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US 6,723,849 B1Granted
Process for making camptothecin derivatives
AssigneeBioNumerik Pharmaceuticals, Inc.
InventorsKesavaram Narkunan, Harry Kochat, Xinghai Chen
Life of this patent
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Abstract
A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with an aldehyde in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.
Claims9
A process for synthesizing camptothecin derivatives having the formula:
- where
- A is —(CH2)n— where n is 1 to 6;
- and R1, R2, and R3 are individually lower alkyl or aryl, the process comprising the steps of:
- a) providing a quantity of substantially pure camptothecin, and dissolving in a strong acid;
- b) adding a strong oxidizing agent to the camptothecin and strong acid solution to form a reaction mixture, then adding the reaction mixture to a vessel containing:
- i) an aldehyde having the formula R1R2R3Si—(CH2)nCHO in sufficient quantities to react with the reaction mixture;
- ii) a nonpolar, aprotic solvent;
- and
- iii) an iron salt;
- c) agitating the vessel for a predetermined time to produce the formula I compound.
7 more elements
Dependencies are inferred from the claim text.