Patent · US Active

Process for the preparation of eribulin mesylate intermediate

US11447499B2 · kind B2 · utility

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3References

1Claims

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Assignee

RK PHARMA INC. · US

Inventors

Ravishanker Kovi · Sparta, US
Jayaraman Kannappan · Mahesana, IN
Shivnath Sahebrao Patil · Dhule, IN

Key dates

Filing date	Jun 11, 2020
Grant date	Sep 20, 2022
Priority date	—
Expiry date	Jun 11, 2040

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07D493/22
WIPO fieldOrganic fine chemistry
WIPO sectorChemistry

Abstract

The present application provides improved processes for the synthesis of eribulin intermediate, which generally comprise the steps of: a) De-protecting the eribulin-enone (compound 1) in tetrahydrofuran by using TBAF solution, buffered with imidazole HCl in the presence of molecular sieve and sodium sulphate to get an insitu mixture of eribulin-dione diastereomer at C12 carbon (compound 2). Then ketalization may be performed of eribulin-dione insitu intermediate containing mixture of diastereomer at C12 carbon (compound 2) with PPTS in dichloromethane to yield eribulin-diol (compound 3).

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.