14529-54-5Relevant articles and documents
Iridium-Catalysed C-H Borylation of 2-Pyridones; Bisfunctionalisation of CC4
Honraedt, Aurélien,Niwetmarin, Worawat,Gotti, Cecilia,Campello, Hugo Rego,Gallagher, Timothy
, p. 3420 - 3429 (2018)
The high regioselectivity associated with the iridium-catalysed borylation of pyridones has been exploited to provide a very direct and efficient entry to C(10) doubly substituted CC4 variants of cytisine. Two approaches have been evaluated based on (i) C-H activation of cytisine (or an N-substituted derivative) followed by N-alkylation (to enable dimer formation) and (ii) direct C-H activation and borylation of CC4 itself. Both approaches provide access to C(10)-functionalized CC4 derivatives, but direct borylation of CC4 allows for a wider range of functional group interconversions to be tolerated.
PROCESS FOR PREPARING BTK INHIBITORS
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Paragraph 0224-0225, (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.
An expeditious copper-catalyzed access to 3-aminoquinolinones, 3-aminocoumarins and anilines using sodium azide
Messaoudi, Samir,Brion, Jean-Daniel,Alami, Mouad
experimental part, p. 1677 - 1687 (2010/10/01)
An efficient copper-catalyzedin in situ C-(sp2)-NH2 bond formation to provide a range of 3-aminoquinolin-2(1H)-ones and 3-aminocoumarins from 3-bromoquinolinones and 3-bromocoumarins, respectively, has been achieved. The reaction conditions involve the use of copper powder as the catalyst, eco-friendly ethanol as the solvent in the pres ence of pipecolinic acid as the ligand and ascorbic acid as the additive. The efficiency of this practical method was demonstrated in the synthesis of various anilines.