A metal-free protocol for the synthesis of substituted 1,6-dihydropyridines with quaternary stereogenic centers via a cascade aza-Wittig/6?-electrocyclization process has been developed. The high functional group compatibility and broad scope this method were demonstrated by using wide range easily available vinyliminophosphoranes ketones, yields up to 97%. modification obtained products allowe...

NHC-catalyzed nucleophilic dearomatization of alkyl pyridiniums has been achieved to generate 1,4-dihydropyridines with high enantioselectivity. This is a rare example of catalytic, asymmetric addition of a nucleophile to the activated pyridinium that prefers C-4 functionalization leading to the 1,4-dihydropyridine with high selectivity.

A Ni/photoredox dual catalytic cross-coupling is disclosed in which a diverse range of (hetero)aryl bromides are used as electrophiles, with 1,4-dihydropyridines serving as precursors to Csp3-centered alkyl radical coupling partners. The reported method is characterized by its extremely mild reaction conditions, enabling access to underexplored cores.

A new calcium blocker, designated leualacin, has been isolated from Hapsidospora irregularis. The compound inhibits the binding of 3H-nitrendipine, a well known synthetic calcium blocker, to cardiac Ca channel in a competitive manner, although its structure is completely different from dihydropyridines.

A variety of novel ligands have been generated by Vilsmeier formylation of Hantzsch pyridines. These compounds which we call DOTTADs contain two aldehyde, imine or amine functions flanking a central pyridine nitrogen and can be homochiral or crown derivatives. The synthesis and manipulation of these systems is discussed. © 2000 Elsevier Science Ltd. All rights reserved. Some years ago we descri...

Chiral amines are an integral part of numerous important bioactive compounds. This privileged structural motif is found in naturally occurring alkaloids and amino acid derivatives as well as in pharmaceuticals, herbicides, and insecticides. Typically, enantiomerically pure amines are key building blocks in the drug-discovery process, but they are also sold on a multi-hundred-ton-scale as kineti...

Antihypertensive treatment with dihydropyridines may be accompanied by sympathetic activation. Data on whether this is common to all compounds and similar in the various phases of treatment are not univocal, however. In 28 untreated essential hypertensives (age, 56.4+/-1.8 years; mean+/-SEM) finger blood pressure (BP, Finapres), heart rate (HR, ECG), plasma norepinephrine (NE, high-performance ...