发明名称 Process of preparing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-yl)pyridin-2-amine
摘要 The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:;
申请公布号 US9464083(B2) 申请公布日期 2016.10.11
申请号 US201514666694 申请日期 2015.03.24
申请人 ArQule Inc. 发明人 Bates Craig;Chen Jian-Xie;Mao Jianmin;Reed David P.
分类号 C07D471/04;C07D213/74 主分类号 C07D471/04
代理机构 Cooley LLP 代理人 Cooley LLP ;Elrifi Ivor R.;Pavao Matthew
主权项 1. A process of preparing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine, comprising the steps of Step 3, reacting tert-butyl (1-(4-((3-amino-6-phenylpyridin-2-yl)amino)phenyl)cyclobutyl)carbamate with 2-amino nicotinaldehyde in the presence of an oxidant and an acid in a polar protic solvent to form tert-butyl (1-(4-(2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl)phenyl)cyclobutyl)carbamate; and Step 4, treating tert-butyl (1-(4-(2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl)phenyl)cyclobutyl)carbamate with an acid in a polar aprotic solvent to form 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine.
地址 Burlington MA US