Synthesis of [2.2]Paracyclophane-Fused Heterocycles via Palladium-Catalyzed C-H Activation/Annulation of [2.2]Paracyclophanecarboxamides with Arynes.

[2.2]Paracyclophane-fused heterocycles represent an important scaffold. Traditional approaches often suffer from tedious synthetic routes, and the development of catalytic synthesis of them remains in its infancy.

A low-nuclear Ag nanocluster as a customized catalyst for the cyclization of propargylamine with CO.

The preparation of 2-Oxazolidinones using CO offers opportunities for green chemistry, but multi-site activation is difficult for most catalysts. Here, A low-nuclear Ag catalytic system is successfully customized, which solves the simultaneous activation of acetylene (-C≡C) and amino (-NH-) and realizes the cyclization of propargylamine with CO under mild conditions. As expected, the Turnover Number (TON) and Turnover Frequency (TOF) values of the Ag nanocluster (NC) are higher than most of reported catalysts.

Novel substituted 4-(Arylethynyl)-Pyrrolo[2,3-d]pyrimidines negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGlu5) Treat depressive disorder in mice.

In view of the fact that the G-protein-coupled receptors (GPCRs) sit at the top of the signaling pathways triggering a diverse range of signaling cascades towards a cellular event, GPCRs are regarded as central drug targets. mGlu5, a type of classical GPCRs, is highly expressed in the central nervous system (CNS) and responds to the neurotransmitter glutamate. Researches show that mGlu5 is a potential drug target for the treatment of depression.

Construction of highly enantioenriched spirocyclopentaneoxindoles containing four consecutive stereocenters via thiourea-catalyzed asymmetric Michael-Henry cascade reactions.

The thiourea-catalyzed asymmetric synthesis of highly enantioenriched spirocyclopentaneoxindoles containing chiral amide functional groups using simple 3-substituted oxindoles and nitrovinylacetamide as starting materials was achieved successfully. This protocol features operational simplicity, high atom economy, and high catalytic asymmetry, thus representing a versatile approach to the synthesis of highly enantioenriched spirocyclopentaneoxindoles.

Enantioselective Assembly of Spirolactones through NHC-Catalyzed Remote γ-Carbon Addition of Enals with Isatins.

A chiral N-heterocyclic carbene (NHC)-catalyzed formal [4 + 2] annulation of β-methyl substituted enals with isatins was developed to construct six-membered spirolactones bearing highly congested quaternary carbon stereocentersin good yields and high enantioselectivities. The strategy realized a challenging remote γ-carbon addition of enals and chiral control of β-methyl substituted enals in the presence of the NHC catalyst only.