Identification of parallel medicinal chemistry protocols to expand branched amine design space was written by Conn, Edward L.;Perry, Matthew A.;Shi, Kecheng;Wang, Guotao;Hoy, Susan;Sach, Neal W.;Qi, Wenying;Qu, Liqiang;Gao, Yu;Xu, Yan;Schmitt, Daniel C.. And the article was included in Organic & Biomolecular Chemistry in 2022.Product Details of 25676-75-9 This article mentions the following:
Methods for the synthesis of 伪-branched heteroaryl amines RCH(R1)NH(R2) (R = tert-Bu, Ph, 1-methyl-1H-imidazol-4-yl, pyridin-2-yl, etc. R1 = 1-methyl-1H-pyrazol-5-yl, pyridin-3-yl, 1-propyl-1H-pyrazol-4-yl, 4-bromo-2-hydroxyphenyl, etc.; R2 = pyridin-2-yl, Ph, 4-phenylpyridin-2-yl, pyrazin-2-yl, etc.) via aldimine addition have been evaluated for compatibility with parallel synthesis. In situ activation of aliphatic carboxylic acids RC(O)OH as redox-active esters enables Zn-mediated decarboxylative radical imine R1CH=NR2 addition to access aliphatic-branched heterobenzylic amines. In situ activation of (hetero)aryl bromides RBr via Li-halogen exchange enables heteroaryl-lithium addition to imines to access (hetero)benzhydryl amines. Condensation of heteroaryl amines RNH2 with heteroaryl aldehydes R1CHO provides aldimines which may be intercepted with aryl Grignard reagents to provide modular access to (hetero)benzhydryl amines. These protocols minimize synthetic step count and maximize accessible design space, enhancing access to 伪-branched heteroaryl amines for medicinal chem. In the experiment, the researchers used many compounds, for example, 4-Bromo-1-methylimidazole (cas: 25676-75-9Product Details of 25676-75-9).
4-Bromo-1-methylimidazole (cas: 25676-75-9) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3鈥揅6) is higher than in water and generally decreases with a Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Product Details of 25676-75-9
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem