IP Library › Granted Patent US 9,233,925
Granted Patent B2
US 9,233,925 · App. 14/736,062 · Granted Jan 12, 2016

Process for preparation of roflumilast

Inventors: Yi-Jing Chen (Meishan Township, TW); Stanislaw Pikul (East Windsor, NJ); Shen-Chun Kuo (Union, NJ); Guo-dong Chu (Jiaxiang County, CN)
Assignee: ScinoPharm (Changshu) Pharmaceuticals, Ltd.
C07D213/74C07C43/2055C07C43/307C07C43/315C07D213/75C07D317/22C07D319/06
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Quick Facts
Patent No.
US 9,233,925
App. No.
14/736,062
Granted
Jan 12, 2016
Kind
B2
Abstract

The present invention provides novel processes for the preparation of N-substituted benzamides having the formula VIc: In some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided.

Claims (5)

1. A compound of formula Vc:

wherein

R l and R 2 are independently selected from the group consisting of H; C 1-6 alkyl; C 3-7 cycloalkyl; C 3-7 cycloalkylmethyl; and C 1-4 alkyl which is partially or completely substituted with fluorine.

2. The compound of claim 1 , wherein R 1 and R 2 are independently selected from the group consisting of C 3-7 cycloalkylmethyl and C 1-4 alkyl which is partially or completely substituted with fluorine.

3. A compound of claim 1 , wherein the compound of formula Vc has the formula:

Assignments (2)
CHANGE OF NAME Recorded Sep 10, 2020
From: SCINOPHARM (CHANGSHU) PHARMACEUTICAL, LTD.
To: SCIANDA (CHANGSHU) PHARMACEUTICALS, LTD.
Reel/Frame 053746/0176 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2015
From: CHEN, YI-JING; PIKUL, STANISLAW; KUO, SHEN-CHUN; CHU, GUO-DONG
To: SCINOPHARM (CHANGSHU) PHARMACEUTICALS, LTD.
Reel/Frame 035998/0676 →
Priority Claims (1)
CN PCT/CN2012/072020 · Mar 7, 2012 · national
Continuity (2)
Division 14382967
Related Publication 20150274667A1 · Oct 1, 2015