Palladium-catalyzed cascade cyclization of α,β-unsaturated -tosylhydrazones with iodoarenes: access to 2-chromenes and 2-quinolines.

A palladium-catalyzed cascade reaction of α,β-unsaturated -tosylhydrazones with iodoarene derivatives containing a nucleophilic group has been developed, which provides facile access to 2-chromenes and 2-quinolines, respectively. Additionally, the double Pd-carbene migratory insertion/nucleophilic substitution processes for the synthesis of a ternary heterocyclic skeleton were possible in the developed catalytic system.

Pd-Catalyzed Cascade Cyclization/Thiocarbonylation with Thioformates: Synthesis of Thioester-Functionalized Oxindoles.

A Pd-catalyzed thiocarbonylative cyclization of N-(-iodoaryl)acrylamides with easily accessible thioformates has been developed. The reaction has a wide substrate scope with good yields and represents a powerful route to the synthesis of thioester-functionalized oxindoles. Both -aryl and alkyl thioformates as the thioester sources were well tolerated.

Palladium-Catalyzed Allylation of P(O)H Compounds: Access to 2-Fluoroallylic Phosphorus Compounds.

An efficient palladium-catalyzed 2-fluoroallylation of P(O)H compounds with -difluorocyclopropanes is presented. The reaction provides a variety of 2-fluoroallylic phosphorus compounds in good yields with high selectivity through the sequential C-C bond activation, C-F bond cleavage, and C-P coupling process. Various H-phosphonates, H-phosphinates, and secondary phosphine oxides are all tolerated.

Palladium-Catalyzed Heck Cyclization with P(O)H Compounds to Construct Phosphinonyl-Azaindoline and -Azaoxindole Derivatives.

We report herein a concise method for the construction of phosphinonyl-azaindoline and -azaoxindole derivatives via a palladium-catalyzed cascade cyclization with P(O)H compounds. Various -phosphonates, -phosphinates, and aromatic secondary phosphine oxides are all tolerated under the reaction conditions. Furthermore, the phosphinonyl-azaindoline isomer families such as 7-, 5-, and 4-azaindolines could be synthesized in moderate to good yields.

Highly regioselective and stereoselective cascade reductive cyclization of δ-ketoamide: practical access to oxa-bridged benzazepines.

A highly regioselective and stereoselective cascade reduction cyclization of -ketoamide is realized under LiAlH-assisted conditions, providing an atom-economical and straightforward approach to access oxa-bridged benzazepines in moderate to good yields. This method overcomes the limitations of aldehydes or other precursors of primary alcohols and realizes the cascade reduction cyclization of secondary alcohol anions generated from ketones. The reaction proceeds with broad substrate scope and good functional group compatibility.

[Establishment of a nude mouse model of orthotopically transplanted human primary malignant lymphoma of the liver].

Objective: To establish a nude mouse model of orthotopically transplanted human primary malignant lymphoma of the liver, and to serve researches on pathogenesis and experimental treatment of this disease.

Methods: Small pieces of lymphoma tissues freshly taken from patients with primary lymphoma of the liver were orthotopically transplanted into the liver parenchyma in nude mice. Tumorgenicity, invasion, metastasis, and morphological characteristics were examined by light and electron microscopy and immunohistochemistry.