10-desacetoxytaxol derivatives

Details 10-desacetoxytaxol derivatives 10-desacetoxytaxol derivatives

1992-09-22

1994-09-27

Dentz, Bernard

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549511, C07D30514

Patent

active

053508661

ABSTRACT:
The present invention relates to 10-desacetoxytaxol and derivatives thereof, which are useful as antitumor agents. These compounds have the formula ##STR1## wherein R.sub.2 is hydrogen, hydroxy or a protected hydroxy group; R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, a protected hydroxy group, methyl, --SH, --NH.sub.2, or --NR.sub.8 R.sub.9 ; R.sub.5 is R.sub.10, or --OR.sub.10 ; R.sub.6 and R.sub.7 are independently hydrogen, alkyl, or aryl; R.sub.8 and R.sub.9 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl; and R.sub.10 is alkoxy, alkyl, alkenyl, alkynl, or aryl.

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: 4942184 (1990-07-01), Haugwitz et al.
patent: 4960790 (1990-10-01), Stella et al.
patent: 5015744 (1991-05-01), Holton
patent: 5136060 (1992-08-01), Holton
patent: 5248796 (1993-09-01), Chen et al.
Denis and Greene, "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.
Holton, "Synthesis of the Taxane Ring System", J. Am. Chem. Soc., 1984, 106, pp. 5731-5732.
Mukerjee et al., ".beta.-Lactams: Retrospect and Prospect", Tetrahedron vol. 34, Report No. 52, pp. 1731-1767 (1978).
Wani et al., "Plant Antitumor Agents, VI. The Isolation and Structure of Taxol, a Novel Antileukemic and Antitumor Agent from Taxus Brevifolia", J. Am. Chem. Soc. 93:9, May 5, 1971, pp. 2325-2327.
Samaranayake et al., "Modified Taxols. 5.1 Reaction of Taxol with Electrophilic Reagents and Preparation of a Rearranged Taxol Derivative with Tubulin Assembly Activity 3.", J. Org. Chem. 1991, 56, 5114-5119.
Kaiser et al., "Synthesis of Esters of Acid-Unstable Alcohols by Means of n-butyllithium", J. Org. Chem., 1970, 35, 1198.
Ojima et al., "New and Efficient Approaches to the Semisynthesis of Taxol and its C-13 Side Chain Analogs by Means of .beta.-Lactam Synthon Method", Tetrahedron vol. 48, No. 34, pp. 6985-7012, 1992.

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