| 摘要 |
<p>There is provided a method for producing a biarylalanine compound of formula (4):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="45" wi="85" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry>
wherein
R<Sup>1</Sup> represents an amino protective group, and R<Sup>2</Sup> represents an amino protective group or a hydrogen atom,
R<Sup>3</Sup> is a carboxy protective group, or
said amino protective and carboxy protective groups together form an amino acid protective group, and
R<Sup>4</Sup> is a substituted or unsubstituted aryl or heteroaryl group, which comprises reacting an aromatic amino acid of formula (1):
<Chemistry id="chema02" num="0002"><Image id="ia02" he="38" wi="85" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry>wherein
X is a halogen atom or a trifluoromethanesulfonyloxy group, and
R<Sup>1</Sup>, R<Sup>2</Sup> and R<Sup>3</Sup> are the same as defined above, with an organic boron compound of formula (2):
<Chemistry id="chema03" num="0003"><Image id="ia03" he="22" wi="50" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> wherein R<Sup>4</Sup> has the same meaning as defined above, and
Q<Sup>1</Sup> and Q<Sup>2</Sup> are the same or different and independently represent a hydroxy group or an alkoxy group having 1 to 4 carbon atoms, or
Q<Sup>1</Sup> and Q<Sup>2</Sup> together form an alkylenedioxy or 1,2-phenylenedioxy group optionally substituted by an alkyl group having 1 to 4 carbon atoms,
or
a boroxine ring compound of formula (3):
<Chemistry id="chema04" num="0004"><Image id="ia04" he="28" wi="47" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry>
wherein R<Sup>4</Sup> has the same meaning as defined above, or a mixture thereof, in the presence of a nickel catalyst and a base.</p> |
