An Efficient Synthesis of 3,5-Dimethoxy-2,4-Difluorobenzoic Acid

2017 ◽  
Vol 41 (4) ◽  
pp. 239-240 ◽  
Author(s):  
Mingguang Zhang ◽  
Lin Qiu ◽  
Shuitao Yu ◽  
Zaixin Chen ◽  
Shifa Wang

3,5-Dimethoxy-2,4-difluorobenzoic acid, as a key intermediate for preparing an impurity of moxifloxacin, was synthesised from 2,3,4,5-tetrafluorobenzoic acid in moderate yield by nitration, methoxyl substitution, reduction of NO2, diazotisation and reduction. The structures of the intermediates and the target compound were identified and determined with IR, NMR and HRMS (ESI).

Synthesis ◽  
2017 ◽  
Vol 50 (04) ◽  
pp. 760-763 ◽  
Author(s):  
Radovan Šebesta ◽  
Kristína Plevová ◽  
Brigita Mudráková

An improved, short and efficient synthesis of vinylferrocene is reported. This three-step synthesis includes Friedel–Crafts acylation, reduction, and a one-pot mesylation/elimination step to afford the target compound in 62% yield over three steps.


2018 ◽  
Vol 42 (9) ◽  
pp. 471-473
Author(s):  
Shanwen Chen ◽  
Peiming Zhang ◽  
Huali Chen ◽  
Pu Zhang ◽  
Yu Yu ◽  
...  

An improved and efficient method for the synthesis of panobinostat was developed. The commercially available starting material 4-(chloromethyl)benzaldehyde was converted to ( E)-methyl 3-[4-(chloromethyl)phenyl]acrylate via the Wittig–Horner reaction and was then directly condensed with 2-(2-methyl-1 H-indol-3-yl)ethanamine to afford the key intermediate ( E)-methyl 3-[4-({[2-(2-methyl-1 H-indol-3-yl)ethyl]amino}methyl)phenyl]acrylate in a one-pot synthesis reactor. Subsequently a nucleophilic substitution reaction was carried out smoothly to generate the desired compound. The key intermediate and target compound were characterised by HRMS, 1H NMR and 13C NMR. This procedure is operationally simple and would be more suitable for industrial production.


Planta Medica ◽  
2009 ◽  
Vol 75 (09) ◽  
Author(s):  
LA Vilaseca ◽  
J Quillaguamán ◽  
L Fuentes ◽  
O Sterner
Keyword(s):  

2012 ◽  
Vol 27 (5) ◽  
pp. 495-500 ◽  
Author(s):  
Da-Wang WU ◽  
Qiu-Lin ZHANG ◽  
Tao LIN ◽  
Mao-Chu GONG ◽  
Yao-Qiang CHEN

2014 ◽  
Vol 34 (1) ◽  
pp. 243-250
Author(s):  
Jianghong DING ◽  
Le XU ◽  
Hao XU ◽  
Haihong WU ◽  
Yueming LIU ◽  
...  

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