abstract |
Provided are an intermediate which can be used for synthesizing halichondrin B, eribulin or an analogue thereof, in particular a C27-C35 structure fragment thereof, a preparation method therefor and use thereof. The starting raw materials of the synthetic route are cheap and easily available, and the optical purity thereof can be ensured, thereby ensuring the optical purity of the C27-C35 structure fragment in halichondrin, eribulin or an analogue thereof. The step and method for constructing the chiral center of C27-C35 structure fragment has high diastereoselectivity and yield, especially the preparation method for the compounds represented by formula (X), formula (XI), formula (XVI) and formula (XV). Some reaction by-products can be removed only by means of recrystallization, which facilitates purification and greatly reduces costs. |