Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof
US6252079A · kind A · utility
7Cited by
1References
7Claims
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Key dates
| Filing date | Jul 2, 1997 |
| Grant date | Jun 26, 2001 |
| Priority date | — |
| Expiry date | Jul 2, 2017 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/582
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursor ##STR1## is reacted with an aryl isonitrile having the formula ##STR2## wherein X is Br or I, and R.sup.4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R.sup.16 is H, a C.sub.1 -C.sub.6 alkoxy group, a ##STR3## group wherein p is an integer between 4 and 12, or a C.sub.1 -C.sub.12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.