40243-87-6Relevant articles and documents
Antibody-catalyzed enantioselective Norrish type II cyclization
Saphier, Sigal,Sinha, Subhash C.,Keinan, Ehud
, p. 1378 - 1381 (2003)
Excellent enantioselectivity (up to 96% ee) was attained in an antibodycatalyzed photochemical Norrish type II reaction, which proceeded via the intermediate diradical 1 to produce the cyclobutanols 4 (absolute stereochemistry unknown). Use of the antibod
Functionalized styrene synthesis via palladium-catalyzed C[sbnd]C cleavage of aryl ketones
Zhang, Xu,Wang, Zhen-Yu,Wang, Xing,Xu, Hui,Dai, Hui-Xiong
, (2022/03/31)
We report herein the synthesis of functionalized styrenes via palladium-catalyzed Suzuki–Miyaura cross-coupling reaction between aryl ketone derivatives and potassium vinyltrifluoroborate. The employment of pyridine-oxazoline ligand was the key to the cleavage of unstrained C[sbnd]C bond. A variety of functional groups and biologically important moleculars were well tolerated. The orthogonal Suzuki–Miyaura coupling demonstrated the synthetic practicability.
Design of Negative and Positive Allosteric Modulators of the Cannabinoid CB2Receptor Derived from the Natural Product Cannabidiol
Navarro, Gemma,Gonzalez, Angel,Sánchez-Morales, Adrià,Casajuana-Martin, Nil,Gómez-Ventura, Marc,Cordomí, Arnau,Busqué, Félix,Alibés, Ramon,Pardo, Leonardo,Franco, Rafael
, p. 9354 - 9364 (2021/07/19)
Cannabidiol (CBD), the second most abundant of the active compounds found in the Cannabis sativa plant, is of increasing interest because it is approved for human use and is neither euphorizing nor addictive. Here, we design and synthesize novel compounds taking into account that CBD is both a partial agonist, when it binds to the orthosteric site, and a negative allosteric modulator, when it binds to the allosteric site of the cannabinoid CB2 receptor. Molecular dynamic simulations and site-directed mutagenesis studies have identified the allosteric site near the receptor entrance. This knowledge has permitted to perform structure-guided design of negative and positive allosteric modulators of the CB2 receptor with potential therapeutic utility.