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US 2010/0249429 A1Published application
Process for the manufacture of valsartan
OwnerDonatienne Denni-Dischert, Hans Hirt +5inventors
InventorsDonatienne Denni-Dischert, Hans Hirt, Dan Neville, Gottfried Sedelmeier, Anita Schnyder, Nadine Derrien, Daniel Kaufmann
Life of this patent
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Abstract
The present invention relates to a process for the manufacture of an angiotensin receptor blocker (ARB; also called angiotension II receptor antagonist or AT1 receptor antagonist) and salts thereof, to novel intermediates and process steps.
Claims10
A process for the manufacture of the compound of formula (I)
- or a salt thereof, comprising
- (a) reacting a compound of formula (II a)
- or a salt thereof, wherein R1 is hydrogen or a tetrazole protecting group, with a compound of formula
- or a salt thereof, wherein R2 represents hydrogen or a carboxy protecting group, under the conditions of a reductive amination;
- and
- (b) acylating a resulting compound of formula (II c)
- or a salt thereof with a compound of formula (II d)
- wherein R3 is an activating group;
- and,
- (c) if R1 and/or R2 are different form hydrogen, removing the protecting group(s) in a resulting compound of formula (II e)
- or a salt thereof;
- and
- (d) isolating a resulting compound of formula (I) or a salt thereof;
- and, if desired, converting a resulting free acid of formula (I) into a salt thereof or converting a resulting salt of a compound of formula (I) into the free acid of formula (I) or converting a resulting salt of a compound of formula (I) into a different salt.
11 more elements
A process for the manufacture of a compound of formula
- wherein R1 represents hydrogen or a tetrazole protecting group and R2 represents hydrogen or a carboxy protecting group,
- comprising reacting a compound of formula (II a)
- or a salt thereof, wherein R1 is hydrogen or a tetrazole protecting group, with a compound of formula
- or a salt thereof, wherein R2 represents hydrogen or a carboxy protecting group, under the conditions of a reductive amination.
1 more element
A compound of formula
- wherein R1 is hydrogen or a tetrazole protecting group and R2 is hydrogen or a carboxy protecting group, excluding a compound of formula (II c) wherein R1 is ethyl and R2 is trityl.
A compound of formula
- wherein R1 is hydrogen or a tetrazole protecting group and R2 is hydrogen or a carboxy protecting group.
A process for the manufacture of a compound of formula
- wherein R1 represents hydrogen or a tetrazole protecting group and R2 represents hydrogen or a carboxy protecting group,
- comprising acylating a resulting compound of formula (II c)
- or a salt thereof with a compound of formula (II d)
- wherein R3 is an activating group.
1 more element
Dependencies are inferred from the claim text.