Straightforward Synthesis of Halopyridine Aldehydes via Diaminomethylation.

A novel two-step method for formylation of fluoropyridines with silylformamidine Me SiC(=NMe)NMe (1) under catalyst-free conditions was developed. A series of all possible 18 fluoropyridines featuring one to four fluorine atoms were subjected to the reaction with 1 existing in equilibrium with its carbenic form Me NC(:)N(Me)SiMe (1'). Among them, 12 fluoropyridines were shown to react via C-H insertion.

Latent Carbene in Diaminomethylation of Benzenes: Mechanism and Practical Application.

Silylformamidine exists in equilibrium with its carbenic form due to an easy migration of the silyl group. The reaction of with variously substituted fluorobenzenes proceeds as an insertion of the nucleophilic carbene into the most acidic C-H bond upon mixing the reagents and does not require any catalyst. According to DFT calculations, the classical interpretation of the insertion reaction proceeding via a three-membered transition state structure requires high activation energy.

Cytotoxic and immunomodulatory potential of a novel [2-(4-(2,5-dimethyl-1H-pyrrol-1-yl)-1H-pyrazol-3-yl)pyridine] in myeloid leukemia.

Cancer ranks among the leading causes of mortality worldwide. However, the efficacy of commercially available anticancer drugs is compromised by the emerging challenge of drug resistance. This study aimed to investigate the anticancer and immunomodulatory potential of a recently developed a novel [2-(4-(2,5-dimethyl-1 H-pyrrol-1-yl)- 1 H-pyrazol-3-yl) pyridine].