37708-25-1Relevant articles and documents
Lipase resolution of new (±)-3-aryloxy-1-halogenopropan-2-ols: Versatile building blocks for β-adrenergic receptor antagonists
Maciejewski, Maciej,Poltorak, Krzysztof,Kaminska, Janina E.
experimental part, p. 248 - 256 (2010/11/02)
Using two commercial immobilized lipases Lipozyme TL and Novozym 435 effective kinetic resolution of several novel 3-aryloxy-1-halogenopropan-2-ols was achieved by acyl transfer reaction in organic solvents, yielding both enantiomers
β-Adrenergic blocking agents: Substituted phenylalkanolamines. Effect of side-chain length on β-blocking potency in vitro
Fuhrer,Ostermayer,Zimmermann,Meier,Mueller
, p. 831 - 836 (2007/10/02)
The synthesis of a group of potential β-blockers bearing a new 5-ethoxysalicylamide substituent on nitrogen is described. These compounds were tested for β-adrenergic blocking potency in vitro and compared with analogous compounds bearing a tert-butyl group on nitrogen. The new N-substituent increased the β-blocking potency substantially. In a series of five homologous compounds of the type Ar(CH2)(n)CHOHCH2NHR (R = 5-ethoxysalicylamide; n = 0-4), two maxima of β-blocking potency were found for n = 0 and 2. Moreover, the carbon isostere of the corresponding (aryloxy)propanolamine still proved to be a very potent β-blocker. The ether oxygen in the side chain is therefore not an absolute requirement for activity. Structure-activity relationships are discussed.
