887581-09-1Relevant articles and documents
Synthesis of a unique isoindoline/tetrahydroisoquinoline-based tricyclic sultam library utilizing a Heck-aza-Michael strategy
Zang, Qin,Javed, Salim,Porubsky, Patrick,Ullah, Farman,Neuenswander, Benjamin,Lushington, Gerald H.,Basha, Fatima Z.,Organ, Michael G.,Hanson, Paul R.
body text, p. 211 - 217 (2012/05/19)
The synthesis of a unique isoindoline- and tetrahydroisoquinoline (THIQ)-containing tricyclic sultam library, utilizing a Heck-aza-Michael (HaM) strategy is reported. Both isoindoline and THIQ rings are installed through a Heck reaction on a vinylsulfonamide, followed by one-pot deprotection and intramolecular aza-Michael reaction. Subsequent cyclization with either paraformaldehyde condensation or 1,1′-carbonyldiimidazole coupling generates a variety of tricyclic sultams. Overall, a 160-member library of these sultams, together with their isoindolines/THIQ and secondary sulfonamides precursors, were constructed using this strategy.
MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 75-76, (2010/08/07)
The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
An efficient preparation of N-alkyl-2-benzazepine derivatives and investigation of their biological activity
Kamimura, Akio,So, Masahiro,Kuratani, Tomohiro,Matsuura, Kenji,Inui, Makoto
scheme or table, p. 3193 - 3195 (2010/03/31)
N-Alkyl-2-benzazepine derivatives are readily prepared through N-alkylation of secondary 2-benzazepines that are constructed via 7-endo selective cyclization of radical cyclization of N-boc-N-(2-bromo-5-methoxyphenylmethyl) methacrylamides. The structure