INTERMEDIATE OF CILASTATIN AND PREPARATION METHOD THEREOF

WIPO Patent Application WO/2010/088862

A1

Disclosed is a method for preparing 7-halo-2-oxo-heptylate, an intermediate of cilastatin. The main steps are as follows: A. Addition reaction, in which 6-halo-hexanal is reacted with a cyanide to obtain 7-halo-α-hydroxyl-heptonitril; B. Hydrolysis reaction, in which 7-halo-α-hydroxyl- heptonitril is converted into 7-halo-α-hydroxyl-heptylic acid; C. Esterification reaction, in which 7-halo-α-hydroxyl-heptylic acid is converted into 7-halo-α-hydroxyl-heptylate, and D. Oxidation reaction, in which 7-halo-α-hydroxyl-heptylate is converted into 7-halo-2-oxo-heptylate.7-halo-α-hydroxyl-heptylic acid or ester, which is a new intermediate for synthesizing 7-halo-2-oxo-heptylate or cilastatin, and a method for synthesizing cilastatin are also disclosed. The methods of the invention are suitable for commercial production because of their simple process and mild reaction condition.

TANG HE (CN)
YUAN WENQIU (CN)
FU JIA (CN)

PCT/CN2010/070560

August 12, 2010

February 08, 2010

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ZHEJIANG HISOAR PHARMACEUTICAL (CN)
TANG HE (CN)
YUAN WENQIU (CN)
FU JIA (CN)

C07C69/716; C07C59/115; C07C67/08; C07C67/313; C07C69/675; C07C319/14; C07C323/59

WO1998015520A1

1998-04-16

CN101475481A	2009-07-08
CN101265187A	2008-09-17
CN1587248A	2005-03-02
EP0441371A1	1991-08-14
US5147868A	1992-09-15
CN1587248A	2005-03-02

J. MED. CHEM., vol. 30, no. 6, 1987, pages 1074 - 1090
JOURNAL OF CHINESE PHARMACEUTICALS, vol. 36, no. 9, 2005, pages 531

BOSS & YOUNG PATENT AND TRADEMARK LAW OFFICE (Tower A Bldg. No. 1, GT International Center,,Jia 3 Yongandongli, Jianguomenwai Avenue,, Chaoyang District, Beijing 2, CN)

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