公开(公告)号：US06407258B1

公开(公告)日：2002-06-18

申请号：US09601032

申请日：2000-07-26

申请人： Bernd Napierski ,  Heinz-Peter Rebenstock ,  Wolfgang Holla

发明人： Bernd Napierski ,  Heinz-Peter Rebenstock ,  Wolfgang Holla

IPC分类号： C07D23390

CPC分类号： C07D233/90

摘要： The invention relates to a process for the preparation of compounds of the formula (I) in which R(2) and R(3) independently of one another are —SR(4) or —COOR(5) and R(1), R(4) and R(5) have the meaning indicated in the description, which comprises cyclizing compounds of the formula II in which R(1), R(2) and R(3) have the meaning defined above, in the presence of alkylphosphonic anhydrides to give compounds of the formula (I), then purifying these in as is known per se by salt formation and, if appropriate, subsequent recrystallization and optionally removing radicals introduced for the protection of other functional groups in a manner known per se; and their use as intermediate for the synthesis of active compounds.

摘要翻译： 本发明涉及制备式（I）化合物的方法，其中R（2）和R（3）彼此独立地为-SR（4）或-COOR（5）和R（1）， R（4）和R（5）具有说明书中指出的含义，其包括使R（1），R（2）和R（3）具有上述定义的式IIin的环化化合物在 烷基膦酸酐，得到式（I）化合物，然后如本身已知的那样通过盐形成和如果合适的话进行随后的重结晶和任选地除去引入的保护其它官能团的基团以本身已知的方式纯化; 以及它们作为合成活性化合物的中间体的用途。