1, 8-Bis (Dimethylamino)Naphthalene

On November 15, 2010, the FDA approved Halaven for the treatment of patients with metastatic breast cancer who have received at least two chemotherapy regimens. There are 19 chiral centers in the fractional structure of eizbrine, which is very difficult to synthesize. Compound Erb and compound P1 are important intermediates for the synthesis of eizbrine.

ERB-2 preparation of ERB process, through the reaction substrate screening suitable reaction conditions, ERB-1 and iodide ene reaction, by using Mn powder as an asymmetric catalyst, and add ligand to the reaction system, and cobalt phthalocyanine, Cr3+, 1, 8-Bis (Dimethylamino)Naphthalene, cobalt phthalocyanine and dichloro-zirconium, Compared with the prior art of Ni/Cr mediated asymmetric synthesis, the chiral center of this reaction has higher selectivity, and the yield and purity of the reaction are significantly improved. Selectively produce diastereomers of the pure chiral compound ERB, which is different from the prior techniques usually taught for the final step of PV protection of the side chain hydroxyl.

In addition,Carboxylic acids and their derivatives are widely found in natural products and drug molecules. The structural modification of these organic small molecule skeletons provides new opportunities for the design and synthesis of innovative drugs. 1, 8-Bis (Dimethylamino)Naphthalene can be used to synthesize carboxylic acid derivatives.