公开(公告)号：EP0710725A1

公开(公告)日：1996-05-08

申请号：EP95117120.6

申请日：1995-10-31

申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

发明人： Nakahama, Kazuo ,  Izawa, Motowo ,  Nagano, Yoichi ,  Tarui, Naoki ,  Matsumoto, Kiyoharu ,  Kori, Masakuni ,  Kanamaru, Tsuneo ,  Nagata, Toshiaki

IPC分类号： C12P41/00

CPC分类号： C12P17/10 ,  C12P7/22 ,  C12P41/004 ,  C12P41/005

摘要： A process for producing an optically active form of a compound of formula (I)

wherein R₁ represents hydrogen or a hydrocarbon group that may be substituted; R₂ and R₃ independently represent hydrogen, a hydrocarbon group that may be substituted, or a heteroaromatic group that may be substituted; X' represents a substituent comprising an esterified carboxyl group or an acylated hydroxyl group; ring A represents a benzene ring that may be substituted or a heteroaromatic ring that may be substituted; ring J' represents a 7- or 8-membered heterocyclic ring containing at most 3 hetero-atoms as ring-constituent members, which may have a further substituent or substituents in addition to R₁, R₂, R₃ and X', and C* denotes a chiral carbon atom or a salt thereof, which comprises subjecting the racemic compound of the formula (I) or a salt thereof, or alternatively a racemic starting compound for synthesizing the compound of the formula (I) to enzymatically enantioselective hydrolysis to provide an optically active form thereof.

摘要翻译： 一种制备光学活性形式的式（I）化合物的方法其中R 1表示氢或可被取代的烃基; R2和R3独立地表示氢，可被取代的烃基或可被取代的杂芳族基; X'表示包含酯化羧基或酰化羟基的取代基; 环A表示可被取代的苯环或可被取代的杂芳环; 环J'表示含有至多3个杂原子作为环构成成员的7或8元杂环，除R1，R2，R3和X'之外，还可以具有另外的取代基或取代基，C *表示 其包括使式（I）的外消旋化合物或其盐或外消旋起始化合物合成式（I）化合物进行酶对映选择性水解以提供光学 其活性形式。