Combinatorial protecting group strategy for multifunctional molecules
AssigneeHK Pharmaceuticals, Inc.
InventorsHubert Koster, Eckart Leikauf
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Abstract
The use of protection schemes and solid phase synthesis reactions to generate molecules of core structure M, which have a plurality of moieties, each of which can be individually deprotected or subsequently derivatized are provided. In one process, M is a multifunctional low molecular weight compound, such as a saccharide, aminosugar, deoxysugar, nucleoside, nucleotide, coenzyme, amino acid, lipid, steroid, vitamin, hormone, alkaloid, or small molecule drug. In another process, M is an oligomeric compound, such as an oligosaccharide, oligonucleotide, peptide or protein.
Claims7
A process for generating a combinatorial library, comprising the steps of:
- (a) preparing a plurality of immobilized molecules selected from a nucleoside and a nucleotide;
- wherein each molecule contains 3 reactive moieties, each reactive moiety being blocked by a blocking group, wherein the three blocking groups on each immobilized molecule are independently removable under three different conditions;
- and
- (b) removing each blocking group and derivatizing the resulting reactive moiety in a preprogrammed, regioselective manner;
- wherein each member of the plurality of immobilized molecules is uniquely derivatized at at least one reactive moiety with a unique substituent, thereby generating a combinatorial library.
Dependencies are inferred from the claim text.