Title:
WATER-SOLUBLE DERIVATIVES OF ANESTHETIC 2,6-DIISOPROPYLPHENOL AND PREPARATION METHOD THEREOF
Document Type and Number:
WIPO Patent Application WO/2008/022541
Kind Code:
A1
Abstract:
Disclosed are a series of esters containing 2,6-diisopropylphenyl and tert-amine, the water-soluble derivatives thereof (II) through reaction with acid, and preparation method thereof. The method uses 2,6-diisopropylphenol (I) as a raw material to obtain said derivatives (II). Said water-soluble derivatives have the general formula (II), wherein: n = 0-7; R = H, methyl, ethyl; and D represents organic groups containing tertiary amine and the salts through reaction with the corresponding acids. The disclosed water-soluble derivatives can release 2,6-diisopropylphenol (I) with narcotic effect after hydrolysis in vivo, thus the derivatives can be used as narcotic prodrugs for injection.
Inventors:
LI QINGGENG (CN)
LI DAIHUA (CN)
TIAN RUI (CN)
WANG JINGYUAN (CN)
WANG TAO (CN)
CHEN PAN (CN)
SUN YANGQIANG (CN)
HE LIANG (CN)
LI DAIHUA (CN)
TIAN RUI (CN)
WANG JINGYUAN (CN)
WANG TAO (CN)
CHEN PAN (CN)
SUN YANGQIANG (CN)
HE LIANG (CN)
Application Number:
PCT/CN2007/002411
Publication Date:
February 28, 2008
Filing Date:
August 13, 2007
Export Citation:
Assignee:
LI QINGGENG (CN)
International Classes:
C07C219/26; A61K31/223; A61P23/00; C07C213/02; C07D295/00
Domestic Patent References:
| WO2005046575A2 | 2005-05-26 |
Other References:
TRAPANI G. ET AL.: "Water-soluble salts of amino acid esters of the anesthetic agent propofol", INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 175, no. 2, 1998, pages 195 - 204, XP002112863, DOI: doi:10.1016/S0378-5173(98)00284-1
Attorney, Agent or Firm:
CHONGQING HENGXIN PATENT AGENT CO., LTD (Longhua Road LongxiYubei District, Chongqing 7, CN)
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