Facial synthesis of key intermediate of obeticholic acid via Pd-catalyzed Kumada-Tamao-Corriu cross-coupling reaction.

Obeticholic acid (OCA) is used to treatment for Primary Biliary Cholangitis and other Famesoid X Receptor related diseases. Through the palladium catalyzed Kumada-Tamao-Corriu cross-coupling reaction, a novel and efficient method for synthesis of OCA with satisfied yield was successfully developed. The absolute configuration of the key intermediate was confirmed by Single-crystal X-ray Diffraction.

Pd(NHC)(cinnamyl)Cl-catalyzed Suzuki cross-coupling reaction of aryl sulfonates with arylboronic acids.

A series of N-heterocyclic carbene (NHC)-palladium catalysts have been synthesized and applied to catalyze the Suzuki coupling reaction efficiently between aryl sulfonates and arylboronic acids with the potassium phosphate heptahydrate as a base. The desired yields are obtained even with less reactive aryl tosylates or aryl mesylates as substrates. This method was applied successfully to the synthesis of the (R)-2-(t-butoxycarbonylamino)-3-(biphenyl-4-yl)-propan-1-ol which is the key intermediate of sacubitril, a component of the newly approved antihypertensive drug "Entresto.

Hydrogen-Bonded Duplexes with Lengthened Linkers.

Connecting basic hydrogen-bonding units with lengthened flexible or rigid linkers generates oligoamide strands that carry new H-bonding sequences and association specificity, leading to H-bonded homo- and heteroduplexes with association constants in the 10 M range in chloroform. Computational and experimental studies indicate that in duplexes with rigid aromatic linkers the oligoamide strands adopt bent conformations that allow the formation of interstrand H-bonds and accommodate the introduced aromatic liners, offering a new series of association units.

A Biocompatible Colorimetric Triphenylamine- Dicyanovinyl Conjugated Fluorescent Probe for Selective and Sensitive Detection of Cyanide Ion in Aqueous Media and Living Cells.

A colorimetric and turn-on fluorescent probe bearing triphenylamine-thiophene and dicyanovinyl groups has been synthesized and used to detect cyanide anion via a nucleophilic addition reaction. Probe exhibited prominent selectivity and sensitivity towards CN in aqueous media, even in the presence of other anions such as S, HS, SO₃, S₂O₃, S₂O₈, I, Br, Cl, F, NO₂, N₃, SO₄, SCN, HCO₃, CO₃ and AcO. Moreover, a low detection limit (LOD, 51 nM) was observed.

[Fractions and Release Risk of Phosphorus in Surface Sediments of Three Headwater Streams with Different Styles of Water Supply].

From May to September 2015, seasonal sediment samples were collected from three headwater streams and ditches which were discharged from sewage plant tail water, food processing wastewater and agricultural drainage-groundwater seepage, respectively, in Hefei, Chaohu Lake basin. The stream-bed sediments were analyzed for phosphorus fractions. The risk assessment on phosphorus release from sediments was conducted using the phosphorus sorption index (PSI), degree of phosphorus saturation (DPS) and the phosphorus release risk index (ERI).

[Transient Storage Characteristics of Artificial Pool Geomorphic Structure in an Agricultural Headwater Stream].

From November 2015 to February 2016, five short-term tracer injections were performed with a conservative tracer (NaCl) in an agricultural headwater stream, Lake Chaohu basin. Thus the data sets of tracer experiments were finally employed for calculating the physical characteristics and transient storage metrics. Through the comparisons between the artificial pool reach and straight reach, characteristics of transient storage for the artificial pool geomorphic structure were interpreted and explored.

Chiral surfactant-type catalyst: enantioselective reduction of long-chain aliphatic ketoesters in water.

A series of amphiphilic ligands were designed and synthesized. The rhodium complexes with the ligands were applied to the asymmetric transfer hydrogenation of broad range of long-chained aliphatic ketoesters in neat water. Quantitative conversion and excellent enantioselectivity (up to 99% ee) was observed for α-, β-, γ-, δ- and ε-ketoesters as well as for α- and β-acyloxyketone using chiral surfactant-type catalyst 2.

Preparation and helical folding of aromatic polyamides.

Long aromatic polyamide chains are prepared from the corresponding monomers. The resultant polymer adopts a hollow helical conformation that is stabilized by intramolecular H-bonding interaction between side chains.