iso-CBI and iso-CI analogs of CC-1065 duocarmycins
AssigneeThe Scripps Research Institute
InventorDale L. Boger
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Abstract
A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhance reactivity.
Claims13
A process for synthesizing a third chemical intermediate of iso-CI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CI analogs, the process comprising the following steps:
- Step A. converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
- wherein R is a radical selected from the following group:
A process for synthesizing an iso-CI analog, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the iso-CI analog as follows:
- wherein R is a radical selected from the following group:
A process for synthesizing a third chemical intermediate of iso-CBI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CBI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CBI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CBI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CBI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
A process for synthesizing a third chemical intermediate of iso-CBI analogs, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the third intermediate as follows:
- wherein R is a radical selected from the following group:
A process for synthesizing an iso-CBI analog, the process comprising the following steps:
- Step A:
- converting a first intermediate to a second intermediate as follows:
- and then
- Step B:
- converting the second intermediate of said Step A to the iso-CBI analog as follows:
- wherein R is a radical selected from the following group:
Dependencies are inferred from the claim text.