Universal Supports

UNYLINKER^TM Universal Support¹ for synthesis of Oligonucleotides:

As the popularity of oligonucleotides has increased, demand for producing large and small size batches of natural and modified oligonucleotides has increasing at very fast pace. Additionally, there has been an increasing emphasis on reducing the costs of oligonucleotide synthesis with improved purity and in a greater yield.

• ChemGenes offers novel UnyLinker Universal Supports (Catalog #: N-4000) for Synthesis of Oligonucleotides.
• UnyLinker Universal Support 1 (Scheme 1) is a conformationally rigid and chemically stable bridge head ring oxygen atom carrying a conventional 4,4′-dimethoxytrityl (DMTr) and succinyl groups locked in a syn orientation.¹

 Salient Features of UnyLinker Universal Supports:

1. UnyLinker supports avoid synthesizing four different supports, thereby avoiding difficult synthesis of 2′ or 3′-modified nucleoside based on support.
2. Cost reduction due to single support for the oligo synthesis instead of several supports.
3. Releases work load of QC and material management and testing of many products verses a single support.
4. UnyLinker supports are fully compatible with standard phosphoramidite reagents and synthesis conditions, observed average coupling efficiency of >99% per step.
5. UnyLinker undergoes quantitative cleavage from support with standard ammonia or methylamine deprotection conditions as illustrated in Scheme 1.
6. Examples demonstrating the versatile nature of UnyLinker supports are shown by syntheses of different chemistries such as 2′-deoxy, 2′-O-methyl, 2′-O-methoxyethyl, Lock nucleic acids (LNA), 2′-r-fluoro nucleic acids (FANA), conjugates such as 5′-phosphate monoester and biotin, and phosphate diester and phosphorothioate backbone modifications.
7. Improvement in the quality of oligonucleotides synthesized, since the quality of succinates can vary from batch to batch and supplier to suppliers.
8. UNYLINKER universal support does not contribute any atom to API and hence need not be classified as a starting material. Therefore offer major advantage when dealing with QA and FDA.

Now, ChemGenes offers UnyLinker on Hybrid Support (Proprietary Product) with ­loading up to 150 umol/g.

Scheme 1: Proposed mechanism for deprotection and release of oligonucleotide using UnyLinker universal support.

References:

1. Ravikumar, V. T. Org. Pro. Res. & Dev. 2008, 12, 399-410; Ravikumar, V. T. U.S. Patent number 7,202,264.

*UNYLINKER^TM is a trademark of Isis Pharmaceuticals, Inc. The above products are covered under Isis patent #7,202,264 and ChemGenes Corp. holds world wide marketing rights.