NAPHTHALENE-2-CARBOXAMIDINE synthesis

Yield:5651-14-9 83 %

Reaction Conditions:

with ammonia in methanol;ethanol at 20;

Steps:

2-substitued-2-aryl-imidamide (5a)

General procedure: Compounds 4a (4.25 mmol) and 4.25 ml of 7 N ammonia in methanol were stirred in 4.25 ml of ethanol at ambient temperature for 12 hours. After compounds 4a disappeared by TLC, they were concentrated in vacuo. The mixture was diluted with ether and stirred until the product isolated as a solid. The solid product was filtered off and washed with ether and then hexanes. The crude product was then crystallized to give 5a as a white solid (81%)

References:

Jun, Joonhong;Yang, Songyi;Lee, Junghun;Moon, Hyungwoo;Kim, Jinwoong;Jung, Hoyong;Im, Daseul;Oh, Youri;Jang, Miyoung;Cho, Hyunwook;Baek, Jihyun;Kim, Hyejin;Kang, Dahyun;Bae, Hyunah;Tak, Chanwool;Hwang, Kyungrim;Kwon, Hoseok;Kim, HyunTae;Hah, Jung-Mi [European Journal of Medicinal Chemistry,2023,vol. 245,art. no. 114894] Location in patent:supporting information