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AssigneeMereo Biopharma 1 Limited
InventorsYunzhong LI, Xiaobin JIANG, Carmen RUIZ, Jerome DAUVERGNE
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Provided is a process for preparing the compound 3 (3) or a salt or a solvate thereof, the process comprising the steps of a) Mixing the compound 4 with a mineral acid (4); b) Adding a nitrite salt or an organic nitrite derivative to the reaction mass to form a diazonium salt; c) Adding a sulfur-containing reducing agent to the reaction mass to form a hydrazyl sulfur complex, such as a hydrazyl sulfite complex; d) Hydrolysing the hydrazyl sulfur complex to provide the compound 3 or a salt or solvate thereof; and e) Optionally isolating the compound 3 or a salt or solvate thereof. Further provided is the use of the compound 3 in the synthesis of 3-[5 -Amino-4-(3-Cyanobenzoyl)-Pyrazol-1-yl]-N-Cyclopropyl-4-Methylbenzamide.
A process for preparing the compound 3
The process of any preceding claim, wherein the sulfur-containing reducing agent is selected from the group consisting of sulfite salts such as alkali metal sulfite salts, such as lithium sulfite, sodium sulfite and potassium sulfite, preferably sodium sulfite;
The process of any preceding claim, wherein after step (a) the reaction mass is cooled, preferably to less than about 10° C.
The process of any preceding claim, wherein steps (b) and (c) are performed at a temperature of less than about 10° C.
The process of any preceding claim, wherein after step (c) the reaction mass is heated, preferably to greater than about 50° C., more preferably to about 60° C.
The process of any preceding claim, wherein hydrolysis of the hydrazyl sulfur complex comprises adding a mineral acid, such as HCl, H2SO4, H3PO4, HBF4 and HBr, preferably HCl.
The process of any preceding claim, wherein after step (d) the pH of the reaction mass is adjusted to about 5 to about 7, preferably about 5.6 to about 5.8.
The process of any preceding claim, wherein after step (e) the compound 3 is slurried in water, then the compound 3 is isolated, washed with water and optionally dried.
The process of any preceding claim, wherein isolating the compound 3 in step (e) comprises filtering the compound 3, washing the filtrate with water, and optionally drying the filtrate.
A product obtained by the process of any preceding claim.
Dependencies are inferred from the claim text.