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US 8,802,860 B2Granted
Method for producing substituted pyridin-2-one
AssigneeBayer Intellectual Property GmbH
InventorsJoachim Krüger, Danja Groβbach, Holger Paulsen, Walter Kroh
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Abstract
The present invention relates to a process for the preparation of substituted 3-(2-hydroxyethyl)-1-[4-nitrophenyl]pyridin-2(1H)-ones which serve as important intermediate compounds for producing drugs.
Claims17
A process for the preparation of a compound of the formula,
- in which
- R1 is hydrogen or C1-C3-alkyl
- and
- R2 is C1-C3-alkyl,
- or
- R1 is hydrogen
- and
- R2 is C1-C3-alkoxy or C1-C3-alkoxymethyl,
- comprising reducing the carboxyl group in a compound of the formula
- in which R1 and R2 are as defined above,
- in the presence of a borane complex.
8 more elements
A compound of the formula
- in which
- R1 is hydrogen or C1-C3-alkyl
- and
- R2 is C1-C3-alkyl,
- or
- R1 is hydrogen
- and
- R2 is C1-C3-alkoxy or C1-C3-alkoxymethyl,
- or a salt thereof.
6 more elements
A process for the preparation of a compound of the formula
- in which
- R1 is hydrogen or C1-C3-alkyl
- and
- R2 is C1-C3-alkyl,
- or
- R1 is hydrogen
- and
- R2 is C1-C3-alkoxy or C1-C3-alkoxymethyl,
- comprising reacting a compound of the formula
- in which R1 and R2 are as defined above,
- is reacted in a one-pot process firstly in the presence of a copper catalyst, wherein the copper catalyst is provided as a bis(2-pyridinecarboxylato)copper(II) complex or a hydrate thereof, with a malonic acid ester and a base and then with a base and water.
8 more elements
A process for the preparation of a compound of the formula
- in which
- R1 is hydrogen or C1-C3-alkyl
- and
- R2 is C1-C3-alkyl,
- or
- R1 is hydrogen
- and
- R2 is C1-C3-alkoxy or C1-C3-alkoxymethyl,
- comprising reacting a compound of the formula
- in which R1 and R2 are as defined above,
- in a one-pot process firstly in the presence of a copper catalyst with a malonic acid ester and a base and then with a base and water, wherein the base is sodium or potassium tert-butylate.
8 more elements
Dependencies are inferred from the claim text.