C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/7.06
C07K 14/70 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1201710
Abstract of the Disclosure A process for preparing a compound of the general formula Image (I) and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D, when applicable, define the chirality; R1 is hydrogen, C1-C3 primary alkyl, or allyl; R2 is hydrogen or C1-C3 primary alkyl, subject to the limitation that when R1 is allyl, R2 is hydrogen; R3 is hydrogen or C1-C3 primary alkyl; R4 is C1-C4 primary or secondary alkyl; R5 is hydrogen or C1-C4 primary or secondary alkyl; R6 is hydrogen or C1-C3 primary alkyl; R7 is hydrogen or C1-C3 primary alkyl; Y is hydrogen or acetyl; Z is Image in which R8 is C1-C3 alkyl or hydrogen; and W is isopropyl, -VR9, or -CH2-X-CH3, in which V is O or S, R9 is C1-C4 alkyl or aralkyl, and X is O, S, or -CH2-, subject to the limitation that, when W is isopropyl, R7 is C1-C3 primary alkyl,and when W is -VR9, wherein V is S and R9 is methyl, then R8 is C1-C3 alkyl; which comprises cleaving the blocking agents from the correspondingly protected compound of formula (I) with a deblocking agent, as for example by the use of a substantially dry acid medium, is described herein. These compounds are useful as analgesic agents.
286528
Frederickson Robert C.a.
Shuman Robert T.
Smithwick Edward L. Jr.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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