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A palladium-catalyzed asymmetric annulative dearomatization of phenols with butene dicarbonate is reported, enabling twofold decarboxylative allylation to regioselectively produce a range of spirocyclohexadienones with 29-95% yields and 74-99% ee. A catalytic dearomative formal [4 + 2] cyclization of 1,1'-biphenyl-2,4'-diols delivered spiro[chromane-4,1'-cyclohexane]-2',5'-dien-4'-ones with high enantioselectivity, whereas enantioenriched spiro[cyclohexane-1,4'-quinoline]-2,5-dien-4-ones were generated starting from 2'-amino-[1,1'-biphenyl]-4-ols as 1,4-dinucleophiles.
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A palladium-catalyzed asymmetric annulative allylic alkylation reaction of 2-[(1H-indol-2-yl)methyl]malonates with (E)-but-2-ene-1,4-diyl dicarbonates is described, leading to the regio- and enantioselective synthesis of dihydropyrido[1,2-a]indoles with a chiral cyclic allyl stereocenter adjacent to the ring-junction nitrogen atom in moderate to good yields. The salient features of this protocol include mild conditions, a broad substrate scope, and good compatibility with substituents as well as high regio- and stereoselectivities, providing a catalytic asymmetric entry for fabricating chiral pyridoindole scaffolds.
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Compostos Alílicos , Estereoisomerismo , Alquilação , Catálise , IndóisRESUMO
Informatization is an effective way to promote the reform and innovation of higher education and improve its quality. Virtual simulation teaching is indispensable in the educational informatization. Here, we describe the development and current situation of virtual simulation teaching, and introduce electronic standardized patient (ESP) based-virtual human body system powered by the real-time human physiological parameters. We also discuss how to build an ESP-based community in the teaching of human physiology, preclinical integrated case learning and other teaching projects. These ESP-based virtual simulation projects display the advantages of interdisciplinary fusion and the combination of basic and clinical knowledge, and open up the third type of functional experiments. Therefore, ESP-based virtual simulation teaching platform presumably becomes a considerable option for the first-class course construction in physiology.
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Humanos , Simulação por Computador , Eletrônica , Aprendizagem , Interface Usuário-ComputadorRESUMO
Objective To compare the proteomic spectrum of cerebrospinal fluid between patients with hypertensive cerebral hemorrhage before surgery and patients with hypertension,between patients with hypertensive cerebral hemorrhage before surgery and after surgery,between healthy controls and patients with hypertension,and find out disease-specific proteins (DSPs) closely correlated with hypertensive cerebral hemorrhage to explore their roles in hypertensive cerebral hemorrhage. Methods Sixty-nine cerebrospinal fluid samples from patients with hypertensive cerebral hemorrhage (before operation,n=24; after operation,n=20),from patients with hypertension (n=10),and from healthy controls (n=15) were detected by surface-enhanced laser desorption/ionization time-of-flight mass spectrometry (SELDI-TOF-MS).Data were analyzed by Biomark Wizard software(Ciphergen Inc.),and DSPs closely correlated with hypertensive cerebral hemorrhage were searched by protein databases.Results By comparing and analyzing the proteomic spectrum of patients from group of hypertensive cerebral hemorrhage before surgery and group of hypertension, from groups of hypertensive cerebral hemorrhage before surgery and after surgery,from group of healthy controls and group of hypertension,the candidate protein peaks were screened,and the number of them was 23,16,and 0,respectively.The 23 different protein peaks between patients with hypertensive cerebral hemorrhage before surgery and patients with hypertension were analyzed by Biomarker pattern software, showing 6 different protein peaks were important; through searching the database according to molecular weight,we noted that these protein might be brain natriuretic peptide (BNP),human neutrophil peptide alpha-defensin (HNP-2),reactive oxygen species (ROS), PCYOX, secretory carrier membrane protein 4 (SCAMP4) and interleukin-31. Conclusion Differentially expressed proteins from patients with hypertensive cerebral hemorrhage could be screened after analyzing the map of cerebrospinal fluid protein mass spectrum,and these differentially expressed proteins are expected to be the molecular markers to forecast hypertensive cerebral hemorrhage.
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This study was conducted to assess the effects of dietary corn oil and vitamin E supplementation on fatty acid (FA) profiles and abundances of acetyl-CoA carboxylase (ACC) and Delta(9) stearoyl-CoA desaturase (SCD) mRNA of Hu sheep. Animals were allocated to three dietary treatments: basal and supplemented with 3% corn oil (CNO), or CNO plus 500 mg/kg vitamin E (COE). The experiment lasted for 10 weeks. No differences were observed in growth performance and carcass qualities among the three treatments (P > 0.05). Feeding CNO and COE diets increased polyunsaturated FAs including cis 9 trans 11 conjugated linoleic acid, and decreased saturated FA in longissimus muscle (P < 0.05). The mRNA abundances of ACC and SCD as detected by real-time PCR were reduced (P < 0.05) in liver and subcutaneous fat by supplementary oil, while the SCD mRNA level in longissimus muscle was also reduced (P < 0.05). Inclusion of vitamin E did not have further effects on mRNA abundances of these two enzymes. It is suggested that dietary corn oil supplementation may reduce FA biosynthesis and influence FA profiles in Hu sheep through decreased expression of both ACC and SCD genes.
Assuntos
Acetil-CoA Carboxilase/genética , Óleo de Milho/administração & dosagem , Ácidos Graxos/biossíntese , Expressão Gênica/efeitos dos fármacos , Ovinos/genética , Estearoil-CoA Dessaturase/genética , Vitamina E/administração & dosagem , Animais , Suplementos Nutricionais , Masculino , Músculo Esquelético/metabolismo , RNA Mensageiro/metabolismo , Ovinos/metabolismoRESUMO
In the title compound, C(3)H(5)N(2) (+)·C(7)H(4)NO(4) (-), the benzene ring forms a dihedral angle of 40.60â (5)° with the imidizolium ring. The nitro-benzoate anion is approximately planar: the benzene ring makes dihedral angles of 3.8â (3) and 3.2â (1)° with the nitro and carboxyl-ate groups, respectively. In the crystal structure, the cations and anions are linked by inter-molecular N-Hâ¯O hydrogen bonds, forming a zigzag chain along the b axis.