申请人:Hirata Norihiko
公开号:US20090118519A1
公开(公告)日:2009-05-07
A process for producing lactams of formula (1) below, including the step of reacting lactones of formula (2) below with imides of any of formulae (3a), (3b) and (3c) to thereby obtain corresponding carboxylic acids (step A); the step of esterifying the carboxylic acids into corresponding esters (step B); and the step of reacting the esters with amines to thereby obtain lactams of the formula (1) (step C). In the formulae (1)-(2) and (3a)-(3c), when R
3
and R
4
are simultaneously hydrogen atoms, R is a substituted methylene or optionally substituted polymethylene; when at least one of R
3
and R
4
is a substituent other than hydrogen atom, R is an optionally substituted methylene or polymethylene; each of R
3
, R
4
, R
5
and R
6
independently is a hydrogen atom, a halogen atom, cyano, etc.; each of A
1
, A
2
, A
3
, A
4
, A
5
, A
6
, A
7
, A
8
, A
9
and A
10
independently is a hydrogen atom, a halogen atom, nitro, etc.; and M is a hydrogen atom or an alkali metal atom.
以下为制备式(1)内的内酰胺的方法,包括将制备式(2)的内酯与制备式(3a)、(3b)或(3c)的亚酰胺反应,从而得到相应的羧酸(步骤A);酯化羧酸以得到相应的酯(步骤B);将酯与胺反应以得到制备式(1)的内酰胺(步骤C)。在制备式(1)-(2)和(3a)-(3c)中,当R3和R4同时为氢原子时,R为取代亚甲基或可选的取代聚亚甲基;当R3和R4中至少有一个是除氢原子以外的取代基时,R为可选的取代亚甲基或聚亚甲基;R3、R4、R5和R6中的每一个独立地是氢原子、卤素原子、氰基等;A1、A2、A3、A4、A5、A6、A7、A8、A9和A10中的每一个独立地是氢原子、卤素原子、硝基等;M为氢原子或碱金属原子。