Intermediates in the preparation of homocamptothecin analogs
View Patent ↗A compound having the formula in racemic form, enantiomerically enriched form or enantiomerically pure form; wherein X is a radical precursor; R 5 is a C 1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group; R 6 is an alkyl group, —Si(R 8 R 9 R 10 ) or —(R 7 )Si(R 8 R 9 R 10 ), wherein R 7 is an alkylene group, an alkenylene group, or an alkynylene group; and R 8 , R 9 and R 10 are independently a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group, an aryl group or a —(CH 2 ) N R 11 group, wherein N is an integer within the range of 1 through 10 and R 11 is a hydroxy group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SR c or a nitro group; and R 13 is H, F or —CH 3 .
1. A compound having the formula
in racemic form, enantiomerically enriched form or enantiomerically pure form;
wherein X is a radical precursor;
R 5 is a C 1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group;
R 6 is an alkyl group, —Si(R 8 R 9 R 10 ) or —(R 7 )Si(R 8 R 9 R 10 ), wherein R 7 is an alkylene group, an alkenylene group, or an alkynylene group; and R 8 , R 9 and R 10 are independently a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group, an aryl group or a —(CH 2 ) N R 11 group, wherein N is an integer within the range of 1 through 10 and R 11 is a hydroxy group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SR c or a nitro group; and
R 13 is H, F or —CH 3 .
2. The compound of claim 1 wherein R 5 is an ethyl group, an allyl group, a benzyl group or a propargyl group.
3. The compound of claim 1 wherein X is Br or I.
4. The compound of claim 3 wherein R 13 is H.
5. The compound of claim 4 wherein R 5 is an ethyl group.