Concise Synthesis of Key Intermediates of Pyriftalid
and Paquinimod via Hydrogenation Method
Posted on 2017-08-21 - 18:13
An efficient and scalable synthesis
of 7-amino-3-methylisobenzofuran-1(3H)-one
(1) and 2-amino-6-ethylbenzoic acid
(2) has been developed via a one-step catalytic hydrogenation.
The triethylammonium salt of 2-acetyl-6-nitrobenzoic acid was used
as the starting material and 1 was prepared in a biphasic
solvent system of toluene/H2O, while 2 was
obtained when the solvent was replaced with H2O. Intermediates 1 and 2 could be used to synthesize Pyriftalid
and Paquinimod, respectively.
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Li, Zhong; Li, Bing; Yang, An-Jiang; Zhang, Fu-Li (2017). Concise Synthesis of Key Intermediates of Pyriftalid
and Paquinimod via Hydrogenation Method. ACS Publications. Collection. https://doi.org/10.1021/acs.oprd.7b00177
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AUTHORS (4)
ZL
Zhong Li
BL
Bing Li
AY
An-Jiang Yang
FZ
Fu-Li Zhang