Alternative synthesis of renin inhibitors and intermediates...

Details Alternative synthesis of renin inhibitors and intermediates... Alternative synthesis of renin inhibitors and intermediates...

C - Chemistry, Metallurgy

07

C

C07C 53/128 (2006.01) C07C 271/10 (2006.01) C07D 207/38 (2006.01) C07D 211/76 (2006.01) C07D 307/32 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2576749

The present invention relates to synthetic routes to prepare a compound of the formula (A); wherein R1 is halogen, C1-6halogenalkyl, C1-6 alkoxy-C1-6 alcoxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1- 6hydroxyalkyl, Cl-6alkoxy-C 1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1- 6aminoalkyl, C1-6alkylamino-C1-6alkyl, Cl-6dialkylamino-C1-6alkyl, C1- 6alkanoylamino~ C1-6alkyl, HO(O)C-Cl-6alkyl, C1-6alkyl-O-(O)C-C1-6alkyl, H2N- C(O)-Cl-6alkyl, C1-6alkyl-HN~C(O)-C1-6alkyl or (C1-6alkyl)2N-C(O)-C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

L'invention concerne des moyens synthétiques permettant de préparer un composé de formule (A); dans laquelle R1 désigne halogène, C1-6halogènalkyle, C1-6 alcoxy-C1-6 alkyloxy ou C1-6alcoxy-C1-6alkyle; R2 représente halogène, C1-4alkyle ou C1-4alcoxy; R3 et R4 représentent de manière indépendante C3-6alkyle ramifié; et R5 désigne cycloalkyle, C1-6alkyle, C1-6hydroxyalkyle, Cl-6alcoxy-C 1-6alkyle, C1-6alkanoyloxy-C1-6alkyle, C1-6aminoalkyle, C1-6alkylamino-C1-6alkyle, Cl-6dialkylamino-C1-6alkyle, C1-6alkanoylamino- C1-6alkyle, HO(O)C-Cl-6alkyle, C1-6alkyl-O-(O)C-C1-6alkyle, H2N-C(O)-Cl-6alkyle, C1-6alkyl-HN-C(O)-C1-6alkyle ou (C1-6alkyl)2N-C(O)-C1-6alkyle; ou un sel acceptable sur le plan pharmaceutique de celui-ci, des intermédiaires clefs obtenus grâce à ces moyens et la préparation de ceux-ci.

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