Following is the structural formula of the antihypertensive drug labetalol, a non- specific B-adrenergic blocker with vasodilating activity. Members of this class have received enormous clinical attention because of their effectiveness in treating hypertension (high blood pressure), migraine headaches, glaucoma, ischemic heart disease, and certain cardiac arrhythmias. This retrosynthetic analysis involves dis- connects to the a-haloketone (B) and the amine (C). Each is in turn derived from a simpler, readily available precursor. OH H N. Ph Ph H,N N. H,N НО НО Labetalol (A) CI + H,N. Ph > Ph H,N НО (В) (C) (D) EtO,C H,N Ph НО (E) (F) НО НО PhCH,CI Salicylic acid Benzyl chloride
Catalysis and Enzymatic Reactions
Catalysis is the kind of chemical reaction in which the rate (speed) of a reaction is enhanced by the catalyst which is not consumed during the process of reaction and afterward it is removed when the catalyst is not used to make up the impurity in the product. The enzymatic reaction is the reaction that is catalyzed via enzymes.
Lock And Key Model
The lock-and-key model is used to describe the catalytic enzyme activity, based on the interaction between enzyme and substrate. This model considers the lock as an enzyme and the key as a substrate to explain this model. The concept of how a unique distinct key only can have the access to open a particular lock resembles how the specific substrate can only fit into the particular active site of the enzyme. This is significant in understanding the intermolecular interaction between proteins and plays a vital role in drug interaction.
Labetalol has two chiral centers and, as produced in this synthesis, is a racemic
mixture of the four possible stereoisomers. The active stereoisomer is dilevalol, which has the R,R configuration at its chiral centers. Draw a structural formula of dilevalol showing the configuration of each chiral center.
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