Iodine(III)-Mediated Photochemical C-H Azolation.

A systematic radical polarity analysis framework is formulated herein for the projection of radical reactivity patterns. An iodine(III)-mediated photochemical C-H azolation reaction has been envisaged and developed based on the set of empirical guidelines. The synthesis features an environmentally benign reagent, mild reaction conditions, an operationally simple protocol, and a broad substrate scope.

Manganese-Catalyzed Cycloalkene Ring Expansion Synthesis of Azaheterocycles.

Herein, a Mn catalytic protocol has been developed for the cycloalkene ring expansion synthesis of azaheterocycles, allowing broad-substrate-scope access to pyridine and isoquinoline derivatives. The initial monoaddition of an azidyl radical to alkene and further as-generated C-radical addition to O, followed by intramolecular rearrangement and aromatization, showcase a distinct Mn-catalyzed radical reactivity mode. The reaction features a short reaction time and a broad substrate scope, with applications demonstrated in complex structure elaboration and gram-scale vismodegib synthesis.

Co(III)-Catalyzed Coupling of Enaminones with Oxadiazolones for Imidazole Synthesis.

Appendage speciation-oriented synthesis, as opposed to the conventional wisdom of skeleton speciation-oriented synthesis, is reported herein, emphasizing the maximization of type-, position-, and configuration-variance of appendages. A Co(III) catalytic protocol in accordance with this synthetic modality has been established for the coupling of enaminones and oxadiazolones to imidazoles, allowing the achievement of full position-variance of appendages. This translates to an expanded reaction and structural development scope and can provide fertile ground for productive organic synthesis.

Synthesis of quinazolinones Cp*Co(III)-catalyzed C-H functionalization of primary amides with oxadiazolones.

Multi-heteroatom heterocycle synthesis through direct C-H bond activation is methodologically appealing but synthetically challenging. An efficient double C-N bond formation sequence to prepare quinazolinones utilizing primary amides and oxadiazolones in a catalytic redox-neutral [CoCp*(CO)I]/AgSbF system, where oxadiazolone could function as an internal oxidant to maintain the catalytic cycle, is reported. Amide-directed C-H bond activation and oxadiazolone decarboxylation are key to the success of this traceless, atom- and step-economic, and cascade approach for the construction of the quinazolinone skeleton.

Effect of Thermal Oxygen Aging Mode on Rheological Properties and Compatibility of Lignin-Modified Asphalt Binder by Dynamic Shear Rheometer.

Lignin is abundant in nature. The use of lignin in the asphalt pavement industry can improve pavement performance while effectively optimizing pavement construction costs. The purpose of this paper is to study the effect of lignin on the anti-aging properties of asphalt.

Synthesis of 5-Chromeno[2,3-]pyrimidin-5-one Derivatives via Microwave-Promoted Multicomponent Reaction.

A microwave-promoted multicomponent reaction of 3-formylchromones, amines, and paraformaldehyde was achieved under catalyst-free and solvent-free conditions, delivering 5-chromeno[2,3-]pyrimidin-5-one derivatives in good to excellent yields via an unexpected annulation pathway, which further expanded the synthetic application of paraformaldehyde as a C1 building block.

Iodine(III) promotes cross-dehydrogenative coupling of N-hydroxyphthalimide and unactivated C(sp)-H bonds.

Cross-dehydrogenative coupling reactions provide a method to construct new chemical bonds by direct C-H activation without any pre-functionalization. Compared to functionalization of a C-H bond α- to ether oxygen, α- to carbonyl, or at a benzylic position, functionalization of unactivated hydrocarbons is difficult and often requires high temperatures, a transition-metal catalyst, or a superstoichiometric quantity of volatile, toxic, and explosive tert-butylhydroperoxide. Here, a cross-dehydrogenative C-O coupling reaction of N-hydroxyphthalimide with unactivated alkanes, nitriles, ethers, and thioethers has been realized by using iodobenzene diacetate as the radical initiator.

Design, synthesis and anticancer activity of naphthoquinone derivatives.

Basis on molecular docking and pharmacophore analysis of naphthoquinone moiety, a total of 23 compounds were designed and synthesised. With the help of reverse targets searching, anti-cancer activity was preliminarily evaluated, most of them are effective against some tumour cells, especially compound : 1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl-4-oxo-4-((4-phenoxyphenyl)amino) butanoate whose IC against SGC-7901 was 4.1 ± 2.