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US 8,445,701 B2Granted
Intermediates for the preparation of analogs of halichondrin B
AssigneeEisai R&D Management Co., Ltd.
InventorsBrian Austad, Charles E. Chase, Francis G. Fang, Marc Pesant
Life of this patent
Estimating the term…
Abstract
Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
Claims6
A compound of formula F-1:
- wherein:
- each of PG1 and PG2 is independently a suitable hydroxyl protecting group, taken with the oxygen atom to which it is bound, selected from the group consisting of an acetate, a carbonate, a sulfonate, a silyl ether, an alkyl ether, an arylalkyl ether, and an alkoxyalkyl ether, or PG1 and PG2 are taken together, with the oxygen atoms to which they are bound, to form a diol protecting group;
- R1 is R or OR;
- R2 is CHO or —CH═CH2;
- and
- each R is independently hydrogen, C1-4 haloaliphatic, benzyl, or C1-4 aliphatic, provided that, when R1 is OMe, then PG1 and PG2 do not form an acetonide group, or PG1 and PG2 are H, R1 is OH, and R2 is —CH═CH2.
3 more elements
Dependencies are inferred from the claim text.