A5100389004- Catalytic C–H Functionalization Methods
- Catalytic Cross-Coupling Reactions
- Asymmetric Hydrogenation and Catalysis
- Pituitary Gland Disorders and Treatments
- Asymmetric Synthesis and Catalysis
- Hormonal Regulation and Hypertension
- Catalytic Alkyne Reactions
- Synthetic Organic Chemistry Methods
- Cancer, Hypoxia, and Metabolism
- Adrenal Hormones and Disorders
- Diabetes Treatment and Management
- Histone Deacetylase Inhibitors Research
- Diabetic Foot Ulcer Assessment and Management
- Sulfur-Based Synthesis Techniques
- Glioma Diagnosis and Treatment
- Thyroid Cancer Diagnosis and Treatment
- Coordination Chemistry and Organometallics
- Oxidative Organic Chemistry Reactions
- Neuroscience of respiration and sleep
- Thyroid and Parathyroid Surgery
- Synthesis and bioactivity of alkaloids
- Genetic and Kidney Cyst Diseases
- Surface Chemistry and Catalysis
- Carbon dioxide utilization in catalysis
- Axial and Atropisomeric Chirality Synthesis
First Affiliated Hospital of Xi'an Jiaotong University
2021-2025
Zhujiang Hospital
2022
Southern Medical University
2022
University of Louisville
2020
First Hospital of Jilin University
2020
Jilin University
2020
Affiliated Hospital of Qingdao University
2018-2019
Qingdao University
2018-2019
Tongji Hospital
2018
Huazhong University of Science and Technology
2018
Ar−Rh(III) pivalate complexes assembled in situ from the reaction of [RhCl(coe)2]2 (coe = cis-cyclooctene), [p-(CF3)C6H4]3P, and CsOPiv effectively catalyzed direct C-arylation free (NH)-indoles (NH)-pyrroles good yields with high regioselectivity. The displayed excellent functional group compatibility low moisture sensitivity. Kinetics studies support a mechanism involving phosphine displacement by indole complex 2 (resting state catalyst), followed rate-limiting C−H bond metalation.
This paper describes a phosphine-free palladium-catalyzed method for direct C-arylation of free (N−H)-indoles and pyrroles with iodo- bromoarene donors. Employing commercially available materials, this new operationally simple procedure provides rapid entry to wide range C-arylated including derivatives tryptamine. In the course study, profound halide effect was uncovered, affecting both efficiency regioselectivity indole arylation.
Reaction of 1-methy-2-(4-pentenyl)indole (1) with a catalytic amount PtCl2 (2 mol %) in dioxane that contained trace HCl (5 at 60 °C for 24 h led to the isolation 4,9-dimethyl-2,3,4,9-tetrahydro-1H-carbazole (2) 92% yield. Platinum-catalyzed cyclization 2-(4-pentenyl)indoles tolerated substitution each position 4-pentenyl chain. Furthermore, protocol was applicable synthesis tetrahydro-β-carbolinones and effective unprotected indoles. 2-(3-Butenyl)indoles underwent platinum-catalyzed...
The new air-stable PdCl2{PR2(Ph-R')}2 complexes, readily prepared from commercial reagents, exhibit unique efficiency as catalysts for the Suzuki−Miyaura coupling reactions of a variety heteroatom-substituted heteroaryl chlorides with diverse range aryl/heteroaryl boronic acids. catalyzed by complexes high product yields (88−99%) and catalyst turnover numbers (up to 10 000 TON).
A new synthetic strategy that turns styrene-type olefins into excellent substrates for Rh-catalyzed asymmetric hydrogenation by installing a 2'-hydroxyl substituent is described. This methodology accommodates trisubstituted olefinic in various E/Z mixtures, leading to valuable benzylic chiral compounds including (R)-tolterodine. It also demonstrated the groups could be readily removed high yield without loss of ee from products. Thus, this technology represents an attractive alternative...
Reaction of 5,5-dimethyl-8-nonene-2,4-dione catalyzed by PdCl2(CH3CN)2 (5 mol %) in the presence CuCl2 (2.5 equiv) at room temperature for 3 h formed 2-acetyl-3,6,6-trimethyl-2-cyclohexenone 96% isolated yield. Palladium-catalyzed intramolecular oxidative alkylation tolerated a range substitution and was applicable to synthesis spirobicyclic compounds cyclization zeta-alkenyl beta-keto esters.
Reaction of benzamide with a catalytic 1:2 mixture [PtCl2(H2CCH2)]2 (2.5 mol %) and PPh3 in dioxane at 120 °C for 24 h led to isolation N-ethylbenzamide 97% yield. A range primary, acyclic aryl alkyl carboxamides secondary cyclic carbamates also underwent platinum-catalyzed addition ethylene propylene.
Remission failure following transsphenoidal surgery in Cushing disease (CD) from pituitary corticotroph tumors (CtTs) remains clinically challenging. Histone deacetylase inhibitors (HDACis) are antitumor drugs approved for clinical use, with the potential to affect adrenocorticotropin hormone (ACTH) hypersecretion by inhibiting pro-opiomelanocortin (POMC) transcription.Testing efficacy of suberoylanilide hydroxamic acid (SAHA) on human and murine ACTH-secreting tumor (AtT-20) cells.Cell...
Importance Older patients may benefit from the hemodynamic stability of etomidate for general anesthesia. However, it remains uncertain whether potential adrenocortical suppression with increase morbidity. Objective To test primary hypothesis that vs propofol anesthesia does not in-hospital morbidity after abdominal surgery in older patients. Design, Setting, and Participants This multicenter, parallel-group, noninferiority randomized clinical trial (Etomidate Propofol In-hospital...
This study was aimed at investigating if the lymph node aspirated wash-out liquid thyroglobulin level and thyroid imaging reporting data system (TI-RADS) nodule score can be predictive factor for cervical metastasis in patients with papillary carcinoma (PTC). The included 251 surgically confirmed PTC. All underwent preoperative ultrasound examination using ACR TI-RADS classification, fine-needle aspiration biopsy (FNAB) BRAF V600E gene detection, (Tg) detection fluid. results of these...
A 1:1 mixture of the platinum dimethyl diimine complex [PhNC(Me)C(Me)NPh]PtMe2 (4a) and B(C6F5)3 catalyzed cyclization/hydrosilylation dipropargylmalonate (1) HSiEt3 to form 1,1-dicarbomethoxy-3-methylene-4-(triethylsilylmethylene)cyclopentane (3) in 82% isolated yield with 26:1 Z:E selectivity. Platinum-catalyzed diyne tolerated a range functional groups including esters, sulfones, acetals, silyl ethers, amides, hindered ketones. Diynes that possessed propargylic substitution underwent...
[reaction: see text] Treatment of 3-butenyl heptyl ketone with substoichiometric amounts PdCl(2)(CH(3)CN)(2) (10 mol %), HCl (0.1 equiv), and CuCl(2) (0.3 equiv) in dioxane at 70 degrees C for 12 h a sealed tube formed 2-hexylcyclohexanone 77% isolated yield. A number alkyl ketones underwent hydroalkylation under these conditions to form 2-substituted cyclohexanones moderate good
PdCl2(CH3CN)2 and [PtCl2(H2CCH2)]2 catalyze the addition of β-dicarbonyl compounds to ethylene propylene.
Ethylene, alpha-olefins, and vinyl arenes undergo platinum-catalyzed hydroarylation with substituted indoles in moderate to good yield.
Reaction of 3-butenyl beta-keto esters or alpha-aryl ketones with a catalytic amount [PdCl2(CH3CN)2] (2) and stoichiometric Me3SiCl Me3SiCl/CuCl2 in dioxane at 25-70 degrees C formed 2-substituted cyclohexanones good yield high regioselectivity. This protocol tolerated number ester aryl groups substitution the allylic, enolic, cis trans terminal olefinic positions. In situ NMR experiments indicated that chlorosilane was not directly involved palladium-catalyzed hydroalkylation, but rather...
Thyroglobulin measurement in fine-needle aspiration (FNA-Tg) is an additional diagnostic tool of lymph node metastasis (LNM) papillary thyroid carcinoma (PTC). However, its performance as a preoperative indicator lateral neck LNM PTC unclear. We evaluated the use FNA cytology and FNA-Tg to detect presurgery using simple methodology, established cut-off value for diagnosing PTC.We performed retrospective cohort study based on hospital records, including 299 measurements from 228 patients with...
Reaction of 8-nonene-2,4-dione with a catalytic amount [PdCl2(CH3CN)2] (2; 5 mol %) and stoichiometric CuCl2 (2.5 equiv) at room temperature for 3 h led to oxidative alkylation formation 2-acetyl-3-methyl-2-cyclohexenone in 80 % isolated yield. The 4-pentenyl beta-diketones tolerated number terminal acyl groups substitution the C1 C3 carbon atoms chain. Likewise, beta-keto esters that possessed geminal disubstitution C1, C2, or atom chain cyclized form 2-carboalkoxy-2-cyclohexenones moderate...
A one-pot procedure for the synthesis of 2-alkyl-2-arylcyanoacetates based on a Pd(OAc)2/DPPF (DPPF = 1,1‘-diphenylphosphino ferreocene)-catalyzed enolate arylation followed by in situ alkylation has been developed. This tolerates diverse range aryl and heteroaryl bromides, provides rapid entry to variety good excellent yield.
Two asymmetric syntheses of AMG 221 (2), an inhibitor 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) discovered in our laboratories, are reported. One the utilizes chiral trimethylsilyl cyanohydrin 12 as starting material and other its enantiomer ent-12. The displacement approach involves conversion to 2 via a six-step sequence, occurs with net inversion configuration, employs amine 6 material. This route features novel toward dialkylsubstituted alpha-mercaptoacids. cyclization...
Pre-operative detection of corticotropin (ACTH) secreting microadenomas causing Cushing's disease (CD) improves surgical outcomes. Current best magnetic resonance imaging fails to detect up 40% these microadenomas.
An expeditious synthetic approach to chiral phenol 1, a key building block in the preparation of series drug candidates, is reported. The strategy includes cost-effective and readily scalable route cyclopentanone 3 from isobutyronitrile (10). sterically hindered enolizable ketone was subsequently employed challenging Grignard addition mediated by LaCl(3)·2LiCl. A novel lanthanide reagent required for this transformation described. To complete process, highly enantioselective hydrogenation...