27-halo derivatives of ll-f28249 compounds

Details 27-halo derivatives of ll-f28249 compounds 27-halo derivatives of ll-f28249 compounds

C - Chemistry, Metallurgy

07

D

167/202, 260/233

C07D 493/22 (2006.01) A01N 43/90 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01)

Patent

CA 1285937

27-HALO DERIVATIVES OF LL-F28249 COMPOUNDS ABSTRACT The present invention relates to novel derivatives of LL-F28249 compounds wherein the pendent C(26,27) olefinic group at C(25) is converted into a 27-bromo or 27-chloro-26-methylene group. The 27-bromo compounds are derived by reacting the LL-F28249 com- pounds or 5-0-trisubstituted silyl LL-F28249 compounds with N-bromoacetamide or N-bromosuccinimide in aqueous acetone, followed by desilylation for silylated LL-F28249 intermediates. The 27-chloro compounds are prepared by reacting LL-F28249 compounds with N-chloro- succinimide in methanol. These novel halo compounds have anthelmintic, ectoparasitic, insecticidal, nema- ticidal and acaricidal activity and are also useful intermediates for the preparation of other novel biologically active compounds. Compositions containing the present compounds as active ingredients thereof are presented.

560560

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