Synthesis of Polycyclic Imidazolidinones via Amine Redox-Annulation

α-Ketoamides undergo redox-annulations with cyclic secondary amines, such as 1,2,3,4-tetrahydroisoquinoline, pyrrolidine, piperidine, and morpholine. Catalytic amounts of benzoic acid significantly accelerate these transformations. This approach provides polycyclic imidazolidinone derivatives in typically good yields

Synthesis of Polycyclic Imidazolidinones via Amine Redox-Annulation

α-Ketoamides undergo redox-annulations with cyclic secondary amines, such as 1,2,3,4-tetrahydroisoquinoline, pyrrolidine, piperidine, and morpholine. Catalytic amounts of benzoic acid significantly accelerate these transformations. This approach provides polycyclic imidazolidinone derivatives in typically good yields

Selective Fluorescence Detection of Cysteine over Homocysteine and Glutathione Based on a Cysteine-Triggered Dual Michael Addition/Retro-aza-aldol Cascade Reaction

In this work, a cysteine (Cys)-triggered dual Michael addition/retro-aza-aldol cascade reaction has been exploited and utilized to construct a fluorescent probe for Cys for the first time. The resulting fluorescent probe 8-alkynylBodipy <b>1</b> contains an activated alkynyl unit as Michael receptor and a Bodipy dye as fluorescence reporter and can highly selectively detect Cys over homocysteine (Hcy)/glutathione (GSH) as well as other amino acids with a significant fluorescence off–on response (∼4500-fold) and an ultralow detection limit (0.38 nM). The high selectivity of <b>1</b> for Cys could be attributed to a kinetically favored five-membered cyclic intermediate produced by the dual Michael addition of Cys with the activated alkynyl unit of <b>1</b>. The big fluorescence off–on response is due to the subsequent retro-aza-aldol reaction of the five-membered cyclic intermediate that results in the release of a highly fluorescent 8-methylBodipy dye <b>2</b>. The probe has been successfully used to detect and image Cys in serum and cells, respectively

A Naphthalimide-Based Glyoxal Hydrazone for Selective Fluorescence Turn-On Sensing of Cys and Hcy

A fluorescent turn-on probe for Cys/Hcy based on inhibiting the CN isomerization quenching process by an intramolecular hydrogen bond was reported. The probe exhibited higher selectivity toward Cys/Hcy over other amino acids as well as thiol-containing compounds

Alternative Sm(II) Species-Mediated Cascade Coupling/Cyclization for the Synthesis of Oxobicyclo[3.1.0]hexane-1-ols

The allylSmBr/HMPA/MsOH system has been found to be an efficient reagent for the “ester-alkene” coupling/cyclization cascade of readily available α-allyloxy esters. Oxobicyclo[3.1.0]­hexane-1-ols were thus prepared in good to excellent yields and diastereoselectivities. Investigation on the mechanism suggested the possible existence of a new Sm­(II) species, namely, CH₃SO₃SmBr, which resulted from the reaction between allylSmBr and MsOH and may be the actual SET reagent

One-Pot Synthesis of Pyrrolo­[3,2,1-<i>kl</i>]pheno­thiazines through Copper-Catalyzed Tandem Coupling/Double Cyclization Reaction

A novel and efficient synthesis of pyrrolo­[3,2,1-<i>kl</i>]­pheno­thiazines has been developed through a Cu­(I)-catalyzed tandem C–S coupling/double cyclization process. Using 2-alkynyl-6-iodoanilines and <i>o</i>-bromo­benzenethiols as the starting materials, a wide range of pyrrolo­[3,2,1-<i>kl</i>]­pheno­thiazine derivatives were facilely and efficiently generated in one pot under Cu­(I) catalysis

Additive Tuned Selective Synthesis of Bicyclo[3.3.0]octan-1-ols and Bicyclo[3.1.0]hexan-1-ols Mediated by AllylSmBr

The selective construction of bicyclo[3.3.0]­octan-1-ols and bicyclo[3.1.0]­hexan-1-ols was achieved by using an allylSmBr/additive(s) system. By employing HMPA as the only additive, the momoallylation/ketone–alkene coupling occurred preferably and afforded bicyclo[3.3.0]­octan-1-ols in good yields with high diastereoselectivities. While the ester–alkene coupling predominated to generate bicyclo[3.1.0]­hexan-1-ols in moderate yields with excellent diastereoselectivities in the presence of a proton source, such as pyrrole as the coadditive with HMPA. The tunable reactivity of allylSmBr by additive(s) would make it a versatile reagent in organic synthesis

Additive Tuned Selective Synthesis of Bicyclo[3.3.0]octan-1-ols and Bicyclo[3.1.0]hexan-1-ols Mediated by AllylSmBr

The selective construction of bicyclo[3.3.0]­octan-1-ols and bicyclo[3.1.0]­hexan-1-ols was achieved by using an allylSmBr/additive(s) system. By employing HMPA as the only additive, the momoallylation/ketone–alkene coupling occurred preferably and afforded bicyclo[3.3.0]­octan-1-ols in good yields with high diastereoselectivities. While the ester–alkene coupling predominated to generate bicyclo[3.1.0]­hexan-1-ols in moderate yields with excellent diastereoselectivities in the presence of a proton source, such as pyrrole as the coadditive with HMPA. The tunable reactivity of allylSmBr by additive(s) would make it a versatile reagent in organic synthesis

DataSheet_1_Construction and validation of nomograms based on the log odds of positive lymph nodes to predict the prognosis of lung neuroendocrine tumors.docx

BackgroundThis research aimed to investigate the predictive performance of log odds of positive lymph nodes (LODDS) for the long-term prognosis of patients with node-positive lung neuroendocrine tumors (LNETs).MethodsWe collected 506 eligible patients with resected N1/N2 classification LNETs from the Surveillance, Epidemiology, and End Results (SEER) database between 2004 and 2015. The study cohort was split into derivation cohort (n=300) and external validation cohort (n=206) based on different geographic regions. Nomograms were constructed based on the derivation cohort and validated using the external validation cohort to predict the 1-, 3-, and 5-year cancer-specific survival (CSS) and overall survival (OS) of patients with LNETs. The accuracy and clinical practicability of nomograms were tested by Harrell’s concordance index (C-index), integrated discrimination improvement (IDI), net reclassification improvement (NRI), calibration plots, and decision curve analyses.ResultsThe Cox proportional-hazards model showed the high LODDS group (-0.79≤LODDS) had significantly higher mortality compared to those in the low LODDS group (LODDSConclusionsWe created visualized nomograms for CSS and OS of LNET patients, facilitating clinicians to bring individually tailored risk assessment and therapy.</p

DataSheet_1_Cotton Fusarium wilt diagnosis based on generative adversarial networks in small samples.pdf

This study aimed to explore the feasibility of applying Generative Adversarial Networks (GANs) for the diagnosis of Verticillium wilt disease in cotton and compared it with traditional data augmentation methods and transfer learning. By designing a model based on small-sample learning, we proposed an innovative cotton Verticillium wilt disease diagnosis system. The system uses Convolutional Neural Networks (CNNs) as feature extractors and applies trained GAN models for sample augmentation to improve classification accuracy. This study collected and processed a dataset of cotton Verticillium wilt disease images, including samples from normal and infected plants. Data augmentation techniques were used to expand the dataset and train the CNNs. Transfer learning using InceptionV3 was applied to train the CNNs on the dataset. The dataset was augmented using GAN algorithms and used to train CNNs. The performances of the data augmentation, transfer learning, and GANs were compared and analyzed. The results have demonstrated that augmenting the cotton Verticillium wilt disease image dataset using GAN algorithms enhanced the diagnostic accuracy and recall rate of the CNNs. Compared to traditional data augmentation methods, GANs exhibit better performance and generated more representative and diverse samples. Unlike transfer learning, GANs ensured an adequate sample size. By visualizing the images generated, GANs were found to generate realistic cotton images of Verticillium wilt disease, highlighting their potential applications in agricultural disease diagnosis. This study has demonstrated the potential of GANs in the diagnosis of cotton Verticillium wilt disease diagnosis, offering an effective approach for agricultural disease detection and providing insights into disease detection in other crops.</p