Synthesis of 4-Alkylated 1,4-Dihydropyridines: Fe(II)-Mediated Oxidative Cascade Cyclization Reaction of Cyclic Ethers with Enaminones.

Syntheses of highly functionalized 4-alkylated 1,4-dihydropyridines (1,4-DHPs) from cyclic ethers and enaminones via iron(II)-mediated oxidative free radical cascade C(sp)-H bond functionalization/C(sp)-O bond cleavage/cyclization reaction have been first developed. This novel synthetic strategy offers an alternative method for the construction of 1,4-DHPs by using esters as the C4 sources, as well as expands the application of ethers in heterocycle synthesis.

Fe-mediated oxidative cascade [1 + 2 + 3]-cyclization/esterification reaction: synthesis of 4-alkylated 1,4-dihydropyridines.

An Fe-mediated four-component reaction of enaminones, anhydrides and tetrahydrofuran through a cascade [1 + 2 + 3]-cyclization/esterification process is presented. This protocol provides a new and effective method to construct 4-alkylated 1,4-dihydropyridines with an ester fragment. Cyclic ether is employed as the C4 source of 1,4-dihydropyridines for the first time.

Systematical characterization of gypenosides in Gynostemma pentaphyllum and the chemical composition variation of different origins.

Gynostemma pentaphyllum (Thunb.) Makino is an herbaceous plant of Cucurbitaceae family, which has been widely used as an herbal tea and traditional Chinese medicine. Since its saponins are similar to ginsenosides and have a wide range of activities, it has attracted wide interest.

[Identification of chemical constituents of Xiaochengqi Decoction by UPLC-Q-TOF/Fast DDA combined with UNIFI software].

Based on the combination of ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF) and Waters UNIFI software, the chemical constituents of the classic prescription Xiaochengqi Decoction were qualitatively analyzed and identified. The UPLC conditions are as follows: Acquity HSS T3 reverse phase column(2.1 mm ×100 mm, 1.

[Analysis of chemical constituents in classical prescription Danggui Buxue Decoction based on RP-Q-TOF-MS and HILIC-Q-TOF-MS].

The chemical constituents of classical prescription Danggui Buxue Decoction were analyzed by reversed-phase(RP) chromatography and hydrophilic interaction chromatography(HILIC) coupled with quadrupole time-of-flight mass spectrometry. RP separation of Danggui Buxue Decoction was performed on ACQUITY UPLC HSS T3(2.1 mm×100 mm, 1.

Might life-threatening acute pulmonary edema occur after using recombinant tissue plasminogen activator? A case report.

Background: Recombinant tissue plasminogen activator (rt-pa) is the first-line drug for the treatment of acute ischemic stroke, and can lead to some complications.There were rare reports of death due to acute pulmonary edema during rt-pa thrombolysis treatment.

Case Presentation: This study reports a 30-year-old man was diagnosed with acute ischemic stroke and underwent rt-pa thrombolytic therapy.

Highly Regioselective and Chemoselective [3 + 3] Annulation of Enaminones with Fluoronitrobenzenenes: Divergent Synthesis of Aposafranones and Their -Oxides.

A base-promoted unprecedented strategy for the regioselective and chemoselective divergent synthesis of highly functionalized aposafranones and their -oxides has been developed from the [3 + 3] annulation of enaminones with -fluoronitrobenzenenes. This novel synthetic strategy offers an alternative method for the construction of aposafranones and their -oxides are meaningful in the fields of both biology and organic synthesis. The established protocol explores the annulation scope of enaminones, and it expands the application of nitro-based cyclization.

Synthesis and biological evaluation of novel 3-benzylcoumarin-imidazolium salts.

A series of novel 3-benzylcoumarin-imidazolium salts were prepared and evaluated in vitro against a panel of human tumor cell lines. The results showed that the existence of 5,6-dimethyl-benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl group were vital for modulating cytotoxic activity. Notably, compound 38 was found to be the most potent derivative with IC values of 2.

Three-Component One-Pot Synthesis of Highly Functionalized Bis-Indole Derivatives.

In this study, we detail the development of a concise and efficient three-component protocol for the regioselective synthesis of highly functionalized bis-indoles through a one-pot, two-step sequential process starting from enaminones , indoles , and acenaphthylene-1,2-dione that is catalyzed by piperidine and -methyl benzenesulfonic acid. This protocol has several advantages including simplicity of experimental operation, high efficiency of bond formation, ready availability and low cost of starting materials, environmentally benign conditions, and target molecular diversity.

Divergent synthesis of dual 1,4-dihydropyridines with different substituted patterns from enaminones and aldehydes through domino reactions.

A concise and efficient protocol for the regioselective synthesis of dual 1,4-dihydropyridines with several substituted patterns has been developed from a cascade cyclization of enaminones and aldehydes in different media (EtOH/CHCN). The one-pot cascade reaction involves at least five reactive sites and generates multiple C-C and C-N bonds. The established protocol explores the chemistry of enaminones by employing their three reactive sites.

Green synthesis of new pyrrolidine-fused spirooxindoles three-component domino reaction in EtOH/HO.

An efficient, green and sustainable approach for the synthesis of novel polycyclic pyrrolidine-fused spirooxindole compounds was developed. The synthesis included a one-pot, three-component, domino reaction of ()-3-(2-nitrovinyl)-indoles, isatins and chiral polycyclic α-amino acids under catalyst-free conditions at room temperature in EtOH-HO. The salient features of this methodology are eco-friendliness, high yields and the ease of obtaining target compounds without the involvement of toxic solvents and column chromatography.

Efficient construction of C-N and C-S bonds in 2-iminothiazoles via cascade reaction of enaminones with potassium thiocyanate.

A novel and highly efficient protocol has been developed for the regioselective synthesis of 2-iminothiazole derivatives with potential biochemical interest by the reaction of enaminones, potassium thiocyanate (KSCN), and N-bromo succinimide (NBS) under mild conditions. The reaction proceeds via the formation of α-bromo enaminones as a versatile intermediate followed by thiocyanation/intramolecular cyclization in a one pot manner. The developed method is particularly attractive due to various advantages including operational simplicity, mild conditions, being catalyst free, and high bond-forming efficiency.

Relationship between hepatocellular carcinoma and hepatitis B virus genotype with spontaneous YMDD mutations.

Aim: To investigate the relationship between hepatitis B virus (HBV) genotype with spontaneous YMDD mutations and hepatocellular carcinoma (HCC) in HBV-related cirrhosis.

Methods: We investigated 264 liver cirrhosis patients who were not treated with antiviral drugs, including 81 patients with HCC. YMDD mutations were detected by fluorescent hybridization bioprobe polymerase chain reaction (PCR) and melting curve assay using the Diagnosis Kit for HBV YMDD Mutation.

Primary hepatic diffuse large B cell lymphoma: A case report: Primary hepatic diffuse large B cell lymphoma.

In this report we describe a rare case of primary hepatic diffuse large B cell lymphoma in a 67-year-old man who presented with abdominal pain, deteriorated liver function, elevated lactate dehydrogenase. He was found to have diffuse nodular intrahepatic space-occupying lesion with normal α-fetoprotein and carcino-embryogenic antigen. The final diagnosis was made by percutaneous biopsy of the liver as the clinical manifestation not consistent with common liver diseases.

[Accuracy of FibroScan for the diagnosis of liver fibrosis influenced by serum alanine aminotransferase levels in patients with chronic hepatitis B].

Objective: To analyze whether or not the accuracy of liver stiffness measurement (LSM) with transient elastography (FibroScan) for the diagnosis of liver fibrosis influenced by serum alanine aminotransferase (ALT) levels in patients with chronic hepatitis B.

Methods: 213 consecutive CHB patients who underwent liver biopsy and LSM were enrolled and divided into three groups by the criteria of ALT < 1 x ULN, 1 x ULN ≤ ALT < 2 x ULN and ALT ≥ 2 x ULN. The areas under the receiver operating curve(AUC) were analyzed and the accuracy of FibroScan for the diagnosis of liver fibrosis were detected in the three groups.

Prospective evaluation of FibroScan for the diagnosis of hepatic fibrosis compared with liver biopsy/AST platelet ratio index and FIB-4 in patients with chronic HBV infection.

Background: The FibroScan (FS), the aspartate aminotransferase-to-platelet ratio index (APRI), and the FIB-4 index are simple and inexpensive methods to detect liver fibrosis.

Aims: The primary objective was to evaluate the performance of FS for the noninvasive diagnosis of hepatic fibrosis in Western Chinese patients with chronic hepatitis B virus (HBV) infection compared with APRI and FIB-4; the secondary objective was to determine liver stiffness measurement (LSM) cutoff values for the noninvasive diagnosis of significant fibrosis and liver cirrhosis.

Methods: Overall, 175 consecutive patients with chronic HBV infection, successful liver biopsy, and alanine aminotransferase levels ≤2× ULN were prospectively studied.