Base-Promoted 1,4-Difunctionalization of [60]Fullerene with H-Phosphonates and Alkyl Bromides.

The DBU-promoted three-component coupling reaction of H-phosphonates, [60]fullerene, and alkyl bromides has been developed as a facile and efficient protocol for the one-pot synthesis of various 1,4-(phosphonyl)(organo)[60]fullerenes. This method exhibits high regioselectivity at the 1,4-position on the [60]fullerene core and features a metal-free nature, easy operation, low cost, and a wide range of substrates.

Inflammatory brain lesions preceding primary central nervous system lymphoma: a case report and genetic analysis.

Background: Primary central nervous system lymphoma (PCNSL) is an aggressive extranodal lymphoma exclusively occurring within the central nervous system. Inflammatory brain lesions as "sentinel lesions" of PCNSL are very rare. We present a rare case of PCNSL with preceding inflammatory lesions in an immunocompetent patient who underwent two biopsies, one craniotomy and two genetic testing.

Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy.

Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class B G protein-coupled receptor and a drug target for the treatment of neuronal, metabolic, and inflammatory diseases. However, our understanding of its mechanism of action and the potential of drug discovery targeting this receptor is limited by the lack of structural information of VIP1R. Here we report a cryo-electron microscopy structure of human VIP1R bound to PACAP27 and Gs heterotrimer, whose complex assembly is stabilized by a NanoBiT tethering strategy.

Anticancer-Active N-Heteroaryl Amines Syntheses: Nucleophilic Amination of N-Heteroaryl Alkyl Ethers with Amines.

A mild amination protocol of N-heteroaryl alkyl ethers with various amines is described. This transformation is achieved by utilizing simple and readily available base as promoter via C-O bond cleavage, offering a new amination strategy to access several anticancer-active compounds. This work is highlighted by the excellent functional group compatibility, scalability, wide substrate scope, and easy derivatization of a variety of drugs.