The present invention produces novel cis-oxazolidinone compound which is racemic form or optically active form, of a formula (1)
wherein R represents C1-C6 alkyl group, C2-C6 alkenyl group, C1-C6 alkoxyl group, C1-C6 alkylamino group, aryl group or halogen atom, and oxazolidinone ring is at cis-configuration, comprising reacting cis-1,2-indene epoxide of a formula (3)
form, with sulfonyl isocyanate compound of a formula (4)
in the presence of metal halide catalyst.
Further, cis-1-amino-2-indanol is produced by hydrolyzing the oxazolidinone compound. The latter compound is useful as an intermediate of HIV-drug.
本发明生产出新型顺式
噁唑烷酮化合物,该化合物为外消旋形式或光学活性形式,其式为(1)
其中 R 代表 C1-C6 烷基、C2-C6 烯基、C1-C6 烷氧基、C1-C6 烷基
氨基、芳基或卤素原子,且
噁唑烷酮环为顺式构型。
与式 (4) 的磺酰
异氰酸酯化合物反应
在
金属卤化物催化剂存在下进行反应。
此外,顺式-
1-氨基-2-茚醇可通过
水解
噁唑烷酮化合物制得。后一种化合物可用作 HIV 药物的中间体。