| 摘要 |
A method of making racemic DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employing novel intermediates of Formula XX and XXI: <IMAGE> XX <IMAGE> XXI as precursors to the DE ring intermediate. The present invention also provides camptothecin analog of Formula I-A <IMAGE> (I-A) wherein: Hal is a halogen is selected from the group consisting of F, Cl, and Br; R may be loweralkyl; R1 may be H, loweralkyl, loweralkoxy, or halo; R2, R3, R4, and R5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkyl-thio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, amninomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. Additionally, novel compounds useful in the preparation of the compounds of Formula I-A are also provided.
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