92788-10-8Relevant articles and documents
Preparation of 2,6-dioxopiperidine derivatives
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, (2008/06/13)
3-Alkyl- or fluoroalkyl-3-(4-pyridyl)piperidine-2,6-diones, useful in the treatment of breast cancer, of formula STR1 wherein R represents an alkyl group having 2 to 10 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and A is hydrogen or an alkyl group having 1 to 4 carbon atoms, are prepared by reacting a 4-pyridylacetate with an alkyl or fluoroalkyl iodide, chloride or bromide, in the presence of a sterically bulky base and reacting the product with acrylamide in the presence of a sodium or potassium branched chain alkoxide. Preferably potassium t-butoxide is used in both stages and they are carried out sequentially at room temperature in an alcoholic or polar, aprotic solvent in a single reaction vessel.
A CONCISE SYNTHESIS OF RACEMIC PYRIDOGLUTETHIMIDE AND ITS RESOLUTION USING CHIRAL STATIONARY PHASE HPLC
Boss, Aileen M.,Clissold, Derek W.,Mann, John,Markson, Andrew J.,Thickitt, Christopher P.
, p. 6011 - 6017 (2007/10/02)
We describe a 'one-pot' synthesis of the aromatase inhibitor pyridoglutethimide and its 3-octyl-analogue, together with details of the resolution of the former using chiral stationary phase hplc.
Glutarimide derivatives for treating oestrogen-dependent tumors
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, (2008/06/13)
In the treatment of oestrogen-dependent tumors, it is desirable to improve the therapy obtainable from the compound aminoglutethimide. It has now been found that 3-ethyl-3-(4-pyridyl)glutarimide derivatives of formula STR1 wherein: (a) R1 represents an ethyl group and R2 represents a methyl group, an alkyl or cycloalkyl group having 3 to 10 carbon atoms, or a fluoroalkyl group having 2 to 10 carbon atoms; (b) R1 represents an alkyl group having 3 to 10 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and R2 represents a hydrogen atom; or, (c) R1 represents an alkyl group having 3 to 8 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and R2 represents an alkyl or fluoroalkyl group having 2 to 8 carbon atoms, provided that the total number of carbon atoms in R1 and R2 is not more than 10; and therapeutically acceptable acid addition salts of the above compounds.