Process for the manufacture of camptothecin derivatives
OwnerKevin E. Henegar, John C. Sihinventors
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Abstract
This invention discloses and claims novel intermediates and procedures for the synthesis of camptothecin derivatives, such as irinotecan, and other compounds related to the synthesis of CPT-11. Related procedures and compounds are also disclosed, such as a novel method of making mappicine.
Claims9
The process for producing the compounds described and labeled in the specification as of formula 13G comprising the step of mixing the compounds described and labeled in the specification as of formula 12G with an acrylate ester in the presence of base;
- wherein
- R4 is optionally substituted C1-8 alkyl, C3-10 cycloalkyl, lower alkyl-C3-10 cycloalkyl, alkenyl, aryl, substituted aryl, alkylaryl, or substituted alkylaryl;
- R6 is optionally substituted C1-8 alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, C3-10 cycloalkyl, lower alkyl-C3-10 cycloalkyl, heteroaryl, or substituted heteroaryl;
- and
- R8 is optionally substituted C1-8 alkyl, C3-10 cycloalkyl, lower alkyl-C3-10 cycloalkyl, alkenyl, aryl, substituted aryl, alkylaryl, or substituted alkylaryl.
The process for producing the compounds described and labeled in the specification as of formula 14G comprising the step of mixing the compounds described and labeled in the specification as of formula 13G with a strong acid;
- wherein
- R6 is optionally substituted C1-8 alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, C3-10 cycloalkyl, lower alkyl-C3-10 cycloalkyl, heteroaryl, or substituted heteroaryl;
- and
- R8 is optionally substituted C1-8 alkyl, C3-10 cycloalkyl, lower alkyl-C3-10 cycloalkyl, alkenyl, aryl, substituted aryl, alkylaryl, or substituted alkylaryl.
Dependencies are inferred from the claim text.