Novel synthesis of bis(phosphonic acid)-steroid conjugates.
An efficient synthesis has been realized for several members of a new class of potential bone resorption inhibitors consisting of steroidal oestrogenic units linked at the 3 and 17 positions to a geminal bisphosphonate moiety through an ester linkage of variable length. The convergent synthesis utilizes benzyl bisphosphonates, transesterification, and Meldrum's acid chemistry and has the potential to allow many oestrogenic derivatives as well as other biologically active compounds to be coupled to the geminal bisphosphonate moeity.
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Department of Chemistry, Loughborough University, Loughborough, Leicestershire LE11 3TU, England.
McKenzie
M J
MJ
Gallagher
J A
JA
D001862:Bone Resorption / Q000517:prevention & control*; D016207:Cytokines / Q000096:biosynthesis; D007202:Indicators and Reagents; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000494:pharmacology*; D010010:Osteoclasts / Q000187:drug effects; D013256:Steroids / Q000138:chemical synthesis* / Q000494:pharmacology*
D016207:Cytokines; D007202:Indicators and Reagents; D063065:Organophosphonates; D013256:Steroids