Hitting a soft drug with a hard nucleophile: Preparation of esmolol's metabolite by treatment with bis(tributyltin) oxide
A facile method for the production of esmolol's metabolite in high purity is described. Bis(tributyltin) oxide is used to disrupt esmolol's ester linkage, and hydrolysis is completed by addition of water, which also allows the inorganic side products to be conveniently extracted into ether. Evaporation of the aqueous phase and trituration with ethyl acetate provides the carboxylic acid-amine internal salt as a white, free-flowing powder. Taylor & Francis Group, LLC.
Zhang, Cunyu A.,Erhardt, Paul W.
p. 722 - 726
(2012/01/13)
MULTI-DOSE CONCENTRATE ESMOLOL WITH BENZYL ALCOHOL
Disclosed are concentrate esmolol injection essentially free from other related esters of esmolol and diluted esmolol compositions. The concentrate esmolol formulation includes from about 25-1000 mg/ml of esmolol and about 1-25% w/v of benzyl alcohol and the combination thereof. The compositions can also be used as multi-dose compositions. The present invention also discloses diluted, ready-to-use compositions of esmolol prepared by dilution of the present invention concentrates. Also disclosed are methods of making and using the ready-to-use compositions of the present invention.
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Page/Page column 2-3
(2009/01/20)
Ultra-Short-Acting β-Adrenergic Receptor Blocking Agents. 2. (Aryloxy)propanolamines Containing Esters on the Aryl Function
Several short-acting β-adrenergic receptor blocking agents have been prepared by incorporating ester functions into the aryl portion of certain (aryloxy)propanolamine systems.In particular, methyl 3-phenyl>propionate hydrochloride (ASL-8052) was found to be a moderately potent, cardioselective compound with a short duration of action when determined in in vivo canine models.
Erhardt, Paul W.,Woo, Chi M.,Anderson, William G.,Gorczynski, Richard J.
p. 1408 - 1412
(2007/10/02)
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