Camptothecin analogs and methods of preparation thereof

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United States of America Patent

PATENT NO 6410731
SERIAL NO

09728031

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A method of synthesizing a compound having the formula ##STR1## via a cascade radical 4+1 annulation includes the step wherein the precursor ##STR2## or the precursor ##STR3## is reacted with an arylisonitrile having the formula ##STR4## wherein X is a radical precursor such as Cl, Br or I. R.sup.6 is preferably --Si(R.sup.8 R.sup.9 R.sup.10) or --(R.sup.7)Si(R.sup.8 R.sup.9 R.sup.10), wherein R.sup.7 is an alkylene group, an alkenylene group, or an alkynylene group; and R.sup.8, R.sup.9 and R.sup.10 are independently a C.sub.1-10 alkyl group, a C.sub.2-10 alkenyl group, a C.sub.2-10 alkynyl group, an aryl group or a --(CH.sub.2).sub.N R.sup.11 group, wherein N is an integer within the range of 1 through 10 and R.sup.11 is a hydroxy group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, --SR.sup.c or a nitro group. R.sup.1 -R.sup.4 can be broadly substituted. R.sup.5 is preferably a C.sub.1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group. R.sup.13 is preferably H, F or --CH.sub.3. R.sup.16 is R.sup.16 is --C(O)R.sup.f or H. The E-ring (the lactone ring) may be opened.

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Patent Owner(s)

Patent OwnerAddress
AKER BIOMARINE ASASTANDVEIEN 15 LYSAKER 1336

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Burke, Thomas G Lexington, KY 18 346
Curran, Dennis P Pittsburgh, PA 56 294
David, Bom Pittsburgh, PA 13 68

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