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# c19) United States 

# c12) Patent Application Publication MURAO et al. 

# (54) PROCESS FOR PRODUCING 3-AMINO-2-HYDROXYPROPIONIC ACID DERIVATIVES 

(75) Inventors: Hiroshi MURAO, Kako-gun (JP); Koki Yamashita, Kobe-shi (JP); Toshihiro Takeda, Takasago-shi (JP); Yasuyoshi Ueda, Himeji-shi (JP) 

Correspondence Address: FOLEY AND LARDNER LLP SUITE 500 3000 K STREET NW WASHINGTON, DC 20007 (US) 

(73) Assignee: KANEKA CORPORATION 

(21) Appl. No.: 11/276,222 

(22) Filed: Feb. 17, 2006 

(62) Division of application No. 10/312,208, filed on Jan. 28, 2003, filed as 371 of international application No. PCT/JP0l/05440, filed on Jun. 26, 2001. 

## (30) Foreign Application Priority Data 

Jun. 26, 2000 (JP) ...................................... 2000-190949 

May 23, 2001 (JP) ...................................... 2001-154074 

(51) Int. Cl. C07D 263/38 (2006.01) C07D 263/04 (2006.01) 

(52) U.S. Cl. ............................................ 548/229; 562/557 

## (57) ABSTRACT 

The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advanta- 

## Related U.S. Application Data 

## Publication Classification 

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US 20060135784Al 

# c10) Pub. No.: US 2006/0135784 Al 

# (43) Pub. Date: Jun. 22, 2006 

geous, and is suitable for an industrial production, which process comprises: 

treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-posi› tion carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-pro› tected-3-aminopropionic acid derivatives (3), 

then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives ( 4) having an inverted steric configu› ration at 2-position carbon, 

and then converting the derivatives into 3-amino-2-hy› droxypropionic acid derivatives (1). 

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