Back to results
US 8,785,642 B2Granted
Process for preparing 6-substituted-1-(2H)-isoquinolinones and intermediate compound
AssigneeSanofi
InventorsSimon Gessler, Theo Wollmann
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel substituted phenyl compounds of the formula and to a process for making them. The compounds can be used as intermediates for making 6-substituted-1-(2H)-isoquinolinone derivatives.
Claims16
A process for the preparation of a compound of the formula
- wherein
- n is 1, 2, 3 or 4;
- and
- R1 is H or a protecting group,
- comprising
- (B) reacting a compound of formula (IV)
- wherein R1 is a protecting group
- with a mixture of a reagent of the formula (R2O)2HC—N(CH3)2 (V), wherein R2 is (C1-C6)alkyl, and pyrrolidine,
- wherein reagent (V) is used in a molar excess of 1.5 or more equivalents and the pyrrolidine is used in a molar excess of 4.0 or more equivalents over a compound of formula (IV);
- and
- optionally removing the protection group in a compound of formula (VI) to give a compound of formula ((VI) wherein R1 is H.
8 more elements
A compound of formula (VI)
- wherein R1 is H or a protecting group and
- n is 1, 2, 3 or 4.
Dependencies are inferred from the claim text.