METHOD FOR REMOVING CARBOXYL AND HYDROXYL PROTECTING GROUP OF β-LACTAM COMPOUND

WIPO Patent Application WO/2018/233477

A1

The present invention discloses a method for removing a carboxyl and hydroxyl protecting group of a β-lactam compound. The method is removing a carboxyl and/or hydroxyl protecting group from a protected β-lactam compound under the action of trichloroacetic acid and a carbocation absorbent to give a deprotected product of the β-lactam compound. The method of the present invention employs trichloroacetic acid instead of trifluoroacetic acid, and combines trichloroacetic acid with phenol or m-cresol, and anisole, greatly reducing the amount of trichloroacetic acid used. In addition, trichloroacetic acid is decomposed in the presence of water into chloroform and carbon dioxide in a subsequent process converting cephalosporin to a sodium salt, and is easy to remove, without the problem of residual trichloroacetic acid, achieving a high reaction yield and producing relatively few impurities. Trichloroacetic acid is cheap and environmentally friendly and is beneficial in industrial production due to cost reductions achieved.

CHAI MINJUN (CN)
YUAN ZHEDONG (CN)
QIAN JINGJIE (CN)
LI PENGCHENG (CN)
LUO JIAYING (CN)
CHEN WANGLU (CN)
CHEN QINGQING (CN)
LIU JING (CN)

PCT/CN2018/089760

December 27, 2018

June 04, 2018

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ZHEJIANG WHITESON PHARMACEUTICAL CO LTD (CN)
HANGZHOU SENZE PHARMACEUTICAL TECH CO LTD (CN)
SHANGHAI DUDE MEDICAL TECH CO LTD (CN)

C07D505/08; C07D499/87; C07D501/04; C07D501/56; C07D505/20

WO2002090364A1	2002-11-14
WO2004039814A1	2004-05-13

US4677100A

1987-06-30

TUO YING LAW OFFICES (SHANGHAI) (CN)

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