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First synthesis of the diastereomeric mixture of Salbutamol dimer (2) is described. The synthesis provides access to multi-gram quantities of 2 for reference supplies and further analytical and toxicology investigations. It also confirmed the proposed structure by comparison to authentic sample. [Copyright &y& Elsevier]

Reaction of N-alkylated glycine esters with excess acrolein in the presence of acid, followed by treatment with triethylamine, provided N-substituted 4-formyl-5-vinyl proline carboxylates in good yields with high regio- and stereoselectivity. [Copyright &y& Elsevier]

• New class of P -stereogenic chiral N H Brønsted acid organocatalysts prepared. • Catalysts were prepared from chiral phosphinamides or secondary phosphine oxides. • Catalysts promoted the asymmetric reduction of quinolones by transfer hydrogenation. • Asymmetric transformation effected by the P -stereogenic chiral environment. • Easily tunable selectivity and reactivity by the substituents of phosphorous. A new class of N H Brønsted acid organocatalysts that feature P -stereogenic chirality was developed. These catalysts were prepared from P -stereogenic chiral phosphinamides and show similar reactivity to BINOL derived phosphoric acid toward the reduction of quinolines via transfer hydrogenation. It shows that stereoselectivity is induced by the P -chiral environment that is created by the substituents attached to the phosphorous atom, which can be readily tuned and modified. [ABSTRACT FROM AUTHOR]

Abstract: Expedient and practical new methodology for the synthesis of substituted imidazoles was developed to provide a rapid access to a variety of 2-substituted, 1,2-disubstituted and 1,2,4-trisubstituted imidazoles by the direct CuCl-mediated reaction of nitriles with α-amino acetals in an intermolecular as well as intramolecular fashion. [Copyright &y& Elsevier]

Abstract: A streamlined and practical approach to 1H-imidazo[1,2-α]imidazol-2-one LFA-1 antagonist (1) that features as the key step a novel intramolecular boronic acid catalyzed cyclocondensation of a urea and an amide is reported. [Copyright &y& Elsevier]