On December 2, 2021, Bartolozzi, Alessandra; Proudfoot, John Robert; Briggs, Timothy; Mancuso, John; Bos, Maxence; Guo, Tianlin; Ly, Vu Linh; Blois, Anna; Lanter, Bernard; Taylor, Steven John; Buckbinder, Leonard published a patent.Synthetic Route of 1820711-82-7 The title of the patent was Synthesis of fused azole heterocycles as AHR antagonists treating cancers. And the patent contained the following:
The synthesis of fused azole heterocycles, I, wherein the dashed bonds can be independently single or double bonds; X can selectively be N, S,CH, or NH depending on bond arrangements; Y can independently be N or CH as it relates to the fused azole; ring A and B are chosen from optionally substituted aryl, heteraryl, cycloalkyl or heterocycloalky moieties; and L is chosen from a bond and -NT-C(O)-, wherein T can be H or Me are presented as pharmaceutically acceptable salts for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling. Of note, II was synthesized and demonstrated an HEPG2 Luc IC50 of less than 100 nM; an aqueous solubility of less than 0.1μM at pH 7/4; and a human hepatocyte clearance of between 20 and 50 mL/min/Kg. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Synthetic Route of 1820711-82-7
The Article related to fused azole heterocycle ahr antagonist anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1820711-82-7