Method for producing inhibitor of activated blood coagulation factor x (fxa)
US-2017050983-A1 · Feb 23, 2017 · US
US10301322B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10301322-B2 |
| Application number | US-201715850882-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 21, 2017 |
| Priority date | Dec 27, 2016 |
| Publication date | May 28, 2019 |
| Grant date | May 28, 2019 |
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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.
Opening claim text (preview).
What is claimed is: 1. A compound of Formula (9-A): wherein R 2 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″, CO 2 R″, CONR″R″, NR″CO 2 R′″, NR″COR′″, SOR′″, SO 2 R′″, CN, NO 2 and CF 3 ; 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. 2. The compound of claim 1 , wherein R 2 is an aliphatic group or a substituted aliphatic group. 3. The compound of claim 2 , selected from the group consisting of:
Ortho-condensed systems · CPC title
with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring · CPC title
The ring being saturated · CPC title
comprising a heterocyclic ring · CPC title
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