195252-56-3Relevant articles and documents
Projected Dose Optimization of Amino- And Hydroxypyrrolidine Purine PI3KδImmunomodulators
Methot, Joey L.,Zhou, Hua,McGowan, Meredeth A.,Anthony, Neville John,Christopher, Matthew,Garcia, Yudith,Achab, Abdelghani,Lipford, Kathryn,Trotter, Benjamin Wesley,Altman, Michael D.,Fradera, Xavier,Lesburg, Charles A.,Li, Chaomin,Alves, Stephen,Chappell, Craig P.,Jain, Renu,Mangado, Ruban,Pinheiro, Elaine,Williams, Sybill M. G.,Goldenblatt, Peter,Hill, Armetta,Shaffer, Lynsey,Chen, Dapeng,Tong, Vincent,McLeod, Robbie L.,Lee, Hyun-Hee,Yu, Hongshi,Shah, Sanjiv,Katz, Jason D.
, p. 5137 - 5156 (2021/05/04)
The approvals of idelalisib and duvelisib have validated PI3Kδinhibitors for the treatment for hematological malignancies driven by the PI3K/AKT pathway. Our program led to the identification of structurally distinct heterocycloalkyl purine inhibitors wit
A One-Pot Synthesis of Highly Functionalized Purines
Zelli, Renaud,Zeinyeh, Wa?l,Haudecoeur, Romain,Alliot, Julien,Boucherle, Benjamin,Callebaut, Isabelle,Décout, Jean-Luc
supporting information, p. 6360 - 6363 (2017/12/08)
Highly substituted purines were synthesized in good to high yields through a one-pot straightforward metal-free scalable method, using the Traube synthesis adapted to Vilsmeier-type reagents. From 5-amino-4-chloropyrimidines, new 9-aryl-substituted chloropurines and intermediates for peptide nucleic acid synthesis were prepared. Variant procedures allowing a rapid synthesis of ribonucleosides and 7-benzylpurine from 5-amidino-6-aminopyrimidines are also reported to illustrate the high potential of this versatile toolbox. This route appears to be particularly interesting in the field of nucleic acids for a direct and rapid access to various new 8-alkylpurine nucleosides.
An efficient one-pot synthesis of 6-alkoxy-8,9-dialkylpurines via reaction of 5-amino-4-chloro-6-alkylaminopyrimidines with N,N-dimethylalkaneamides and alkoxide ions
Baraldi, Pier Giovanni,Broceta, Asier Unciti,Infantas, Maria Josè Pineda De Las,Mochun, Juan Josè Dìaz,Espinosa, Antonio,Romagnoli, Romeo
, p. 7607 - 7611 (2007/10/03)
The synthesis of a number of new 6-alkoxy-8,9-(disubstituted)purines has been accomplished by the cyclization of the corresponding intermediate 5-amino-4-chloro-6-(alkylamino)pyrimidines promoted by alkoxides and various N,N-dimethyl amides, where the latter act as solvent-reagents. By this three-component condensation reaction we are able to introduce an alkyl group in the 8 position of the purine ring with the concomitant nucleophilic replacement of the 6-chloro group with an alkoxy moiety.
