C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 491/22 (2006.01) C07D 471/04 (2006.01) C07D 471/14 (2006.01)
Patent
CA 2144048
The present invention provides a process for preparing certain pyrrolo[3,4-b]quinolines, certain 1H-pyrano[3',4':6,7]indo- lizino[1,2-b]quinolin-3,14(4H,12H)-diones, specifically camptothecin and its analogs, and certain 8-methyl-7-(oxopropyl)-indoliz- ino[1,2-b]quinolin-9(11H)-ones, specifically mappicine ketones and mappicines, said process comprising the step of intramolecu- lar [4 + 2] cycloaddition of the N-arylimidate portion of a compound of formula (IV) where: X = OH, OAlCl2, Cl, Br, I, F, OR, OSO2CF3 or any good leaving group or H; R1 = H, or OR, where R is an ester protecting group; R2 = H, NO2, or a protect- ed amine function; R3 = H, C2H5, or a trialkylsilyl; R4 = H or CH2COOEt; R5 = COOMe or tosyl; or R4 and R5 are joined together to form a substituted pyridone (IVa): Y= H or Y,R1 = -OCH2O-, formula in which A = H,COOR, or a functionnali- ty for preparation of the hydroxymethyl (C-17) portion of an E ring lactone; B = H, OH, an appropriate leaving group such as halide or O(trifluoromethanesulfonate) or a functionality for preparation of C-(18-21) of the E ring lactone portion of camptothecin, with the unactivated acetylene portion of said compound.
Fortunak Joseph
Zhuang Zhiping
Gowling Lafleur Henderson Llp
Smithkline Beecham Corporation
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