Claim Your Author Page
A series of 4,4-disubstituted cyclohexylamine NK(1) antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.
The total synthesis of the novel antitumor agent callipeltoside A, as well as several analogues, is accomplished and allows assignment of the stereochemistry not previously established. A convergent… (More)
Abstract The asymmetric [2+3] cycloaddition reaction between chiral oxazoline N -oxide 1 and α,β-unsaturated lactone 2 was studied. A double diastereoselection was observed, (1 R )- 1 and ( R )- 2… (More)
We report the discovery and optimization of an amine-promoted Friedel–Crafts alkylation of cinnamaldehyde with 4-hydroxymethyl phenol. This reaction has been used successfully on commercial scale… (More)
Abstract The regioselective, scaleable synthesis of three 4-(2-alkyl-5-methyl-2 H -pyrazol-3-yl)-piperidines is discussed.
Oxetanone 1233A 1 has been synthesized in 22 steps and 3.43% overall yield from 3-methylglutaric anhydride. Asymmetric carbon at C7 was introduced by a diastereoselective esterification of… (More)
[reaction: see text] A [2+3] cycloaddition of camphor-derived oxazoline N-oxide to alpha,beta-unsaturated ester afforded adduct 8. Tetrahydrolipstatin 1 was prepared from this compound in a nine-step… (More)