216870-24-5Relevant academic research and scientific papers
NEW PROCESS FOR PREPARING LORATADINE FROM A KETONE INTERMEDIATE
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Page/Page column 12, (2015/06/18)
This application is directed to a last step synthetic process for making loratadine from ketone intermediate.
Process for preparing tricyclic compounds having antihistaminic activity
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, (2008/06/13)
Disclosed is a process for preparing a compound having the formula: wherein R1is selected from the group consisting of: alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, and cycloalkylalkyl, R1being optionally substituted by substituents selected from halo, —OH, alkyl, alkoxy, or —CF3, said process comprising the following steps: (a) reacting a ketone having the formula with a carbanion having the formula wherein R1is as defined above, and R2and R3are independently selected from the group consisting of —ORAand —RA, wherein RAis alkyl, phenyl, substituted phenyl, cycloalkyl, substituted cycloalkyl, cycloalkylalkyl, or substituted cycloalkylalkyl; (b) treating the reaction mixture from step (a) with a protonating agent; and (c) thermally decomposing the product of 16, to form the compound of formula (I). The compounds made by this process have antihistaminic activity, e.g., loratadine. Also disclosed are novel intermediates having the formula wherein R1, R2and R3are as defined above.
Syntheses of novel piperidin-4-ylphosphinic acid, and piperidin-4-ylphosphonic acid analogues of the inhibitory neurotransmitter 4-aminobutyric acid (GABA)
Kehler, Jan,Ebert, Bjarke,Dahl, Otto,Krogsgaard-Larsen, Povl
, p. 3241 - 3243 (2007/10/03)
Piperidin-4-ylphosphinic acid, methyl(piperidin-4-yl)phosphinic acid and piperidin-4-ylphosphonic acid analogues of the GABAA agonist piperidin-4-ylcarboxylic acid (isonipecotic acid) were synthesised. The acid groups were introduced using a sequential Pudovik addition followed by a Barton deoxygenation procedure and finally followed by acidic hydrolysis. The mild and efficient procedure gave the target amino acids in good yields.
