1174303-95-7Relevant articles and documents
Development of scalable syntheses of selective PI3K inhibitors
Huang, Qinhua,Richardson, Paul F.,Sach, Neal W.,Zhu, Jinjiang,Liu, Kevin K.-C.,Smith, Graham L.,Bowles, Daniel M.
, p. 556 - 564 (2011/12/02)
On the basis of a more practical and scalable route to an iodothiophene, an efficient and reliable synthesis has been developed for three selective PI3K inhibitors. From this advanced intermediate, the three title compounds were each prepared in five additional steps. Key learnings also include: high throughput experimentation (HTE) screening toward a more robust Suzuki coupling, a more efficient triazole synthesis, and an acid/base cleanup developed to purify the final compounds. The final enabled synthesis required no column chromatography.
THIOPHENES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE (PI3K) INHIBITORS
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Page/Page column 43-44, (2009/09/05)
This invention provides thiophene compounds of formula (I) : wherein R1, R2, R3, R4, n, p, and m are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
