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Title:
HIMBACINE ANALOGUE AND METHOD FOR PREPARING INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/095684
Kind Code:
A1
Abstract:
The present invention provides a himbacine analogue and a method for preparing an intermediate thereof, and particularly provides a new method for preparing a compound A, a compound 4, a compound D and a compound C. In the solution for preparing the compound A according to the present invention, the carboxylic acid does not need to be reduced into aldehyde, and instead, the corresponding alcohol is directly oxidized into the corresponding aldehyde, so the operation is safe, and the harsh condition of using anhydrous palladium-carbon in the prior art is avoided when the carboxylic acid is converted into acyl chloride and is then hydrogenated into aldehyde under the catalysis of the palladium catalyst. The preparation method is simple and the operation steps are simple and convenient. Especially, when the hydroxyl protective group P is a benzyl group, the nitro group can be reduced into an amino group when the protective group P is removed, the reaction steps are largely simplified, and the raw materials and reagents are saved. The whole route is low in production cost, high in yield and suitable for industrial production.

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Inventors:
YUAN JIANDONG (CN)
CHEN YAO (CN)
SUN QIYANG (CN)
HANG WENMING (CN)
Application Number:
PCT/CN2015/095744
Publication Date:
June 23, 2016
Filing Date:
November 27, 2015
Export Citation:
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Assignee:
BRIGHTGENE BIO MEDICAL TECHNOLOGY CO LTD (CN)
International Classes:
C07D307/92; C07C201/12; C07C205/55; C07D405/06; C07F7/18
Foreign References:
CN101511852A2009-08-19
CN101553484A2009-10-07
Other References:
XING, QIYI ET AL.: "Basic Organic Chemistry", ADVANCED EDUCATION PRESS, 30 November 1993 (1993-11-30), pages 386 - 387
Attorney, Agent or Firm:
SUNSHINE INTELLECTUAL PROPERTY INTERNATIONAL CO., LTD (CN)
北京三聚阳光知识产权代理有限公司 (CN)
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