Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).

Twenty novel N-diarylalkenyl-piperidinecarboxylic acid derivatives were synthesized and evaluated as gamma-aminobutyric acid uptake inhibitors. The biological assay showed that (R)-1-[4,4-bis(3-phenoxymethyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic hydrochloride possessed almost as strong GAT1 inhibitory activity as tiagabine. The synthesis and structure-activity relationships are discussed.

[Changes of plasma von Willebrond factor and soluble E-selectin levels in patients with coronary artery disease].

Objective: To observe the changes of plasma von Willebrand factor (vWF) and soluble E-selectin (sE-selectin) in patients with coronary artery disease (CAD) and evaluate their clinic significance.

Methods: The level of plasma vWF and sE-selectin of 60 cases with coronary artery disease were detected by enzyme-linked immunosorbent assay (ELISA) and 20 healthy persons acted as the control group. Risk factors for coronary artery disease were obtained by asking the medical history and the relation ship was analyzed with coronary artery disease.

A highly efficient and direct approach for synthesis of enantiopure beta-amino alcohols by reductive cross-coupling of chiral N-tert-butanesulfinyl imines with aldehydes.

A highly efficient and practical approach for the synthesis of optically pure beta-amino alcohols by the SmI2-induced reductive cross-coupling of chiral N-tert-butanesulfinyl imines with aldehydes was developed. This method allows the preparation of a broad range of chiral beta-amino alcohols, including functionalized ones under mild conditions. It provides a straightforward access to enantiopure beta-amino alcohols that are widely applicable in asymmetric synthesis.

A new entry to asymmetric synthesis of optically active alpha,gamma-substituted gamma-butyrolactones, using a carbohydrate derived amide as both a chiral auxiliary and a proton source.

A new entry for the asymmetric synthesis of optically active alpha,gamma-substituted gamma-butyrolactones was developed by using a carbohydrate-derived amide as both a chiral auxiliary and a proton source. Unlike the previously reported examples, the chiral auxiliary employed in this reaction also successfully functioned as a protonating agent. Excellent asymmetric induction could be achieved by this dual stereoselective control in the reaction process.

Highly diastereoselective and enantioselective synthesis of enantiopure C2-Symmetrical vicinal diamines by reductive homocoupling of chiral N-tert-butanesulfinyl imines.

[reaction: see text] An efficient and straightforward method for the preparation of highly enantiomerically enriched C2-symmetrical vicinal diamines by the reductive homocoupling of aromatic N-tert-butanesulfinyl imines in the presence of SmI2 and HMPA was developed. It gives access to a variety of enantiopure C2-symmetrical 1,2-diamines in a very mild and practical way.

Toward the total synthesis of phorboxazole B: an efficient synthesis of the C20-C46 segment.

An efficient synthesis of the C20-C46 segment of phorboxazole B is described. The key steps involved Hg(OAc)(2)/I(2)-induced cyclization to construct the cis-tetrahydropyran moiety, the coupling of the metalated 2-methyloxazole 7 with lactone 6, and Julia olefination to furnish the conjugated diene moiety.

Samarium diiodide-induced asymmetric synthesis of optically pure unsymmetrical vicinal diamines by reductive cross-coupling of nitrones with N-tert-butanesulfinyl imines.

[reaction: see text] An efficient method for the preparation of optically pure unsymmetrical vicinal diamines by the SmI(2)-induced reductive cross-coupling of nitrones with chiral N-tert-butanesulfinyl imines was developed. This is the first successful example of the highly diastereoselective and enantioselective cross-coupling between two different imine species. It provides a straightforward access to enantiopure unsymmetrical vicinal diamines that are widely applicable in asymmetric synthesis.

A practical high through-put continuous process for the synthesis of chiral cyanohydrins.

A practical high through-put continuous process for the synthesis of chiral cyanohydrins is reported. Pretreated almond meal (or other solid raw enzyme sources) was loaded in a column to form a reactor, to which were attached a supplying system to deliver a solution of substrate and HCN in solvent on one end and a collecting-separating system on the other end. By controlling the flowing rate, optimal conditions were achieved for the hydrocyanation of various aromatic carboxaldehydes in a "micro-aqueous" medium to produce chiral cyanohydrins in high yields and high enantiomeric excess (ee) with high substrate/catalyst ratio.