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US 2017/0253585 A1Published application
Processes for the preparation of intermediates of raltegravir
AssigneeMylan Laboratories Limited
InventorsSiva Ram Prasad Vellanki, Raja Babu Balusu, Kiran Mitchanagatla
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Abstract
The present disclosure provides a process for the preparation of 2-(2-amino propan-2-yl)-N-(4-fluorobenzyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidine-4-carboxamide by debenzylation of benzyl(2-{4-[(4-fluorobenzyl)carbamoyl]-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl}propan-2-yl)carbamate. This process may be used in the synthesis of raltegravir and pharmaceutically acceptable salts thereof.
Claims10
A process for the preparation of 2-(2-amino propan-2-yl)-N-(4-fluorobenzyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidine-4-carboxamide of formula III, comprising:
- a. debenzylation of benzyl(2-{4-[(4-fluorobenzyl)carbamoyl]-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl}propan-2-yl)carbamate (Formula IV) in the presence of an acid;
- and
- b. isolating 2-(2-amino propan-2-yl)-N-(4-fluorobenzyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidine-4-carboxamide (Formula
Dependencies are inferred from the claim text.