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US 7,030,243 B1Granted
Process for making camptothecin derivatives
AssigneeBioNumerik Pharmaceuticals, Inc.
InventorsYe Wu, Kesavaram Narkunan, Jianyan Wang, Harry Kochat
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 a silylated heterocyclic compound in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.
Claims7
A process for synthesizing a compound having the formula I:
- where A is —(CH2)m—;
- m is 1 to 6;
- and R1, R2, and R3 are individually lower alkyl or aryl substitutent groups;
- the process comprising:
- a) providing a quantity of substantially pure camptothecin, and dissolving said camptothecin in a solution of a strong acid;
- b) providing a quantity of a compound having the formula II:
- R3R2R1Si—Am—X (II),
- wherein X is 1,3-dioxolane and dissolving II in an organic-based solution;
- and
- c) mixing the solutions from steps a) and b) for a sufficient period of time to allow them to react to form the formula I compound.
7 more elements
Dependencies are inferred from the claim text.