Process for the preparation of tubulin inhibitors

Details Process for the preparation of tubulin inhibitors Process for the preparation of tubulin inhibitors

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01)

Patent

CA 2546899

The present invention provides a process for the preparation of 6- [(substituted) phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R1 is CF3 or C2F5; R2 is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R3 and R4 are each independently H or C,-C3 alkyl; or R3 and R4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R5; R5 is C,-C3 alkyl; wherein the dotted line is an optional bond.

La présente invention concerne un procédé de fabrication d'un sel acide dicarboxylique de 6-[(substituée phényl]-triazolopyrimidine qui, en tant que sel hydraté, est représenté par la formule (I) suivante. Dans cette formule: R?1¿ est CF¿3? ou C¿2?F¿5?; R?2¿ est H ou C¿1?-C¿3? alkyle; n est un entier de 2, 3, ou 4; X est Cl ou Br; R?3¿ et R?4¿ sont chacun indépendamment H ou C,-C¿3? alkyle; ou R?3¿ et R?4 ¿, lorsqu'ls sont éventuellement pris avec l'atome d'azote auquel ils sont chacun liés, forment un noyau hétérocyclique saturé de 4 à 6 éléments comptant 1-2 atomes d'azote et 0-1 atome d'oxygène ou 0-1 atome de soufre, et éventuellement substitué avec R?5¿; R?5¿ est C,-C¿3? alkyle; la ligne en pointillé représentant une éventuelle liaison.

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