Search & Buy on-line at EnamineStore.com Look for more at Chem-Space.com [email protected], www.enamine.net References 1. www.drugbank.ca 2. G. Wuitschik et al. Angew. Chem. Int. Ed. 2008, 4512. 3. G. Wuitschik et al. J. Med. Chem. 2010, 3227. 4. A. Shcherbatiuk et al. Tetrahedron 2013, 3746. 5. A. D. Tereshchenko et al. Tetrahedron 2017, 750. 6. A. Kirichok et al. Chem. Eur. J. 2018, 5444. N H O N H O N H O N H O N H O N H O N H O N H O N H O EN300-81038 EN300-113203 EN300-96084 EN300-99316 EN300-102855 EN300-123162 EN300-91609 EN300-82709 EN300-122734 EN300-114690 EN300-119630 N H O O N H O EN300-89738 N H O N H O N H O N H O N H O N H O N H O EN300-105822 N H O H H N H H H O N H H H O N H O N H O EN300-89737 O N H O N H H H N H O F F N H O CF 3 N H O CF 3 EN300-225470 EN300-312472 EN300-208936 EN300-268654 EN300-247469 EN300-187643 EN300-82592 EN300-151039 EN300-261880 EN300-93028 EN300-121856 EN300-53465 EN300-83277 N H O EN300-200454 N H O EN300-305645 EN300-142416 N H O O N H EN300-6496797 H H N H O O N H N H O H H H H H H EN300-93931 EN300-79411 EN300-261920 O N H EN300-82710 N H O EN300-55844 N H O CHF 2 EN300-73253 EN300-82713 F F N H O EN300-89741 F F N H F F O EN300-52620 EN300-1703705 N H O CF 3 CF 3 N H O O S O N H O O O N H H H EN300-1387244 NH N H O EN300-6493026 H H EN300-1601327 EN300-131408 H H H H H H We offer >100 unique morpholine analogues on a 5-50 g scale from stock. N H O Morpholine bioisosteres N H O Bicyclic N H O H H N H O Spiro Bridged Fused Design More than 20 FDA-approved drugs contain the morpholine moiety, although it is often metabolically labile. 1 Morpholine-based analogues may advantageously alter important pharmacokinetic properties such as lipophilicity and metabolic stability when grafted onto molecular scaffolds. 2,3 Herein we have designed and synthesized a library of morpholine analogues for drug design. 4-6 N S N N H O N O N O CF 3 N N N F N H H N O H N CO 2 H O N N N O NH NH Cl Cl NH O F 3 C O H N H N O N N N N N N O O HN N N O HN N O O N Boc mPGES-1 inhibitor WO 2012/076673 A1 Boehringer Ingelheim Peptide deformylase inhibitor EP 2015/2217226 B1 GlaxoSmithKline Janus kinase inhibitor US 2018/10072025 B2 Merck&Co. Alpha 7 positive allosteric modulator EP 2015/2504333 B1 Janssen Pharm. Inhibitor of PI3K US 2013/109670 A1 Pfizer Introduction Morpholine Bioisosteres for Drug Design