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Title:
A SULPHONYL TETRAZOLE COMPOUND, ITS PREPARATION METHOD AND ITS USE FOR PREPARING LAETISPICINE
Document Type and Number:
WIPO Patent Application WO/2010/091540
Kind Code:
A1
Abstract:
A sulphonyl tetrazole compound 7 with the following structure, its preparation method and its use for preparing laetispicine. The said sulphonyl tetrazole compound 7, (1-phenyl-5-(3,4-methylenedioxyphenyl ethyl) sulphonyl tetrazole), is obtained from piperonal as raw material and by steps of Darzens condensation, hydrolysis, decarboxylation, reduction, condensation and oxidation. Laetispicine is prepared from the said compound as raw material, by condensation with 9-carbonyl-2E-4E-nonadienoic acid isobutyramide (compound 14), or by reaction with 5-(tetrahydropyran-2-oxo) n-pentanal (compound 10), deprotection, Swern oxidation, Wittig-Horner reaction, hydrolysis and amidation. As shown in H NMR, C NMR, MS and IR, the laetispicine prepared from the above-said compound is consistent with the laetispicine extracted from natural products.

Inventors:
SHEN JINGKANG (CN)
YAO SHUYI (CN)
PAN SHENGLI (CN)
HU DINGYU (CN)
QIAN FUGANG (CN)
YAO CHUNYAN (CN)
WANG XIN (CN)
Application Number:
PCT/CN2009/001246
Publication Date:
August 19, 2010
Filing Date:
November 11, 2009
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Assignee:
SHANGHAI INST MATERIA MEDICA (CN)
SHEN JINGKANG (CN)
YAO SHUYI (CN)
PAN SHENGLI (CN)
HU DINGYU (CN)
QIAN FUGANG (CN)
YAO CHUNYAN (CN)
WANG XIN (CN)
International Classes:
C07D405/12; A61P25/24; C07D317/60
Foreign References:
CN88101155A1988-09-28
CN1389462A2003-01-08
CN1593399A2005-03-16
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (Block B KingSound International Center, 116 Zizhuyuan Road, Haidian District, Beijing 7, CN)
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