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US 5,621,108 AGranted
Processes and intermediates for preparing macrocycles
AssigneeThe Trustees of the University of Pennsylvania
InventorsAmos B. Smith, III, Stephen M. Condon, Johnnie L. Leazer, Jr., Robert E. Maleczka, John A. McCauley, James W. Leahy
Life of this patent
Estimating the term…
Abstract
Novel processes for the preparation of lactam- and lactone-containing macrocyles are provided. In preferred embodiments, rapamycin and demethoxyrapamycin are prepared by a convergent synthesis regime. Intermediates useful in the synthetic processes are also provided.
Claims10
A compound of formula VII:
- ##STR20## wherein:
- R.sub.1, R.sub.4, and R.sub.9 are, independently, hydrogen or a hydroxyl protecting group;
- R.sub.2 is alkyl having from one to about six carbon atoms;
- R.sub.7 is hydrogen or alkoxy having one to about six carbon atoms;
- R.sub.10 is H, OH, or alkoxy having one to about six carbon atoms;
- R.sub.13 is a carbonyl group or a protected derivative thereof;
- R.sub.21 is alkyl having one to about six carbon atoms;
- M is a tetravalent metal atom;
- and
- X is halogen.
7 more elements
A compound of formula:
- ##STR21## wherein:
- R.sub.1, R.sub.4, and R.sub.9 are, independently, hydrogen or a hydroxyl protecting group;
- R.sub.2 is alkyl having from one to about six carbon atoms;
- R.sub.7 is hydrogen or alkoxy having one to about six carbon atoms;
- R.sub.10 is H, OH, or alkoxy having one to about six carbon atoms;
- R.sub.13 is a carbonyl group or a protected derivative thereof;
- R.sub.21 is alkyl having one to about six carbon atoms;
- M is Sn;
- and
- X is halogen.
7 more elements
Dependencies are inferred from the claim text.