On February 14, 2008, McCormick, Kevin D.; Boyce, Christopher W.; Shih, Neng-Yang; Huang, Chia-Yu; Aslanian, Robert G.; Fevrier, Salem; Liang, Bo; Liu, Rong-Qiang; Liu, Ruiyan; Mangiaracina, Pietro; De Lera Ruiz, Manuel; Yu, Younong; Guise-Zawacki, Lisa; Zheng, Junying published a patent.SDS of cas: 50743-01-6 The title of the patent was Preparation of imidazolylmethylbenzoxazines and related compounds as α2c adrenoreceptor agonists.. And the patent contained the following:
Title compounds [I; A = (substituted) 5-membered heterocyclyl; X = O, S, SO, SO2, NR6; J1-J4 = N, NO, CR2; R2 = H, OH, halo, cyano, NO2, (substituted) alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, etc.; R3 = H, O, (substituted) alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, etc.; R4 = H, cyano, (substituted) alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, aryloxy, aralkyl, heteroaryl, heterocyclyl, etc.; R6 = H, (substituted) alkyl, alkoxy, alkenyl, alkenyloxy, cycloalkyl, aryl, aryloxy, aralkyl, heteroaryl, heterocyclyl, heterocyclylalkyl, etc.; m = 1-5; n = 1-3; p = 0-4; with provisos], were prepared Thus, 2,3-dihydro-1,4-benzoxazine was stirred with imidazole-4-carboxaldehyde, NaBH(OAc)3, and HOAc in dichloroethane at 60° overnight to give 50% title compound (II). II and other I showed α2c adrenoreceptor agonist activity at ≥30% Emax (GTPγS assay). The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).SDS of cas: 50743-01-6
The Article related to imidazolylmethylbenzoxazine preparation adrenoreceptor agonist, rhinitis nasal congestion pain diarrhea glaucoma treatment benzoxazine imidazolylmethyl, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.SDS of cas: 50743-01-6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem