α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases

The present study offers a new approach for designing inhibitors of protein tyrosine phosphatases. We have synthesized the cyclam derivatives with α,α-difluoro-β-ketophosphonate fragments covalently attached to tetraazamacrocyclic scaffold, which is known to be of medical interest. The obtained functionalized macrocycles were evaluated as inhibitors of PTP1B, TC-PTP, CD45, and other protein tyrosine phosphatases.Запроновано новий пiдхiд до розробки iнгiбiторiв протеїнтирозинфосфатаз. Синтезовано похiднi цикламу з α,α-дифторо-β-кетофосфонатними фрагментами, ковалентно зв’язаними з тетраазамакроциклiчною платформою. Отриманi функцiоналiзованi макроцикли було дослiджено як iнгiбiтори PTP1B, TC-PTP, CD45 та iнших протеїнтирозинфосфатаз.Предложен новый поход к разработке ингибиторов протеинтирозинфосфатаз. Синтезированы производные циклама с α,α-дифтор-β-кетофосфонатными фрагментами, ковалентно связанными с тетраазамакроциклической платформой. Полученные функционализированные макроциклы были изучены в качестве ингибиторов PTP1B, TC-PTP, CD45 и других протеинтирозинфосфатаз

XI Conferenza Europea di Chimica Organometallica

J. Org. Chem. (Russian

(±)-1,1'-Binaphtalene-2,2'-diol-derived phosphoric diester: immobilization on polyethylene glycol support and application in the Pudovik reaction

International audience(±) 1,1´ Binaphthalene 2,2´ diol (BINOL) was immobilized on polyethylene glycol (PEG) by means of triazole linkers, which were constructed by the [3+2] cycloaddition between azide and ethynyl fragments, preliminary incorporated into the molecules of these reactants. Treat ment of these BINOL derivatives with phosphorus oxychloride leads to the corresponding PEG immobilized 1,1´ binaphthalene 2,2´ diylphosphoric acids. The latter efficiently cata lyze the Pudovik reaction and can be reused without loss of catalytic activity

Cu(I) complexes with diethoxyphosphoryl-1,10-phenanthrolines in catalysis of C–C and C–heteroatom bonds formation

International audienc

Conjugated G0 Metallo-Dendrimers, Functionalized with Tridentate 'Pincer' -type Ligands

1, 3,5-Tris{3,5-bis[(diphenylphosphino)methyl]phenylethynyl}benzene (1) and hexakis{3,5-bis[(diphenylphosphino)methyl]phenylethynyl}benzene (2) have been synthesized and characterized. Furthermore, 1 was successfully cyclopalladated

Acetylene-bridged P,C,P'-Ligands and Corresponding Cyclopalladated Compounds

Bis-'pincer'-cyclopalladates 1 and 2 containing an ethynediyl- or a butadiynediyl-bridge have been synthesized, characterized and used as precatalysts in the Heck reaction