d(3)-Cerivastatin was synthesized as an internal standard for use in a LC/MS/MS method developed for the simultaneous quantitative determination of the drug in human serurn. d(3)-Cerivastatin was efficiently prepared on large scale from d(3)-iodomethane using improved procedures. Copyright (c) 2006 John Wiley & Sons, Ltd.

A new facile method for the preparation of trans-2-aryl-3,3-dimethylcyclopropane-1-carboxylic acids was developed. The new method involved [2+2]-cycloaddition of styrenes with N,N,2-trimethylpropionamide followed by bromination and rearrangement of the resulting 3-aryl-2,2-dimethylcyclobutanones, affording the title compounds in two steps in 60–84% overall yields.

An improved synthesis of 1-(imidazolyl)methyl-4-sulfonylbenzodiazapines, new farnesyltransferase inhibitors, was achieved using a novel reductive N-alkylation method. The new method involves reaction of a secondary amine with an aldehyde using triethylsilane in the presence of trifluoroacetic acid, giving a tertiary amine in 90–95% isolated yields.

A novel, efficient, and regiospecific method for the construction of the imidazo[1,5-a]quinoxalin-4(5H)-one template is described. The key reaction involves an intramolecular cyclization process and provides the desired products in excellent yield.

D-5-labeled isotopomers of atorvastatin, atorvastatin lactone and its hydroxy metabolites were synthesized as internal standards for use in a LC/MS/MS method developed for the simultaneous quantitative determination of atorvastatin and its hydroxy metabolites in human serum, d(5)-Atorvastatin and d(5)-atorvastatin lactone were prepared from d(5)-aniline whereas their corresponding hydroxy metabolites were synthesized using d(5)-benzaldehyde.

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