New synthetic methodologies found during API process R&D are also able to support drug discovery activities.
For example, we have developed convenient and diversified synthetic methods for pharmacore of drug candidates (e.g. heterocycle), and a reliable functional group transformation method, etc. The synthetic methods can contribute to accelerating drug discovery research timeline, providing large amount of the key intermediates of medicinal chemistry.
| Examples of synthesis | paper·oral presentation |
|---|---|
| Synthetic reagent for quinolines (Novel vinamidinium salt) | Tetrahedron, 2014, 70, 2370 |
| Synthetic method for cores of kinase inhibitors (α-carboline) | Tetrahedron, 2014, 70, 5550 J. Org. Chem, 2015, 80, 1564 Tetrahedron, 2017, 73, 5946 Interphex Japan (2014) |
| Synthetic method for pyrazoles | Tetrahedron, 2015, 71, 2833 Interphex Japan (2016) |
| Synthetic method for naphthalenes (Analogues of lignan type natural products) | Tetrahedron, 2006, 62, 8539 Outlook of support research for drug discovery (CMC Publishing, 2008) |
| Conversion of phenol to aniline (effective Smiles rearrangement) | Org. Lett. 2005, 7, 3629 Organic Syntheses, 2007, 84, 325 |
SPERA provides CMC solutions from early-stage through new drug application.
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