In a recent EurJOC paper Enamine chemists have reported an efficient synthesis of twelve novel cyclic amines and carboxylic acids containing diazirine moiety. Although diazirines are well-known photoaffinity probes and are widely used in biomedical research, only few spirocyclic derivatives were known previously. But now, our stereochemically diverse spirocyclic library includes diazirine derivatives of four-, five-, six- and seven-membered functionalized building blocks, which can be easily incorporated into a ligand by the formation of amide bond.
In a joint venture, Enamine and BioSolveIT built the world's largest chemical space and made it ultra-fast searchable. And now using REAL Space Navigator you can access 11 billion compounds from Enamine REAL space and do efficient hit exploration, from finding previously unknown analogs to scaffold hopping. The REAL space encoded with more than 100 Enamine synthesis protocols and in-stock building blocks, provides an escape from availability bias of current stock screening collections towards IP free areas. The REAL compounds will be synthesized in 3-4 weeks with an exceptional success rate of 80% and above.
Larotrectinib (VITRAKVI®, Loxo Oncology Inc. and Bayer) is an inhibitor of receptors TrkA, TrkB, and TrkC which was approved by FDA for adult and pediatric patients with solid tumors that have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, that are either metastatic or where surgical resection is likely to result in severe morbidity, and who have no satisfactory alternative treatments or whose cancer has progressed following treatment on November 26, 2018.
Lofexidine (Lucemyra®, US Woldmeds LLC) is a medication historically used to treat high blood pressure which was approved by FDA as a first non-opioid drug for the mitigation of withdrawal symptoms to facilitate abrupt discontinuation of opioids in adults on May 16, 2018. Lucemyra is not a treatment for opioid use disorder (OUD), but can be used as part of a broader, long-term treatment plan for managing OUD.
Enamine has the world’s largest catalogue of building blocks which is monthly enriched with ca. 2,000 newly designed and synthesized compounds. Most of these compounds have been previously unknown and may already provide elegant solutions to your today’s challenges.