Recent Advances in the Synthesis of Tamoxifen and Analogues in Medicinal Chemistry

Abstract Abstract: Tamoxifen is one of the important tricyclicethylene moieties and recognized as an important drug candidate because of extensive applications in the field of medicinal and pharmaceutical chemistry. Recently, ample attention is given to this analogue by organic and medicinal chemistry community due to its successful utilization for the inhibition of estrogen receptor in MCF‐7 breast cancer cell lines. Due to its structural character, tamoxifen is also useful in material chemistry. The synthesis of tamoxifen and its anlogues is desirable from easily available chemicals as an important drug candidate. Here, we report a review on various synthetic schemes for tamoxifen and its anlogues employing use of different strategies such as formation of C−C, C=C and C≡C bonds, C−H functionalization, addition to alkynes, insertion reaction, nucleophilic substitution and addition reactions, elimination reaction, reductive couplings etc.