35256-74-7Relevant academic research and scientific papers
Development of a Scalable and Practical Synthesis of AB928, a Dual A2a/A2bReceptor Antagonist
Debien, Laurent P. P.,Jeffrey, Jenna L.,Leleti, Manmohan R.,Miles, Dillon H.,Powers, Jay P.,Rosen, Brandon R.,Sharif, Ehesan U.
, p. 1254 - 1261 (2020/08/14)
AB928 is a potent and selective dual antagonist of the A2a and A2b receptors, which is currently in clinical trials. Here, we report the development of two scalable and practical syntheses of AB928. The first-generation synthesis was used to successfully
PROCESSES FOR PREPARING AMINOPYRIMIDINE COMPOUNDS
-
, (2020/12/29)
Provided herein are improved processes for preparing aminopyrimidine compounds of Formula (I). The disclosed processes advantageously proceed through a β-diketoester intermediate of Formula (A) and avoid the direct linking of a pyrimidine and phenyl moiet
Improved synthesis of sterically encumbered heteroaromatic biaryls from aromatic β-keto esters
Rosen, Brandon R.,Ul Sharif, Ehesan,Miles, Dillon H.,Chan, Nicholas S.,Leleti, Manmohan R.,Powers, Jay P.
supporting information, (2020/03/25)
A protocol for the synthesis of hindered 4-aryl 2-aminopyrimidines from β–keto esters is described. The process employs trifluoroethanol as an essential additive to promote the guanidine condensation reaction, enabling the synthesis of 25 aryl- and heteroaryl substituted aminopyrimidines in good yields and high purities with no column chromatography. The conditions described herein are readily scalable and have been employed in the large-scale synthesis of the clinical A2a/A2bR antagonist AB928.
