Clemens Lamberth

CONCISE APPROACH TO 1-THIAHYDANTOCIDIN

Abstract The synthesis of 1-thiaHydantocidin, a close analog of the total herbicide Hydantocidin, is described starting from 2,3,5-tri-O-benzoyl-β-D-ribofuranosyl cyanide.

Synthesis and acaricidal activity of 4-pyrimidinyloxy- and 4-pyrimidinylaminoethylphenyl dioxolanes and oxime ethers

Novel types of mitochondrial respiration inhibitors at complex I, with emphasis on acaricidal activity, have been designed and prepared. The synthetic approach to these 4-pyrimidinylphenyl ethyl ethers and amines with a specific ketal or oxime function in the phenyl side chain is outlined. Bioassays demonstrate their high potential against important spider mites, like Tetranychus urticae and Panonychus ulmi. Structure-activity relationship studies and several biological parameters are discussed.

Regio- and Stereoselective Alkoxycarbonylmethylenation of Partially Saturated Heterobicyclic Compounds: First Synthesis of 2-Substituted Quinazoline-8-acetic Acid Esters

Abstract The three-step synthesis of 2-substituted quinazol-8-yl acetates is described, introducing a completely new method for the regio- and stereoselective alkoxycarbonylmethylenation of tetrahydroquinazolines. # Novartis Crop Protection Ltd., Research Department, 975 California Avenue, Palo Alto, CA 94303, USA.

Dimethyl Acetylsuccinate as a Versatile Synthon in Heterocyclic Chemistry — A Facile Synthesis of Heterocyclic Acetic Acid Derivatives

The preparation of novel acetic acid derivatives of pyrazole 3a,b and pyrimidine 2a—e is achieved by condensation of dimethyl acetylsuccinate (1) with appropriate reaction partners. Also triethyl 1,1,2-ethanetricarboxylate (6) is a valuable starting material, which is demonstrated by the synthesis of previously unknown pyrimidin-5-yl acetates.

Synthesis of 4‐substituted imidazo[1,2‐a]quinoxalines

A concise approach to 4-substituted imidazo[1,2-a]quinoxalines 7 is described, starting from 1-fluoro-2-nitrobenzene (3). The high variability in the functionalization of the imidazo [1,2-a]quinoxaline-4-position is due to the easy introduction of these substituents by N-acylation in the second last step.