Intermediates for preparation of taxols

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United States of America Patent

PATENT NO 5274137
SERIAL NO

07902390

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A taxol intermediate selected from the group consisting of: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each selected from hydrogen, hydroxyl, or a protected hydroxyl; or R.sup.1 and R.sup.2 together form an oxo or a protected oxo; R.sup.3 is formyl, a protected formyl, or --CH(X)--OY wherein X is hydrogen or a monovalent metal and Y is hydrogen or a hydroxyl protecting group; and R.sup.4 and R.sup.5 are different and each selected from chloro or cyano; or R.sup.4 and R.sup.5 together form an oxo or a protected oxo, with the proviso that R.sup.1 and R.sup.2 are not both hydroxyl; R.sup.6 is hydroxyl or a protected hydroxyl; R.sup.7 is hydrogen, hydroxyl, or a protected hydroxyl; R.sup.8 is carboxyl, hydroxylmethyl, or a protected hydroxylmethyl; or R.sup.7 and R.sup.8 when taken together with carbon atoms 3 and 4, form an oxetane ring; or R.sup.6 and R.sup.8 when taken together with carbon atoms 1 and 4, form a bridged lactone; R.sup.9 is hydrogen or a hydroxyl protecting group; R.sup. 10 is hydroxyl or a protected hydroxyl; or R.sup.8 and R.sup.10 when taken together with carbon atoms 4 and 5, form a .gamma.-butyrolactone ring; R.sup.11 is alkoxycarbonyl, formyl, a protected formyl, hydroxylmethyl or a protected hydroxylmethyl; or R.sup.6 and R.sup.11 when taken together with carbon atoms 1 and 6, form a 2,2-dimethyl-1,3-dioxane ring; and the dotted line between the 2- and 3-positions of the six-membered ring represents an optional bond.

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Patent Owner(s)

Patent OwnerAddress
SCRIPPS RESEARCH INSTITUTE THE10666 NORTH TORREY PINES ROAD LA JOLLA 92307 CA UNITED STATES OF AMERICA

International Classification(s)

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Hwang, Chan-Kou 5035 Camino Playa Malaga, San Diego, CA 92124 21 373
Liu, Jin-Jun 9528 Poole St., La Jolla, CA 92037 37 500
Nicolaou, K C 9625 Blackgold Rd., La Jolla, CA 92037 15 306
Sorensen, Erik J 3959-C Miramar St., La Jolla, CA 92037 25 387

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