c19)  United States  c12)  Patent Application Publication  MURAO et al.  c10)  Pub. No.: US 2006/0135784 Al  (43)  Pub. Date:  Jun. 22, 2006  (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)  (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.  (51)  Int. Cl.  C07D  263/38  (2006.01)  C07D  263/04  (2006.01)  (52)  U.S. Cl.  ............................................  548/229;  562/557  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).  Correspondence Address:  FOLEY AND LARDNER LLP  SUITE 500  3000 K STREET NW  WASHINGTON, DC 20007 (US)  geous, and is suitable for an industrial production, which  process comprises:  Jun. 26, 2000  (JP) ...................................... 2000-190949  May 23, 2001  (JP) ...................................... 2001-154074  The present invention provides a process for preparing  3-amino-2-hydroxypropionic acid derivatives (1) which  does not use dangerous reagents, is economically advanta- (57)  ABSTRACT  Publication Classification  (30)  Foreign Application Priority Data  Related U.S. Application Data  US 20060135784Al  (1)  R3  I  R $^{1}$R$^{2}$C-N-H  I  HC-OH  I  COOR  (2)  R3  I  R $^{1}$R$^{2}$C-N-S1  I  HO-CH  I  coos 2  (3)  (4)  R3  I  R $^{1}$R$^{2}$C-N-S6  I  HC-o-s 5  I  coos 4 