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|Title:||Convenient synthesis of Carvedilol utilizing 3-(9H-carbazol-4-yloxy)-1-chloropropan-2-yl phenyl carbonate as a key intermediate|
|Authors:||Kumar, B Anand|
|Keywords:||Carvedilol;3-(9H-carbazol-4-yloxy)-1-chloropropan-2-yl phenyl carbonate;3-(9H-carbazol-4-yloxy)-1-chloropropan-2-yl2-(2-methoxyphenoxy) ethylcarbamate;Impurity B;β-Adrenergic blocking agent;β-Amino alcohol|
|Abstract:||Convenient synthesis of pharmaceutically important moiety Carvedilol, 1 (β-adrenergic blocking agent) has been reported utilizing 3-(9H-carbazol-4-yloxy)-1-chloropropan-2-yl phenyl carbonate 8 as a key intermediate. The synthetic scheme involves the reaction of intermediate 8 with 2-(2-methoxy phenoxy)ethanamine 5 by using N,N-Dimethyl-4-aminopyridine (DMAP) in N,N-dimethylformamide (DMF) which yield 3-(2-(2-methoxyphenoxy)ethyl)-5-((9H-carbazol-4-yloxy)methyl)oxazolidin-2-one 7 via 1-(9H-carbazol-4-yloxy)-3-chloropropan-2-yl 2-(2-methoxyphenoxy)ethylcarbamate 6. The resulted compound 7 has further been converted to the required Carvedilol and this approach could be useful for the preparation of many β-amino alcohols without formation of Impurity B.|
|Appears in Collections:||IJC-B Vol.51B(05) [May 2012]|
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