937046-98-5Relevant articles and documents
Regioselective mono-bromination of pyrrolo[2,1-f][1,2,4]triazin-4-amine
Bi, Lei,Fang, Sheng,Zhang, Ran,Yin, Xianzhen,Fu, Chenchao,Yao, Lei
, p. 7083 - 7084 (2014)
Pyrrolo[2,1-f][1,2,4]triazin-4-amine is regioselectively brominated when treated with 1,3-dibromo-5,5-dimethylimidazolidine-2,4-dione in different solvents. The brominated product, 5,7-dibromopyrrolo[2,1-f][1,2,4]triazin-4-amine predominates when the reaction is run in dichloromethane. The subsequent debromination process utilizes lithium-bromine exchange to give the desired product 5-bromo-pyrrolo[2,1- f][1,2,4]triazin-4-amine.
Preparation method 7-bromopyrrolo [2,1-f][1, 2, 4]-thiazine -4- amine (by machine translation)
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, (2020/03/12)
[, ] The preparation method 7 - of [2,1 - f][1, 2, 4]-(, amino - ((((((((aopipelineao :1) aminopyrrolo 2,5 - thiopyrrole I,) obtained by reacting the intermediate 1 - Boc - 1 - with the formamidine in the following step ;2) can obtain the intermediate I (II, amino-(EC 1 - Boc - 1 -) to obtain the intermediate ;3), namely, II amino-(III, aminopyrrolopyrrole - 2 2-methanonitrile hydrochloride 1 -) to form the intermediate ;4) through the reaction of the intermediates III and the bromination reagent to obtain a final product IV, of the present invention. in an acidic condition and reacting the intermediate body with the bromination reagent. to obtain a final product (4 -aminopyrrolopyridine - 4 4) intermediate, [2,1 - f][1, 2, 4] [2,1 - f][1, 2, 4] obtained by the reaction of the intermediate body with the. bromination reagent and ;5) amino- pyrrolidine. IV-amine,aminopyrroyl hydrochloride 7 . (by machine translation)
Development of 4-Heteroarylamino-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octanes] as α7 Nicotinic Receptor Agonists
Hill, Matthew D.,Fang, Haiquan,King, H. Dalton,Iwuagwu, Christiana I.,McDonald, Ivar M.,Cook, James,Zusi, F. Christopher,Mate, Robert A.,Knox, Ronald J.,Post-Munson, Debra,Easton, Amy,Miller, Regina,Lentz, Kimberley,Clarke, Wendy,Benitex, Yulia,Lodge, Nicholas,Zaczek, Robert,Denton, Rex,Morgan, Daniel,Bristow, Linda,Macor, John E.,Olson, Richard
supporting information, p. 133 - 137 (2017/12/12)
We describe the synthesis of quinuclidine-containing spiroimidates and their utility as α7 nicotinic acetylcholine receptor (nAChR) partial agonists. A convergent synthetic route allowed for rapid SAR investigation and provided a diverse set of fused 6,5-heteroaryl analogs. Two potent and selective α7 nAChR partial agonists, (1′S,3′R,4′S)-N-(7-bromopyrrolo[2,1-f ][1,2,4]triazin-4-yl)-4H-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octan]-2-amine (20) and (1′S,3′R,4′S)-N-(7-chloropyrrolo[2,1-f ][1,2,4]triazin-4-yl)-4H-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octan]-2-amine (21), were identified. Both agonists improved cognition in a preclinical rodent model of learning and memory. Additionally, 5-HT3A receptor SAR suggested the presence of a steric site that when engaged led to significant loss of affinity at that receptor.