C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 333/54 (2006.01) C07D 333/56 (2006.01) C07D 333/62 (2006.01) C07D 409/12 (2006.01) C07F 5/02 (2006.01)
Patent
CA 2216100
The present invention provides processes for preparing compounds of formula (I), wherein R1 is -H, -OH, or OR3, in which R3 is a hydroxy protecting group; and R2 is -H, -OH, or OR4, in which R4 is a hydroxy protecting group, and for preparing compounds of formula (VII), wherein R1 is -H, -OH, or OR3, in which R3 is a hydroxy protecting group; R2 is -H, -OH, or OR4, in which R4 is a hydroxy protecting group; R5 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1- pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; R6 is bromo, chloro, iodo, or an activating ester group; and n is 2 or 3. Also provided are processes for preparing compounds of formula (VII) in addition to intermediates of formula (IX), wherein R1' is -OH, or -OR3, in which R3 is a hydroxy protecting group; and Z is bromo, iodo, triflate, or -B(OH)2.
L'invention concerne la préparation de composés de la formule (I), où R?1¿ est -H, -OH, ou OR?3¿, où R?3¿ est un groupe de protection hydroxy; et R?2¿ est -H, -OH, ou OR?4¿ , où R?4¿ est un groupe de protection hydroxy. L'invention concerne aussi des composés de formule (VII), où R?1¿ est -H, -OH, ou OR?3¿, où R?3¿ est un groupe de protection hydroxy; R?2¿ est -H, -OH, ou OR?4¿, où R?4¿ est un groupe de protection hydroxy; R?5¿ est 1-pipéridinyle, 1-pyrrolidinyle, méthyle-1-pyrrolidinyle, diméthyle-1-pyrrolidinyle, 4-morpholino, diméthylamino, diéthylamino, diisopropylamino, ou 1-hexaméthyléneimino; R?6¿ est un bromo, chloro, iodo, ou un groupe ester d'activation; et n vaut 2 ou 3. L'invention concerve en outre des procédés de préparation de composés intermédiaires de formule (VII) s'ajoutant à des intermediaires de formule (IX) où R?1'¿ est -OH, ou -OR?3¿, où R?3¿ est un groupe de protection hydroxy et Z est bromo, iodo, triflate, ou -B(OH)¿2?.
Hauser Kenneth Lee
Palkowitz Alan David
Sall Daniel Jon
Thrasher Kenneth Jeff
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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