Intermediates for substituted azetidinones useful as anti-inflam

Details Intermediates for substituted azetidinones useful as anti-inflam Intermediates for substituted azetidinones useful as anti-inflam

1991-09-20

1992-09-22

Dentz, Bernard

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D30778

Patent

active

051498383

ABSTRACT:
Disclosed is a process for the enantioselective synthesis of the compound of Formula I and related compounds. The process comprises the synthesis of the benzofuranyl carboxaldehyde; introduction of the benzylic amine functionality with control of the absolute stereochemistry; preparation of the azetidinone fragment and its coupling to the benzofuranyl amine fragments. The carboxylic acid in Formula I is liberated using heterogenous palladium catalyzed de-allylation of the allyl esters. Compounds I have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents. ##STR1##

REFERENCES:
patent: 4680391 (1987-07-01), Firestone et al.
Organic Synthesis, Coll. vol. 5, pp. 251-254 (1967).
Graalmann et al., Chem. Ber., vol. 117, pp. 2988-2997 (1984).
Lal et al., Tet. Letters, No. 23, pp. 1977-1980 (1977).
Yoshioka et al., Tet. Letters, vol. 30, No. 13, pp. 1657.congruent.1660 (1989).

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