Intermediate of eribulin and synthesis method and use thereof
US11976081B2 · kind B2 · utility
Assignee
Inventor
Key dates
| Filing date | Apr 2, 2020 |
| Grant date | May 7, 2024 |
| Priority date | — |
| Expiry date | Aug 16, 2040 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.