Glaxo Wellcome Inc.

Osi Pharmaceuticals, Inc.

Other

Smithkline Beecham Corporation

North Carolina State University

Gilead Sciences, Inc.

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Francis Gerard Fang

Daniel L Comins

Edward McDonald Huie

Melissa Williams Lowery

Suzanne Elaine Keeling

Chuen Chan

Brian Cox

Alison Judith Redgrave

David George Allen

Richard Peter Charles Cousins

Heather Hobbs

Joanna Victoria Geden

Thomas Davis Roper, Iv

The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I&prime;) known by the chemical name &ldquo;7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin&rdquo;, which comprises cyclising the compound of formula (II&prime;), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I&prime;) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I&prime;) or a salt thereof into a physiologically acceptable salt or solvate thereof.

Preparation of a camptothecin derivative by intramolecular cyclisation

Method for preparing camptothecin derivatives

A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2 receptor are described.

2-(Purin -9-yl)-tetrahydrofuran-3,4-diol derivatives

Preparation of a camptothecin derivative by intramolecular cyclization

The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation,

Method of removing heavy metal contaminants from organic compounds

A process of providing novel compounds of Formula (I) below, which are useful as intermediates in the preparation of camptothecin and camptothecin-like compounds, ##STR1## wherein: R.sup.1 represents alkyl, particularly methyl, R.sup.2 represents H or alkyl, particularly methyl, R3 represents H or alkyl, particularly H; Q represents triflate or halo particularly bromo and iodo more particularly iodo and Y represents H, chloro or OR.sup.4, wherein R.sup.4 represents alkyl or triflate, or particularly H.

Intermediates in pharmaceutical camptothecin preparation

Growing community of inventors

Cary, NC, United States of America

Shiping Xie