Stereoselective Synthesis of Baloxavir Marboxil Using Diastereoselective Cyclization and Photoredox Decarboxylation of l-Serine.

Baloxavir marboxil (; BXM) is a potent drug used for treating influenza infections. The current synthetic route to BXM () is based on optical resolution; however, this method results in the loss of nearly 50% of the material. This study aimed to describe an efficient and simpler method for the synthesis of BXM.

Stereoselective Construction of Spiro-Fused Tricyclic Frameworks by Sequential Reaction of Enynes, Imines, and Diazoalkenes with Rh(I) and Rh(II) Catalysts.

Stereoselective construction of spiro-fused tricyclic compounds from enynes having a tethered imine with diazoalkenes was achieved by Rh(I)- and Rh(II)-catalyzed sequential reactions. This method consists of three reactions, i.e.

Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125).

Monopolar spindle 1 (Mps1) is essential for centrosome duplication, the spindle assembly check point, and the maintenance of chromosomal instability. Mps1 is highly expressed in cancer cells, and its expression levels correlate with the histological grades of cancers. Thus, selective Mps1 inhibitors offer an attractive opportunity for the development of novel cancer therapies.

Asymmetric 1,3-dipolar cycloadditions of N-benzyl and N-diphenylmethyl nitrones and alpha,beta-unsaturated aldehydes catalyzed by bis-titanium chiral Lewis acids.

Bis-titanium chiral Lewis acids that contain two oxygen-bridged titanium centers were successfully applied to the asymmetric 1,3-dipolar cycloaddition of nitrones and alpha,beta-unsaturated aldehydes. The introduction of the diphenylmethyl group as the N substituent on the nitrones, with the aim of destabilizing the nitrone-Lewis acid complex, led to the drastic enhancement of not only the reactivity but also the enantioselectivity. By employing this approach, 1,3-dipolar cycloadditions of nitrones and the rather unreactive methacrolein were facilitated to give cycloadducts that bear one all-carbon quaternary center with unique regioselectivity and excellent stereoselectivity.