134031-24-6Relevant articles and documents
Reactivity and regioselectivity in Stille couplings of 3-substituted 2,4-dichloropyridines
Khoje, Abhijit Datta,Gundersen, Lise-Lotte
, p. 523 - 525 (2011)
The influence of substituents at C-3 of 2,4-dichloropyridines on their reactivity and regioselectivity in Pd-catalyzed cross-couplings is studied. As a model reaction, the (Ph3P)2PdCl2-catalyzed Stille coupling between 2-furyl(tributyl)tin and pyridines is chosen. Increased electron-withdrawing ability of a substituent at the pyridine 3-position improves the overall reactivity. Absolute selectivity for coupling at C-2 is achieved with an amino group at C-3, and the selectivity is totally reversed when the amino group is exchanged for a nitro substituent.
PROCESS FOR PREPARING BTK INHIBITORS
-
Paragraph 0286-0297, (2018/07/05)
Methods for preparing the Bruton's Tyrosine Kinase ("BTK") inhibitor compound 2- {3'-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2- ylamino]-6-oxo-1,6-dihydro-[3,4']bipyridinyl-2'-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H- cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
-
Paragraph 0402, (2015/05/05)
The present application discloses compounds that are inhibitors of Btk, compounds that are inhibitors of ΡΒΚδ, and compounds that are dual inhibitors of both Btk and PI3Kδ. Also described are methods for synthesizing such inhibitors and methods for using such inhibitors for the treatment of diseases wherein inhibition of Btk and PI3Kδ provides a therapeutic benefit to a patient having the disease.
