ia) or (Ib).
Dependencies are inferred from the claim text.