660390-78-3

Upstream product

• 50-00-0 formaldehyd 
• 2923-83-3 4,6-di(tert-butyl)-3-fluorophenol 
• 1364916-71-1 5-iodo-3'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-2'-deoxyuridine monophosphate 
• 1364916-69-7 5-iodo-3'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-2'-deoxyuridine monophosphate 
• 1313031-74-1 5-iodo-5'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-3'-fluoro-2',3'-dideoxyuridine monophosphate 
• 1313031-67-2 5-iodo-5'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-3'-fluoro-2',3'-dideoxyuridine monophosphate 
• 1150314-78-5 5-[⁽¹²⁵⁾I]iodo-5'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-3'-fluoro-2',3'-dideoxyuridine monophosphate 
• 1150314-79-6 5-[⁽¹²⁵⁾I]iodo-5'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-3'-fluoro-2',3'-dideoxyuridine monophosphate 
• 1026558-43-9 cyclo-3,5-di(tert-butyl)-6-fluoro chlorophosphite 
• 1313031-57-0 5-iodo-5'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-2'-deoxyuridine monophosphate 
• 1313031-73-0 5-iodo-5'-O-[cyclo-3,5-di(tert-butyl)-6-fluorosaligenyl]-2'-deoxyuridine monophosphate 
• 372-20-3 3-fluorophenol 
• 660390-76-1 1-[5-(6,8-di-tert-butyl-5-fluoro-2-oxo-4H-2λ⁵-benzo[1,3,2]dioxaphosphinin-2-yloxymethyl)-2,5-dihydro-furan-2-yl]-5-methyl-1H-pyrimidine-2,4-dione 

Relevant academic research and scientific papers

Radiolabeled cyclosaligenyl monophosphates of 5-iodo-2′-deoxyuridine, 5-iodo-3′-fluoro-2′,3′-dideoxyuridine, and 3′-fluorothymidine for molecular radiotherapy of cancer: Synthesis and biological evaluation

Targeted molecular radiotherapy opens unprecedented opportunities to eradicate cancer cells with minimal irradiation of normal tissues. Described in this study are radioactive cyclosaligenyl monophosphates designed to deliver lethal doses of radiation to cancer cells. These compounds can be radiolabeled with SPECT- and PET-compatible radionuclides as well as radionuclides suitable for Auger electron therapies. This characteristic provides an avenue for the personalized and comprehensive treatment strategy that comprises diagnostic imaging to identify sites of disease, followed by the targeted molecular radiotherapy based on the imaging results. The developed radiosynthetic methods produce no-carrier-added products with high radiochemical yield and purity. The interaction of these compounds with their target, butyrylcholinesterase, depends on the stereochemistry around the P atom. IC50 values are in the nanomolar range. In vitro studies indicate that radiation doses delivered to the cell nucleus are sufficient to kill cells of several difficult to treat malignancies including glioblastoma and ovarian and colorectal cancers.

PRODRUGS OF AZACITIDINE 5'-PHOSPHATE

The present disclosure relates to analogs or derivatives of azacitidine with improved pharmaceutical properties and methods for the treatment of proliferative disease utilizing said analogs or derivatives.

Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship

A large number of cycloSal-nucleotide triesters 1-49 have been studied concerning their ability to inhibit cholinesterases of different origins as well as to inhibit HIV replication in cell culture. It was shown that none of the triesters showed inhibitor

3,5-Di-(tert-Butyl)-6-fluoro-cycloSal-d4TMP - A Pronucleotide with a Considerably Improved Masking Group

A new, considerably improved cycloSal masking group has been developed. This new group combines four desirable properties and has been attached to the anti-HIV drug 2′,3′-dideoxy-2′,3′-didehydrothymidine (d4T, 1) to give 3,5-(di-tert-butyl)-6-fluoro-cycloSal-d4TMP (2i). This phosphate triester has a reasonable chemical half-life, highly selectively released d4TMP, has poor - if any - inhibitory effect on butyrylcholinesterase (BChE), and achieved the TK-bypass. ( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).