[EN] PROCESS FOR PREPARING 2-ALKYL-3-AROYL-5-NITRO-BENZOFURANS<br/>[FR] PROCÉDÉ DE PRÉPARATION DU 2-ALKYLE-3-AROYLE-5-NITRO-BENZOFURANE
申请人:LONZA AG
公开号:WO2010040261A1
公开(公告)日:2010-04-15
The present invention relates to a process for the preparation of a compound of formula (I), wherein R1 is selected from C1-6-alkyl, C3-6-cycloalkyl and aralkyl, and wherein R2 at each occurrence independently is halogen or C1-6-alkyl, and m is an integer from 0 to 4, Q is selected from halogen, -NO2 and -NR3R4, wherein R3 and R4 are independently selected from hydrogen, C1-6-alkyl, C3-6-cycloalkyl, aryl, aralkyl, mesyl and tosyl, or wherein R3 and R4 together form a C4-6-alkylene group, Y at each occurrence is hydrogen or a hydroxy protection group W that can be hydrolytically cleaved under acidic conditions, and n is an integer from 1 to 3, and n is an integer from 1 to 3, with the proviso that n and m together are not greater than 5.
本发明涉及一种制备式(I)化合物的方法,其中R1从C1-6-烷基,C3-6-环烷基和芳基中选择,R2在每次出现时独立地为卤素或C1-6-烷基,m为0到4的整数,Q从卤素,-NO2和-NR3R4中选择,其中R3和R4独立地选择自氢,C1-6-烷基,C3-6-环烷基,芳基,芳基烷基,甲苯磺酰基和对甲苯磺酰基,或者R3和R4一起形成一个C4-6-烷基烯基,Y在每次出现时是氢或可在酸性条件下水解的羟基保护基W,n为1到3的整数,且n为1到3的整数,但须满足n和m的总和不大于5。