927671-03-2Relevant articles and documents
Rapid synthesis of pomalidomide-conjugates for the development of protein degrader libraries
Brownsey, Duncan K.,Rowley, Ben C.,Gorobets, Evgueni,Gelfand, Benjamin S.,Derksen, Darren J.
, p. 4519 - 4525 (2021)
Current methods for the preparation of heterobifunctional pomalidomide-conjugates rely on methods that are often low yielding and produce intractable byproducts. Herein we describe our strategy for the reliable and succinct preparation of pomalidomide-linkers which is essential to the formation of these conjugates. We present the preparation of 18 pomalidomide-linkers in high yield compared to current literature methods. Our findings show that secondary amines consistently afford greater yields than their primary counterparts, a trend that we were able to exploit in the synthesis of several new pomalidomide homo-dimers in enhanced yields compared to similar literature syntheses. This trend was further utilised to develop the first one-pot synthesis of JQ1-pomalidomide conjugates in yields up to 62%, providing a method that is suited to rapid preparation of conjugate libraries as is frequently required for the development of new protein degraders.
Isoindole-imide compounds and compositions comprising and methods of using the same
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Page/Page column 75, (2010/11/26)
This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.