Novel Stereoselective Synthesis of 11.beta.-Carbon-Substituted Estradiol Derivatives

Design and Synthesis of an Aromatic-steroid Derivative

“…Nevertheless, despite its wide scope, have some drawbacks e.g., several agents used have a limited stability and their preparation require condition specials [10][11][12][13] . Analyzing these data, in this study we report a straightforward route for synthesis of 5 using some strategies.…”

Synthetic Routes to 11-Oxygenated 14α,17α-Ethanoestradiols

“…[6] While the epoxidationϪrearrangement sequence is higher yielding overall, and also provides access to the 9β-series, [7] albeit as minor products, the directness and selectivity of the hydroborationϪoxidation sequence offer advantages for practical synthesis of the target intermediates.…”

“…[5] Additionally, the presence of a 17α-ethynyl group does not reduce the high receptor binding affinity of these analogues, and in some cases enhances the stability of the receptorϪligand complex. [5,6] It was therefore considered of interest to examine the effect of the 14α,17α-ethano bridge in conjunction with functionality at C-11 towards receptor binding, and a programme was initiated towards this end. In order to develop a versatile synthesis of the desired analogues, the introduction of an oxygen functionality at C-11 of 14α,17α-ethanoestradiols was identified as a primary objective.…”

Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using “click” chemistry

“…The latter route may be shorter but it is less effective for aryl than alkyl derivatives. 60,61 The incorporation of the protected phenolic group in the aryl moiety would subsequently permit the attachment of a variety of substituents via Williamson or Mitsunobu chemistry. Oligoethylene glycols provided several advantages as linkers.…”