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1.
Org Lett ; 21(11): 4111-4115, 2019 06 07.
Article in English | MEDLINE | ID: mdl-31124683

ABSTRACT

A protocol for highly enantioselective hydrogenation of racemic α-arylamino lactones with catalysis by site-specifically modified chiral spiro iridium complexes has been developed. With the optimized catalyst, racemic α-arylamino-γ-lactones and α-arylamino-δ-lactones could be hydrogenated to the corresponding chiral 2-amino diols with good to excellent enantioselectivities.

2.
Onco Targets Ther ; 10: 2249-2256, 2017.
Article in English | MEDLINE | ID: mdl-28461759

ABSTRACT

This study aimed to explore the relationship between computed tomography morphology and prognosis of patients with stage I non-small cell lung cancer (NSCLC). From May 2009 to May 2011, a total of 124 patients diagnosed with stage I NSCLC were included. All patients had complete chest computed tomography scans. Five-year follow-up was conducted. Univariate and multivariate Cox regression analyses were performed to estimate the prognostic factors for patients with stage I NSCLC. The 5-year survival rate was 67.74% (84/124). The 5-year survival rates of patients with stage T1a, T1b, and T2a were 89.19%, 75.00%, and 41.86%, respectively. The 5-year survival rates of patients with homogeneity, inhomogeneity, vacuole, and cavity were 68.42%, 72.09%, 59.46%, and 83.33%, respectively. The 5-year survival rates of patients with different margin features were 83.33% (slick margin), 79.73% (lobulation sign), and 39.47% (short burr). The 5-year survival rates of patients with normal, halo, vessel convergence, bronchial transection, and vascular bundle thickening were 84.38%, 72.73%, 71.79%, 52.00%, and 47.06%, respectively. The 5-year survival rates of patients with normal and pleura thickening/indentation were 81.93% and 39.02%. Univariate analysis demonstrated that tumor node metastasis staging, tumor margin, tumor periphery, and pleural invasion were related to the prognosis of stage I NSCLC patients. Cox regression analysis confirmed that T2a stage, pleura thickening/indentation were independent risk factors for poor prognosis of stage I NSCLC. In conclusion, our findings indicate that T2a stage, pleura thickening/indentation might be prognostic factors in stage I NSCLC.

3.
Org Lett ; 19(1): 118-121, 2017 01 06.
Article in English | MEDLINE | ID: mdl-27936808

ABSTRACT

A highly efficient Ir-catalyzed asymmetric hydrogenation of racemic ß-keto lactams via dynamic kinetic resolution (DKR) for the synthesis of optically active ß-hydroxyl lactams has been described. With the Ir-SpiroSAP catalyst, a series of racemic ß-keto lactams including ß-keto γ-, δ-, and ε-lactams were hydrogenated to chiral ß-hydroxy lactams in high yields (87-99%) with excellent enantio- and diastereoselectivity (83-99.9% ee, syn/anti: 97:3->99:1) at low catalyst loading under mild reaction conditions. This efficient method has been successfully applied in the synthesis of the chiral intermediate of fluoroquinolone antibiotic premafloxacine.


Subject(s)
Iridium/chemistry , beta-Lactams/chemistry , Anti-Bacterial Agents/chemical synthesis , Catalysis , Drug Design , Fluoroquinolones/chemical synthesis , Hydrogenation , Kinetics , Molecular Structure , Pyrroles/chemical synthesis , Stereoisomerism
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