Study of Michael Addition Desymmetrization for the Asymmetric synthesis of R Mexiletine S Enciprazine and N Homo serine lactone

Abstract

The Michael reaction is the conjugate addition of nucleophile or a carbanion to newlinean and#945;, and#946;-unsaturated carbonyl compound. It is the most useful method for the newlineformation of C-C, C-N, and C-O bond formation. There have been many reports newlineii newlineof enantioselective Michael additions with chiral catalysts, including metal-based newlinecatalysts and multi metallic catalysts as well as organic catalysts. A practical newlineMichael addition of 1, 3-dicarbonyl compounds to nitro alkenes remain largely newlineunexplored to develop Michael addition. newlineB. Desymmetrization: newlineThe stereochemical modification of molecules called desymmetrization. The newlineformation of chiral compounds from prochiral or meso molecule with multiple newlinestereo centres is done in one step. For the synthesis of chiral compound, newlineenantioselective desymmetrization reactions have achieved much attention. Now newlinea day s desymmetrization of prochiral or meso molecule to yield an newlineenantiomerically improved product is becoming a powerful synthetic tool. newlineC. Mexiletine: newlineMexiletine is first developed clinical drug, which belong to the group Ib sodium newlinechannel blockers. Mexiletine is also clinically used as an antiarrhythmic, newlineantimyotonic, analgesic, and pain relief oral drug in its racemic form. The and#946;- newlineblockers are play key role to block only catecholamines hormones in brain, heart, newlineand blood vessels that results the heart beats more slowly with less force. The newlinesynthesis of (R)-Mexiletine was used from glycerol by modified newlinedesymmetrization strategy. newlineD. Enciprazine: newlineEnciprazine is one of the and#946;-blockers which are also known as and#946;-adrenergic newlineblocking agents or adrenergic inhibitors that belong to a larger class of newlinemedicines. The Scottish pharmacologist Sir James W. Black was invented the newlinePropranolol which is the first clinically useful and#946;-blockers in the year of 1950s in newlineEli Lilly Laboratories. For the year of 1988 Sir James W. Black was awarded newlinewith the Nobel Prize in Medicine for their discoveries of important principles for newlinedrug treatment. Enciprazine is a non-benzodiazepine anxiolytic drug, as it newlinecontains