申请人:Seki Masahiko
公开号:US20080119655A1
公开(公告)日:2008-05-22
The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): 1 wherein R
1
and R
2
may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R
3
represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): 2 wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.
本发明提供了一种制备生物素合成中间体的工业优势过程,并揭示了一种制备由式(I)表示的化合物的过程:其中R1和R2可以相同也可以不同,分别表示氢原子,苯基(苯环上可能有取代基),苯基甲基(苯环上可能有取代基),或三苯甲基(苯环上可能有取代基);R3表示氰基,羧基,烷氧基羰基,烷基硫氧基羰基或氨基甲酰基(可能带有取代基),或其盐,该过程包括将式(II-a)表示的化合物:其中符号具有上述定义的相同含义,或其盐进行环转化。