Abstract

Recent results from the author's laboratory in the area of dihydropyrimidine chemistry are summarized.

Highlights

  • In recent years interest has focused on aza-analogs such as dihydropyrimidines of type 4 (DHPMs) which show a very

  • In this report we summarize our results in the area of dihydropyrimidine chemistry and present a literature survey on recent developments in this field

  • In the context of our computational studies on DHPM conformers we have developed synthetic methodology leading toward novel types of conformationally restricted dihydropyrimidine derivatives of type 11 that closely mimic the recently proposed receptor-bound conformation of DHP/DHPM calcium channel modulators shown in Figure 2 [26]

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Summary

Introduction

4-Aryl-1,4-dihydropyridines of the nifedipine type (DHPs, e.g 1-3) are the most studied class of organic calcium channel modulators and, since their introduction into clinical medicine in 1975, have become almost indispensable for the treatment of cardiovascular diseases such as hypertension, cardiac arrhythmias, or angina [1]. More than 20 years after the introduction of nifedipine (1), many DHP analogs have been synthesized and numerous second-generation commercial products have appeared on the market (e.g. 2, 3) [2]. In recent years interest has focused on aza-analogs such as dihydropyrimidines of type 4 (DHPMs) which show a very

Biographical Sketch
Me N O H
Ph H
The Mechanism of the Biginelli Reaction
Conformational Studies
Me N O
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Enantiomerically Pure Dihydropyrimidines
Synthetic Studies
Ph O N Me
NC N Me
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