Synthetic method for the preparation of an alkoxymethylene-benzoylacetonitrile
AssigneeMereo Biopharma 1 Limited
InventorsMark MEISENBACH, Benjamin MARTIN, Niek Johannes RONDE
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Abstract
Provided is a process for preparing a compound of Formula A (Formula A) or a salt or solvate thereof, the process comprising the step of: a) Reacting the compound 1 (1) with a trialkyl orthoformate to provide a compound of Formula A or a salt or solvate thereof, wherein R is the alkyl moiety of the trialkyl orthoformate. Further provided is the compound 2 or a salt or solvate thereof. (2) The use of these compounds in the synthesis of 3-[5-Amino-4-(3-Cyanobenzoyl)-Pyrazol-1-yl]-N-Cyclopropyl-4-Methylbenzamide is also provided.
Claims14
A process for preparing a compound of Formula A
- or a salt or solvate thereof, the process comprising the step of:
- a) Reacting the compound 1
- with a trialkyl orthoformate to provide a compound of Formula A or a salt or solvate thereof,
- wherein R is the alkyl moiety of the trialkyl orthoformate.
The process of any preceding claim, wherein the trialkyl orthoformate is triethyl orthoformate and Formula A is the compound 2
The process of any preceding claim, wherein step (a) comprises the steps of
- a) Adding the compound 1 in an aprotic solvent;
- b) Distilling the reaction mass;
- and
- c) Adding the trialkyl orthoformate to the reaction mass during distillation to provide a compound of Formula A.
The process of any preceding claim, further comprising the step of adding to the reaction mass an organic acid anhydride, preferably selected from the group consisting of acetic anhydride, propionic anhydride, butyric anhydride, acetic propionic anhydride and acetic butyric anhydride, more preferably acetic anhydride.
A product obtained by the process of any preceding claim.
The compound 2
- or a salt or solvate thereof.
Dependencies are inferred from the claim text.