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US 10,301,322 B2Granted
Processes for the preparation of edoxaban and intermediates thereof
AssigneeApotex Inc.
InventorsPrabhudas Bodhuri, Avedis Karadeolian, Eduardo Gustavo Cammisa, Stuart P. Green, Melanie R. A. Green, Alfredo Paul Ceccarelli
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Abstract
The present invention provides processes for the preparation of Edoxaban (1) and salts thereof, as well as intermediates thereof. In particular, intermediate compounds and/or salts of the Formulae (3), (4), (6-A), (7-A), (8-A), (9-A) and (10-AS) are provided.
Claims3
A compound of Formula (9-A):
- wherein
- R2 is selected from the group consisting of an aliphatic group, substituted aliphatic group, aryl, substituted aryl, arylalkyl, and substituted arylalkyl;
- wherein the aliphatic group is an alkyl group selected from the group consisting of methyl, ethyl, n-propyl, iso-propyl, n-butyl, t-butyl, sec-butyl, hexanyl, 2-methyl-2-hexanyl, cyclohexyl, 1-methylcyclohexyl, cyclopropylmethyl, and isomers of n-pentyl, n-hexyl, n-heptyl, and n-octyl;
- and
- wherein substituted refers to the replacement of one or more hydrogen atoms with a substituent selected from the group consisting of R′″, OR″, NR″R″, SR″, halogen, SiR′″R′″R′″, OCOR′″, COR″, CO2R″, CONR″R″, NR″CO2R′″, NR″COR′″, SOR′″, SO2R′″, CN, NO2 and CF3;
- R″ is selected, independently, from the group consisting of hydrogen, an aliphatic group, aryl and arylalkyl;
- and
- R′″ is selected, independently, from the group consisting of an aliphatic group, aryl and arylalkyl.
5 more elements
Dependencies are inferred from the claim text.