Rh(III)-Catalyzed spiroannulation of ketimines with cyclopropenones via sequential C-H/C-C bond activation.

An unprecedented Rh(III)-catalyzed [3+3]-spiroannulation of ketimines with cyclopropenones to access spiro[4,5]dienones has been developed. Sequential C-H/C-C bond activation and subsequent nucleophilic addition are disclosed in this process. This procedure represents the first example of the construction of spirolactams utilising cyclopropenones as 3C synthons. The remarkable advantages of this protocol are excellent chemo- and regio-selectivity, wide functional group tolerance, high reaction yields, and tolerance towards H2O.

Kangfuxin Liquid Ameliorates Dextran Sulfate Sodium (DSS)-Induced Acute Ulcerative Colitis in Mice by Modulating Immune Response and Suppressing Inflammation.

BACKGROUND The aim of this study was to determine the effect of kangfuxin liquid (KFXL) on inflammatory response, and its underlying mechanism in treating acute ulcerative colitis (UC) in mice induced by dextran sulfate sodium (DSS). MATERIAL AND METHODS Mice were provided drinking water containing DSS (3%) for 7 days to induce acute enteritis. The mice were divided into 6 groups: a control group, a DSS-induced (vehicle) group, a sulfasalazine (SASP) group, and low-, medium-, and high-dose kangfuxin liquid groups. Disease activity index (DAI), colon mucosa damage index (CMDI), histopathological score (HS), and organ index were monitored daily. The levels of interleukin-1ß (IL-1ß), interleukin-10 (IL-10) in serum and interleukin-17 (IL-17) and epidermal growth factor (EGF) in colon tissue were assessed by enzyme-linked immunosorbent assay (ELISA). Flow cytometry was used to assess the changes of T lymphocyte subsets in spleens of mice to evaluate the therapeutic effect of drugs on acute UC in mice. RESULTS Different doses of kangfuxin liquid reduced the DAI, CMDI, and HS scores (P<0.01 or P<0.05) of acute UC mice, reduced the level of IL-1ß and IL-17 in serum, increased the expression of IL-10 in serum and EGF in colon tissue, increased the number of CD3⁺ T cells, and decreased the level of CD4⁺ T cells and the ratio of CD4⁺/CD8⁺. CONCLUSIONS Kangfuxin liquid has a therapeutic effect on DSS-induced acute UC in mice, and its mechanism of action may be associated with regulating immune function and reducing intestinal inflammatory response.

Ag(I)-Catalyzed Addition of Cyclopropenones and Nitrones to Access Imides.

An unprecedented Ag-catalyzed addition reaction of cyclopropenones and nitrones to access imides was developed. Sequential C-C bond cleavage, N-O bond cleavage, and Mumm rearrangement were uncovered in this process. This protocol exhibited high efficiency, regioselectivity, good yields, and a broad tolerance of various functional groups.

Ag(I)-Catalyzed [3 + 2]-Annulation of Cyclopropenones and Formamides via C-C Bond Cleavage.

An unprecedented Ag-catalyzed [3 + 2]-annulation of cyclopropenones and DMF via C-C bond cleavage is disclosed. This protocol exhibited excellent chemo- and regio-selectivity, and tolerated various functional groups. More importantly, DMF served as the C═O bond in the cycloaddition reaction, providing an efficient way to construct γ-aminobutenolides. In addition, transesterification reaction occurred when DMF was replaced by esters.