Angelmicin B (hibarimicin B) has been shown to be a highly specific inhibitor of v-Src type protein tyrosine kinase (IC₅₀: 23 μM). It has also been shown to inhibit the growth of tumor cells and to induce differentiation in human myeloid leukemia cell lines HL-60 (IC₅₀: 57 nM). The complexity and the intriguing bioactivity make it an important synthetic target. We have previously described a Ring Closing Eneyne Metathesis/Intramolecular Diels-Alder, and tandem alkoxy radical fragementation-etherification sequence for the synthesis of AB subunit synthon. Herein we present the further advances toward the total synthesis of Anglemicin B.