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Roflumilast

CAT#: H300320

CAS#: 162401-32-3

Description: Roflumilast is a drug which acts as a selective, long-acting inhibitor of the enzyme PDE-4. It has anti-inflammatory effects and is under development as an orally administered drug for the treatment of inflammatory conditions of the lungs such as asthma, and chronic obstructive pulmonary disease (COPD). In June 2010, Daxas was approved in the EU for severe COPD associated with chronic bronchitis.[9] In March 2011, Daliresp gained FDA approval in the US for reducing COPD exacerbations.

Synthetic Routes

Roflumilast - Synthetic Route 1

Synthetic reference

Ni, Feng; Li, Jianqi. A new route to Roflumilast via copper-catalyzed hydroxylation. Synthesis. Volume 44. Issue 23. Pages 3598-3602. Journal. (2012).

Roflumilast - Synthetic Route 2

Synthetic reference

Xiang, Zuo-juan; Sun, Hong-bin. Synthesis and polymorphic study of roflumilast N-oxide. Zhongguo Yaoke Daxue Xuebao. Volume 43. Issue 6. Pages 492-496. Journal. (2012).

Roflumilast - Synthetic Route 3

Synthetic reference

Huang, Huan; Huang, Qingguo; Li, Kai; Huang, Qingyun. Method for preparing roflumilast. Assignee Anhui Qingyun Pharmaceutical Co., Ltd., Peop. Rep. China. CN 109516949. (2019).

Roflumilast - Synthetic Route 4

Synthetic reference

Dong, Dandan. Roflumilast anti-inflammatory drug intermediates for inhibiting PDE4 enzyme activity. CN 108117515. (2018).

Roflumilast - Synthetic Route 5

Synthetic reference

Chen, Yu; Yang, Taotao; Gong, Tengwen. Process for preparation of high-purity Roflumilast. Assignee Shandong Luoxin Pharmaceutical Group Co., Ltd., Peop. Rep. China. CN 105254559. (2016).

Roflumilast - Synthetic Route 6

Synthetic reference

: Lin, Guoliang; Liu, Zhidong; Han, Shuo; Geng, Yuxian; Ma, Yuezhong. Method for preparing roflumilast intermediate. Assignee Beijing Winsunny Pharmaceutical Co., Ltd., Peop. Rep. China. CN 103539671. (2014).

Roflumilast - Synthetic Route 7

Synthetic reference

Gavhane, Sachin Baban; Wakade, Sanjay Maruti; Kadam, Suresh Mahadev. Novel process for the preparation of 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy) benzamide. Assignee Glenmark Generics Limited, India. IN 2011MU01345. (2014).

Roflumilast - Synthetic Route 8

Synthetic reference

Salaet Ferre, Josep; Marquillas Olondriz, Francisco. A process for the preparation of roflumilast. Assignee Interquim, S.A., Spain. WO 2014060464. (2014).

Roflumilast - Synthetic Route 9

Synthetic reference

Chen, Yi-Jing; Pikul, Stanislaw; Kuo, Shen-Chun; Chu, Guo-Dong. Process for preparation of roflumilast. Assignee ScinoPharm (Changshu) Pharmaceutical, Ltd., Peop. Rep. China. WO 2013131484. (2013).

Roflumilast - Synthetic Route 10

Synthetic reference

Li, Jianqi; Ni, Feng; Zhu, Haoyang; Su, Wenrou; Wang, Jiajing. Method to prepare 3-cyclopropylmethoxy-4-halobenzoic acid derivatives as intermediates in synthesizing roflumilast. Assignee Shanxi C&Y Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Institute of Pharmaceutical Industry. CN 102617339. (2012).