Process and intermediates for making substituted aspartic...

Details Process and intermediates for making substituted aspartic... Process and intermediates for making substituted aspartic...

2006-09-19

2006-09-19

Owens, Amelia A. (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

07109357

ABSTRACT:
Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I:wherein R1is an optionally substituted group selected from an aliphatic group, aralkyl group, heterocyclylalkyl group or aryl group, and R2is preferably a P2—P4moiety of a caspase inhibitor. Key intermediates include the azidolactones III and VIII:

REFERENCES:
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patent: WO 99/03852 (1999-01-01), None
Lakshmipathi, P., et al., “Efficient Conjugate Addition of Hydrogen Azide to Enoates,”Tetrahedron Letters, 38(14):2551-2552 (1997).
Chu, C.K., et al., “An Efficient Total Synthesis of 3′-Azido-3′-Deoxythymidine (AZT) and 3′-Azido-2′, 3′-Dideoxyuridine (AZDDU, CS-87) From D-Mannitol,”Tetrahedron Letters, 29(42):5349-5352 (1988).

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