C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/325
C07D 217/16 (2006.01) C07D 207/16 (2006.01)
Patent
CA 1231714
ABSTRACT METHOD FOR MAKING SUBSTITUTED PROLINES A process is provided for making substituted prolines of the structure Image wherein X is lower alkyl or aryl, R is H, lower alkyl or an alkali metal and Z is an N-protecting group, which method includes the step of reacting a compound of the structure Image wherein Z and R are as defined above and Q is Br, tosyloxy or mesylate, with an organic copper lithium compound of the structure XYCuLi wherein X is as defined above and Y is lower alkyl, aryl or CN. Where X is phenyl, the corresponding 4-cyclohexyl compound may be produced by conventional hydrogenation techniques. The compounds produced are useful as intermediates in the preparation of phosphinic acid derivatives useful in the treatment of hypertension.
463515
Brandt Steven
Floyd David M.
Moniot Jerome L.
Thottathil John K.
Osler Hoskin & Harcourt Llp
Squibb (e.r.) & Sons Inc.
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