C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/695 (2006.01) C07D 493/08 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2091001
The present invention is directed to isolation of a new taxane of the formula 1: (See Formula I) wherein R1 when taken individually is hydrogen; and R19 when taken individually is hydrogen, tri(C1-8 alkyl)silyl, or alkanoyl of 2 to 9 carbon atoms, unsubstituted or mono-, di-, or trisubstituted with halogen or monosubstituted with phenyl which is unsubstituted or mono-, di-, or trisubstituted with halogen, C1-8 alkoxy, or C1-8 haloalkoxy; or R1 and R14, when taken together, are carbonyl or C1-8 alkylidene, unsubstituted or substituted with phenyl; each of R7 and R10 is hydrogen, tri(C1-8 alkyl)silyl, or alkanoyl of 2 to 9 carbon atoms, unsubstituted or mono-, di-, or trisubstituted with halogen or monosubstituted with phenyl which is unsubstituted or mono-, di-, or trisubstituted with halogen, C1-8 alkoxy, or C1-8 haloalkoxy; and R13 is hydrogen, trialkylsilyl, -COCHOHCH- (C6H5)NHCOC6H5, -COCHOHCH(C6H5)NHCOOC(CH3)3, alkanoyl of 2 to 9 carbon atoms, unsubstituted or mono-, di-, or trisubstituted with halogen or monosubstituted with phenyl which is unsubstituted or mono-, di-, or trisubstituted with halogen, C1-8 alkoxy, or C1-8 haloalkoxy; Ac is acetyl having pharmaceutical activity, 1a 14-beta-hydroxy-10-deacetyl- baccatine III and hemisynthesis of some derivatives useful as antitumor agents and intermediates.
Bombardelli Ezio
Gabetta Bruno
Indena S.p.a.
Kirby Eades Gale Baker
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