Title:
METHOD FOR PREPARING BORON SALT OF DIPEPTIDE OF VALINE-PROLINE
Document Type and Number:
WIPO Patent Application WO/2021/043187
Kind Code:
A1
Abstract:
Provided is a method for preparing a boron salt of a dipeptide of valine-proline. The method uses pyrrolidine boric acid protected by an R1 group and valine protected by an R4 group as the initial raw materials, and avoids the problem of product loss caused by complex post-processing during deprotection, thereby greatly improving the yield of a target product, and facilitating mass production thereof; and same also uses a resolution method by means of a resolving agent, and avoids the problem of excessive loss of a product with a target configuration caused by using resolution methods with different solubilities, thereby greatly improving the yield of the product with the target configuration.
Inventors:
LAI ZHEN (CN)
LIN ZENGMING (CN)
LIN ZENGMING (CN)
Application Number:
PCT/CN2020/113131
Publication Date:
March 11, 2021
Filing Date:
September 03, 2020
Export Citation:
Assignee:
BALMXY PHARMACEUTIC CO LTD (CN)
International Classes:
C07F5/02
Domestic Patent References:
| WO2008066729A2 | 2008-06-05 | |||
| WO1991016339A1 | 1991-10-31 | |||
| WO2018187698A2 | 2018-10-11 |
Foreign References:
| CN1073946A | 1993-07-07 |
Other References:
GIBSON FRANK S., SINGH AMBARISH K., SOUMEILLANT MAXIME C., MANCHAND PERCY S., HUMORA MICHAEL, KRONENTHAL DAVID R.: "-Valyl-pyrrolidine-(2 R )-boronic Acid: Efficient Recycling of the Costly Chiral Auxiliary (+)-Pinanediol", ORGANIC PROCESS RESEARCH & DEVELOPMENT, AMERICAN CHEMICAL SOCIETY, US, vol. 6, no. 6, 1 November 2002 (2002-11-01), US, pages 814 - 816, XP055789568, ISSN: 1083-6160, DOI: 10.1021/op025587b
Attorney, Agent or Firm:
XI'AN BESHININGQIN INTELLECTUAL PROPERTY AGENCY (CN)
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