申请人:Lucky, Ltd.
公开号:US05502200A1
公开(公告)日:1996-03-26
The present invention relates to a novel reactive thiophosphate derivative of thia(dia)zole acetic acid which can be very effectively used in the preparation of .beta.-lactam antibiotics, and which is represented by the following general formula (I): ##STR1## in which R.sup.1 represents hydrogen or an amino-protecting group; R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, or --C(R.sup.a)(R.sup.b)CO.sub.2 R.sup.c, wherein R.sup.a and R.sup.b are identical or different from each other and represent hydrogen or C.sub.1 -C.sub.4 alkyl, or R.sup.a and R.sup.b together with a carbon atom to which they are bound can form a C.sub.3 -C.sub.7 cycloalkyl group and R.sup.c is hydrogen or a carboxy-protecting group; R.sup.3 represents C.sub.1 -C.sub.4 alkyl or phenyl or R.sup.3 together with an oxygen atom and a phosphorus atom to which it is bound can form a 5- or 6-membered heterocyclic ring; and Q represents N or CH, and to a process for preparing the same.
本发明涉及一种新型的噻(二)唑乙酸反应性硫代磷酸酯衍生物,可非常有效地用于制备β-内酰胺类抗生素,其通式如下(I):其中R1代表氢或氨基保护基;R2代表氢、C1-C4烷基或--C(R.sup.a)(R.sup.b)CO2R.sup.c,其中R.sup.a和R.sup.b相同或不同,代表氢或C1-C4烷基,或R.sup.a和R.sup.b连同其所连接的碳原子可以形成C3-C7环烷基,R.sup.c代表氢或羧基保护基;R3代表C1-C4烷基或苯基,或R3连同其所连接的氧原子和磷原子可以形成5-或6-成员杂环环;Q代表N或CH,以及其制备方法。