Springer Nature
Research on Chemical Intermediates
,  volume 39 ,  issue 5 ,  pages 2107-2113

A convenient method for the synthesis of roflumilast

Yan Lin 1
, 
Huang Peijun 2
, 
Shuai Liu 1
, 
Lifeng Sima 1
, 
Ligong Chen 1
, 
Donghua Wang 3
1
 
2
 
Tianjin Bohai Chemical Industry Group Co. Ltd, Tianjin, People’s Republic of China | 
3
 
Publication type: Journal Article
Publication date: 2012-08-07
Springer Nature
scimago Q2
wos Q2
SJR: 0.528
CiteScore: 5.7
Impact factor: 3.5
ISSN: 09226168, 15685675
General Chemistry
Abstract
A convenient synthetic method has been developed for the synthesis of roflumilast from 4-difluoromethoxy-3-hydroxybenzaldehyde and bromomethyl cyclopropane via O-alkylation, oxidation and N-acylation. With sodium hydroxide as alkali in the last step, the total yield of roflumilast can be up to 68.3 % and the purity of the target product reached 99.2 %. It was obvious that sodium hydroxide showed more economic advantage for scale-up production than sodium hydride or potassium tert-butoxide.
Found 
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GOST |
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GOST Copy
Lin Y. et al. A convenient method for the synthesis of roflumilast // Research on Chemical Intermediates. 2012. Vol. 39. No. 5. pp. 2107-2113.
GOST all authors (up to 50) Copy
Lin Y., Peijun H., Liu S., Sima L., Chen L., Wang D. A convenient method for the synthesis of roflumilast // Research on Chemical Intermediates. 2012. Vol. 39. No. 5. pp. 2107-2113.
RIS |
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RIS Copy
TY - JOUR
DO - 10.1007/s11164-012-0742-3
UR - https://doi.org/10.1007/s11164-012-0742-3
TI - A convenient method for the synthesis of roflumilast
T2 - Research on Chemical Intermediates
AU - Lin, Yan
AU - Peijun, Huang
AU - Liu, Shuai
AU - Sima, Lifeng
AU - Chen, Ligong
AU - Wang, Donghua
PY - 2012
DA - 2012/08/07
PB - Springer Nature
SP - 2107-2113
IS - 5
VL - 39
SN - 0922-6168
SN - 1568-5675
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2012_Lin,
author = {Yan Lin and Huang Peijun and Shuai Liu and Lifeng Sima and Ligong Chen and Donghua Wang},
title = {A convenient method for the synthesis of roflumilast},
journal = {Research on Chemical Intermediates},
year = {2012},
volume = {39},
publisher = {Springer Nature},
month = {aug},
url = {https://doi.org/10.1007/s11164-012-0742-3},
number = {5},
pages = {2107--2113},
doi = {10.1007/s11164-012-0742-3}
}
MLA
Cite this
MLA Copy
Lin, Yan, et al. “A convenient method for the synthesis of roflumilast.” Research on Chemical Intermediates, vol. 39, no. 5, Aug. 2012, pp. 2107-2113. https://doi.org/10.1007/s11164-012-0742-3.