Title:
PREPARATION METHOD FOR WATER-SOLUBLE FLORFENICOL AMINO ACID ESTER SALT
Document Type and Number:
WIPO Patent Application WO/2021/223301
Kind Code:
A1
Abstract:
Provided is a preparation method for water-soluble Florfenicol amino acid ester salt, the method comprising the steps of: using Florfenicol and N-Cbz-amino acid as starting raw materials, and subjecting same to acyl chlorination, esterification, deprotection, and acidification to form a salt so as to obtain the water-soluble Florfenicol amino acid ester salt. The raw materials are commercially available and low in cost. During the reactions, the reaction conditions in each unit are mild and controllable. Yields are high. The obtained Florfenicol amino acid ester salt is highly pure and water-soluble. The method is suitable for application in large-scale productions of water-soluble Florfenicol amino acid ester salts.
Inventors:
HAO ZHIHUI (CN)
ZHAO LEKAI (CN)
CUI LIANGLIANG (CN)
XIE LONGXIAO (CN)
HAO JIANGNAN (CN)
ZHAO LEKAI (CN)
CUI LIANGLIANG (CN)
XIE LONGXIAO (CN)
HAO JIANGNAN (CN)
Application Number:
PCT/CN2020/097656
Publication Date:
November 11, 2021
Filing Date:
June 23, 2020
Export Citation:
Assignee:
UNIV CHINA AGRICULTURAL (CN)
International Classes:
C07C315/04; C07C269/06; C07C271/22; C07C315/06; C07C317/32
Domestic Patent References:
| WO2004014860A2 | 2004-02-19 |
Foreign References:
| CN101605756A | 2009-12-16 | |||
| US4311857A | 1982-01-19 | |||
| US20050014828A1 | 2005-01-20 | |||
| US20080188556A1 | 2008-08-07 |
Other References:
HARDOUIN CHRISTOPHE, BAILLARD SANDRINE, BARIÈRE FRANÇOIS, COPIN CHLOÉ, CRAQUELIN ANTHONY, JANVIER SOLENN, LEMAITRE SYLVAIN, LE ROU: "Multikilogram Synthesis of a Potent Dual Bcl-2/Bcl-x L Antagonist. 1. Manufacture of the Acid Moiety and Development of Some Key Reactions", ORGANIC PROCESS RESEARCH & DEVELOPMENT, AMERICAN CHEMICAL SOCIETY, US, vol. 24, no. 5, 15 May 2020 (2020-05-15), US , pages 652 - 669, XP055863535, ISSN: 1083-6160, DOI: 10.1021/acs.oprd.9b00364
Attorney, Agent or Firm:
BEIJING HUAKE UNION PATENT OFFICE(GENERAL PARTNERSHIP) (CN)
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