Valodex - Tamoxifen

Tamoxifen Nolvadex Soltamox Selective estrogen Treatment of breast Tamaxin Tamoplex receptor modulator cancer Valodex mp 97 °C... 

Tamoxifen 449 is known as an estrogen antagonist and effective for metastatic breast cancer. Tamoxifen is the typical regiment for hormone receptor-positive breast cancer in premenopausal women, and it was developed by ICI Pharmaceuticals (now AstraZeneca, London, U.K.) under the trade names of Nolvadex, Istubal, and Valodex. While the previous synthetic approaches involved stoichiometric reagents or a multistep synthetic manipulations, Taniguchi applied his stereoselective copper-catalyzed alkyne functionalization to introduce halide and sulfide groups (Scheme 46.51) and to provide an access to 447. " In this approach, tamoxifen 449 was prepared in three steps from diphenyl acetylene 445 as a starting material with 51% overall yield 7JE = 93/7). 

---