Method for preparation of taxol using .beta.-lactam

Details Method for preparation of taxol using .beta.-lactam Method for preparation of taxol using .beta.-lactam

1989-09-29

1992-12-29

Tsang, Cecilla

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549214, 549511, 540354, C07D30514, C07F 708

Patent

active

051753154

ABSTRACT:
A .beta.-lactam of the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; and process for the preparation of taxol comprising contacting said .beta.-lactam and an alcohol in the presence of an activating agent to provide a taxol intermediate, and converting the intermediate to taxol.

REFERENCES:
patent: 4814470 (1989-03-01), Colin et al.
patent: 4857653 (1989-08-01), Colin et al.
patent: 4924011 (1990-05-01), Denis et al.
patent: 4924012 (1990-05-01), Colin et al.
patent: 5015744 (1991-05-01), Holton
patent: 5136060 (1992-08-01), Holton
Journal of Medicinal Chemistry vol. 17 p. 390, 1970.
Katritzky, "Handbook of Heterocyclic Chemistry", Pergamon Press, p. 173.
March, "Advanced Organic Chemistry" John Wiley & Sons, 3rd Ed., p. 351.
Wani et al., "Plant Antitumor Agents. VI. The Isolation and Structure of Taxol, a Novel Antileukemic and Antitumor Agent from Taxus brevifolia24", J. Am. Chem. Soc. 93:9, May 5, 1971, p. 2325-2327.
Holton, "Synthesis of the Taxane Ring System", J. Am. Chem. Soc. 1984, 106, pp. 5731-5732.
Denis et al., "A Highly Efficient, Practical Approach to Natural Taxol", J. Am. Chem. Soc. 1988, 110, 5917-5919.
Holton et al., "A Synthesis of Taxusin", J. Am. Chem. Soc., 1988, 110, pp. 6558-6560.

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