Aerobic oxidative cyclization under Pd(II) catalysis: a regioselective approach to heterocycles.

[chemical reaction: see text]. An efficient Yb(OTf)3-promoted palladium-catalyzed oxidative cyclization of gamma-heteroalkenyl beta-keto amides has been developed. Under simple aerobic condition, a variety of six-, seven-, and eight-membered-ring N- and O-heterocycles were obtained regioselectively in excellent yield.

The influence of NAT2 genotypes on the plasma concentration of isoniazid and acetylisoniazid in Chinese pulmonary tuberculosis patients.

Background: Isoniazid (INH) is widely used in the therapy of tuberculosis. Poor metabolizer (PM) of the NAT2 is an important reason of inter-individual difference of the plasma INH concentration. We studied the relationship between NAT2 genotype and INH and its metabolite acetylisoniazid (AcINH) concentration in Chinese people.

Recyclable and reusable Pd(OAc)2/DABCO/PEG-400 system for Suzuki-Miyaura cross-coupling reaction.

[reaction: see text] A stable and efficient Pd(OAc)2/DABCO (triethylenediamine) catalytic system for Suzuki-Miyaura cross-coupling reaction has been developed. In the presence of Pd(OAc)2 and DABCO, coupling of aryl halides with arylboronic acids was carried out smoothly to afford good to excellent yields and high turnover numbers (TONs) (the maximal TONs were up to 960,000 for the reaction of 1-iodo-4-nitrobenzene with phenylboronic acid) using PEG-400 as the solvent. Moreover, the Pd(OAc)2/DABCO/PEG-400 system could be recycled and reused five times without any loss of catalytic activity for aryl iodides and bromides.

Efficient and reusable PdCl2(MeCN)2/CuCl2/PEG-400 system for cyclization of alkenyl beta-keto esters and amides.

PEG-400 [poly(ethylene glycol-400)] was found as an effective medium for the PdCl(2)(MeCN)(2)-catalyzed hydroalkylation cyclization of alkenyl beta-keto esters and amides. In PEG-400, no additives such as Me(3)SiCl and Ln(OTf)(3) were required for the complete conversion of alkenyl beta-keto esters. The results also showed that CuCl(2) could promote the reaction.

Efficient palladium-catalyzed homocoupling reaction and Sonogashira cross-coupling reaction of terminal alkynes under aerobic conditions.

An efficient method for palladium-catalyzed homocoupling reaction of terminal alkynes in the synthesis of symmetric diynes is presented. The results showed that both Pd(OAc)(2) and CuI played crucial roles in the reaction. In the presence of 2 mol % Pd(OAc)(2), 2 mol % CuI, 3 equiv of Dabco, and air, homocoupling of various terminal alkynes afforded the corresponding symmetrical diynes in moderate to excellent yields, whereas low yields were obtained without either Pd(OAc)(2) or CuI.

Ni(II)-catalyzed Conia-ene reaction of 1,3-dicarbonyl compounds with alkynes.

[reaction: see text]. We have discovered a Ni(II)-catalyzed Conia-ene reaction of 1,3-dicarbonyl compounds with alkynes. In the presence of Ni(acac)2 and Yb(OTf)3, various acetylenic 1,3-dicarbonyl compounds underwent Conia-ene reaction to give mono- and bicyclic olefinic cyclopentanes.

Efficient Stille cross-coupling reaction catalyzed by the Pd(OAc)2/Dabco catalytic system.

[reaction: see text] An efficient Pd(OAc)2/Dabco-catalyzed Stille cross-coupling reaction procedure has been developed. In the presence of Pd(OAc)2 and Dabco (triethylenediamine), various aryl halides including aryl iodides, aryl bromides, and activated aryl chlorides were coupled efficiently with organotin compounds to afford the corresponding biaryls, alkene, and alkynes in good to excellent yields. Furthermore, high TONs [turnover numbers, up to 980,000 TONs for the coupling reaction of 1-bromo-4-nitrobenzene and furan-2-yltributyltin] for the Stille cross-coupling reaction were observed.

High-performance liquid chromatography-electrospray ionization mass spectrometric determination of nisoldipine in human plasma.

A selective and sensitive high-performance liquid chromatography-electrospray ionization mass spectrometry (MS) for the determination of nisoldipine in human plasma is first presented. With nimodipine as the internal standard, nisoldipine is extracted from plasma with ethyl acetate. The organic layer is evaporated and the residue is resuspended in the mobile phase of methanol-water (80:20, v/v).

General and selective synthesis of (Z)-3-haloacrylates via palladium-catalyzed carbonylation of terminal alkynes.

A general and selective palladium-catalyzed carbonylation of terminal alkynes method for the synthesis of (Z)-3-haloacrylates is presented. In the presence of a catalytic amount of PdX2 and 5 equiv of CuX2 (X=Cl and Br), terminal alkynes were carbonylated to afford the corresponding (Z)-3-haloacrylates exclusively in moderate to good yields. The results showed that the effect of solvent had a fundamental influence on the chemoselectivity and stereoselectivity of the palladium-catalyzed carbonylation reaction.

Mild and selective palladium-catalyzed dimerization of terminal alkynes to form symmetrical (Z,Z)-1,4-dihalo-1,3-dienes.

A regioselective and stereoselective palladium-catalyzed dimerization of terminal alkynes method for the synthesis of symmetrical (Z,Z)-1,4-dihalo-1,3-dienes is presented. In the presence of a catalytic amount of PdX(2) and 3 equiv of CuX(2) (X = Cl and Br), terminal alkynes were dimerized to afford (Z,Z)-1,4-dihalo-1,3-dienes in good yields. The results showed that the effect of solvent had a fundamental influence on the chemoselectivity of the dimerization reaction.

Dabco as an inexpensive and highly efficient ligand for palladium-catalyzed Suzuki-Miyaura cross-coupling reaction.

An inexpensive and highly efficient Pd(OAc)(2)/Dabco catalytic system has been developed for the cross-coupling of aryl halides with arylboronic acids. A combination of Pd(OAc)(2) and Dabco (triethylenediamine) was observed to form an excellent catalyst, which affords high TONs (turnover numbers; TONs up to 950 000 for the reaction of PhI and p-chlorophenylboronic acid) for Suzuki-Miyaura cross-coupling of various aryl iodides and bromides with arylboronic acids. [reaction: see text]

New role of CO2 as a selective agent in palladium-catalyzed reductive Ullmann coupling with zinc in water.

Carbon dioxide was found to promote the palladium-catalyzed zinc-mediated reductive Ullmann coupling of aryl halides. In the presence of carbon dioxide, Pd/C, and zinc, various aromatic halides including less reactive aromatic chlorides were coupled to give the corresponding homocoupling products in good yields.

[Experimental study on spermatogenic and strengthening yang action of baxian capsule].

Objective: To discuss spermatogenic and strengthening yang action of Baxian(BX) capsule and its possible mechanism.

Methods: Rats or mice were divided randomly into five groups: control group, Baxian groups(2.5 g/kg, 7.

Lanthanide triflate-promoted palladium-catalyzed cyclization of alkenyl beta-keto esters and amides.

[reaction: see text] Lanthanide triflates were found to promote the palladium-catalyzed cyclization of alkenyl beta-keto esters and amides. In the presence of catalytic amounts of PdCl(2)(MeCN)(2) and Ln(OTf)(3), various alkenyl beta-keto esters and amides underwent regioselective cyclization reactions to give six-, seven-, or eight-membered-ring carbocycles in moderate to excellent yields.