Copper-Catalyzed Asymmetric Nucleophilic Substitutions of TsSCF: Synthesis of Chiral SCF-Containing Compounds.

By employing electrophilic TsSCF as an efficient SCF source, we reported Cu/ (chiral sulfoxide-phosphine ligand)-catalyzed enantioselective nucleophilic substitutions. Under this protocol, α-pyridyl-α-fluoro esters as latent carbon nucleophiles, compounds containing a C-SCF stereocenter along with azacycles and fluorine atoms, were obtained in good yields and enantioselectivities under mild conditions (up to 68% yield, 92% ee).

Enantioselective Cu-Catalyzed Nucleophilic Substitutions of Polyfluoroarenes: Synthesis of Chiral Polyfluoroaryl Diarylmethanes.

Optically pure diarylmethanes are frequently presented in pharmaceuticals and bioactive molecules. However, minor efforts have been devoted to chiral polyfluoroarene-containing diarylmethanes, and their synthesis is still challenging. Herein, we describe an enantioselective Cu/sulfoxide phosphine () catalyzed nucleophilic substitution reaction by using polyfluoroarenes as the polyfluoroaryl reagent.

A Novel Method to Construct 2-Aminobenzofurans via [4 + 1] Cycloaddition Reaction of In Situ Generated -Quinone Methides with Isocyanides.

A new approach for the synthesis of 2-aminobenzofurans has been described via Sc(OTf) mediated formal cycloaddition of isocyanides with the in situ generated -quinone methides (-QMs) from -hydroxybenzhydryl alcohol. Notably, as a class of readily available and highly active intermediates, -QMs were first used in the construction of benzofurans. This [4 + 1] cycloaddition reaction provides a straightforward and efficient methodology for the construction of 2-aminobenzofurans scaffold in good yield (up to 93% yield) under mild conditions.

Enantioselective Cu-Catalyzed Nucleophilic Addition of Fluorinated Reagents: C-C Bond Formation for the Synthesis of Chiral Vicinal Difluorides.

Herein we described the first enantioselective Cu/sulfoxide phosphine (SOP) complex catalyzed nucleophilic addition of fluorinated enolates to -difluoroalkenes. The enantioenriched vicinal difluorides, containing a chiral tertiary fluoride and a fluoroalkene, were successfully afforded via C-C bond formation in good yields (up to 94% yield), high /-selectivity (5:1 → 50:1 for -isomer), and excellent enantioselectivities (up to 98.5:1.

Enantioselective Copper-Catalyzed Electrophilic Sulfenylation of Cyclic Imino Esters.

Herein we report an enantioselective sulfenylation of cyclic imino esters with the efficient and versatile sulfenylation reagent -alkyl 4-methylbenzenesulfonothioates. By utilizing the Cu/Bu-Phosferrox catalytic system, we can assemble diverse -alkyl groups into the cyclic imino esters under mild conditions in good yields and with excellent enantioselectivities. Remarkably, this method demonstrates a high tolerance of diverse functional groups and proves to be applicable in the late-stage functionalization of pharmaceuticals.

Associations of Prostate-Specific Antigen, Prostate Carcinoma Tissue Gleason Score, and Androgen Receptor Expression with Bone Metastasis in Patients with Prostate Carcinoma.

BACKGROUND Prostate carcinoma (PCa) is often not diagnosed until advanced disease with bone metastasis. Predictive factors for bone metastasis are required to improve patient outcomes. The study aimed to analyze the factors associated with bone metastases in newly diagnosed patients with PCa.

[Predictive factors for bone metastases of prostate cancer].

Objective: To investigate the correlation between a diverse of clinical factors and bone metastases of prostate cancer.

Methods: The clinical data of 80 patients with prostate cancer were collected and analyzed. The correlations of age, alkaline phosphotase (ALP), prostate specific antigen (PSA), erythrocyte sedimentation rate (ESR), Gleason score, and expressions of androgen receptor (AR) and Ki-67 with bone metastases were analyzed by one-way ANOVA and Logistic regression analysis.

Comparison of long-term impact of immunosuppressants at therapeutic doses on hepatic function and histological changes in unilateral nephrectomized rats.

Cyclosporine, tacrolimus and sirolimus are commonly used in renal transplant recipients to prevent rejection. Various adverse effects of these agents on the multiple organ system have been reported clinically. However, animal studies are necessary to determine and compare these effects on individual organ given the presence of multiple confounding factors and multi-pharmacy in clinical settings.

Long-term impact of immunosuppressants at therapeutic doses on male reproductive system in unilateral nephrectomized rats: a comparative study.

Cyclosporine, tacrolimus, and sirolimus are commonly used in renal transplant recipients to prevent rejection. However, information for comparative effects of these agents on the male productive system is extremely limited and controversial. In a physiologically and clinically relevant rat model of unilateral nephrectomy, we demonstrated that long-term oral administration of both cyclosporine and sirolimus at doses equivalent to the therapeutic levels used for postrenal transplant patients significantly affects testicular development and the hypothalamic-pituitary-gonadal axis accompanied by profound histological changes of testicular structures on both light and electron microscopic examinations.

Approximately diagonalizing matrices over C(Y).

Let X be a compact metric space which is locally absolutely retract and let ϕ: C(X) → C(Y,M(n)) be a unital homomorphism, where Y is a compact metric space with dim Y ≤ 2. It is proved that there exists a sequence of n continuous maps α(i,m): Y → X (i = 1,2,…,n) and a sequence of sets of mutually orthogonal rank-one projections {p(1,m),p(2,m),…,p(n,m)} C(Y,M(n)) such that [see formula]. This is closely related to the Kadison diagonal matrix question.