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# c12) United States Patent Jiao et al. 

# (54) PREPARATION METHOD OF MICAFUNGIN SODIUM 

(75) Inventors: Guangjun Jiao, Shanghai (CN); Shidong Liu, Shanghai (CN); Bingming He, Shanghai (CN); Zhijun Tang, Shanghai (CN); Xiaoming Ji, Shanghai (CN) 

(73) Assignee: Shanghai Techwell Biopharmaceutical Co., Ltd., Shanghai (CN) 

( *) Notice: Subject to any disclaimer, the term ofthis patent is extended or adjusted under 35 U.S.C. 154(b) by O days. 

(21) Appl. No.: 14/116,947 

(22) PCT Filed: May 11, 2012 

(86) PCT No.: PCT /CN2012/075339 § 371 (c)(l), (2), ( 4) Date: Jan.2,2014 

(87) PCT Pub. No.: WO2012/152225 PCT Pub. Date: Nov.15, 2012 

## (65) Prior Publication Data 

US 2014/0114049 Al Apr. 24, 2014 

## (30) Foreign Application Priority Data 

May 12, 2011 (CN) .......................... 2011 1 0121705 

(51) Int. Cl. 

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(52) U.S. Cl. CPC ................ C07K 1114 (2013.01); C07D 413112 (2013.01); C07K 11113 (2013.01); C07K 7156 (2013.01) 

( 58) Field of Classification Search None See application file for complete search history. 

## (56) References Cited 

2014/0371422 Al* 12/2014 Gunnes et al. ................ 530/329 

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PCT International Search Report and Written Opinion dated Aug. 23, 2012 issued in PCT/CN2012/075339 (WO/2012/152225). 

## U.S. PATENT DOCUMENTS 

## FOREIGN PATENT DOCUMENTS 

## OTHER PUBLICATIONS 

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# (IO) Patent No.: US 9,115,177 B2 

# (45) Date of Patent: Aug. 25, 2015 

Ohigashi et al. (2006) "Process development ofmicafungin. a novel lipopeptide antifungal agent." Yuki Gosei Kagaku Kyokaishi .. 64( 12): 1294-1303. 

Tomishima et al. (2008) "Novel echinocandin antifungals. Part 2: Optimization of the side chain of the natural product FR901379. Discovery of micafungin" Bioorganic & Medicinal Chemistry Let› ters 18: 2886-2890. 

* cited by examiner 

Primary Examiner - Jeffrey E Russel 

(7 4) Attorney, Agent, or Firm - Tom Hunter; Weaver Austin Villeneuve & Sampson LLP 

## (57) ABSTRACT 

The method of the preparation of micafungin sodium com› prises the step of mixing the weak base and the aqueous solution containing micafungin acid (the structure is illus› trated by formula I) or the mixed aqueous solution containing the compound of formula I and organic solvent in order to obtain the sodium salt of micafungin (the structure is illus› trated by formula II). 

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US0091151 77B2 

17 Claims, 4 Drawing Sheets 

