Influencing and improving the environmental performance of a large multi-national pharmaceutical company can be achieved with the help of electronic education tools, backed up by site champions and strong site teams. This paper describes the development of two of those education tools.

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Cross-conjugated dienone 18, a known precursor to (±)-coriolin, is prepared in 13 steps from simple lactone 4. Selective epoxidation of 18 provides (±)-hypnophilin. Key steps in the synthesis of 18 include a highly efficient SN2'-anti opening of 4 to give the necessary trans-3,5-disubstituted cyclopentene 11 and the novel Sml2-induced tandem radical cyclization of aldehyde 14.

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We have undertaken a staged development of certain estrogen-fluorophore conjugates, in order to prepare a fluorescent estrogen suitable for determination of the estrogen receptor content of individual cells. Since non-steroidal estrogens with bulky substituents are often more readily bound by receptor than their steroidal counterparts, we have investigated fluorophore conjugates with derivatives of the non-steroidal estrogen hexestrol [3R*, 4S*)-3,4-bis(4-hydroxyphenyl)hexane). On the basis of the receptor-binding affinity of model compounds, we prepared a prototypical set of three ring- and side-chain-substituted fluorescent hexestrol derivatives, whose binding and fluorescence properties ultimately led to the preparation of a series of side-chain-substituted nitrobenzoxadiazole derivatives. The compounds prepared have binding affinities for the estrogen receptors that range from ca. 1% to 5% that of estradiol, and they have very favorable fluorescence characteristics, similar to those of fluorescein.

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