IP Library Granted Patent US 9,802,957
Granted Patent B2
US 9,802,957 · App. 14/699,500 · Granted Oct 31, 2017

Processes of preparing a JAK1 inhibitor and new forms thereto

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Quick Facts
Patent No.
US 9,802,957
App. No.
14/699,500
Granted
Oct 31, 2017
Kind
B2
Abstract

This invention relates to processes for preparing a JAK1 inhibitor having Formula Ia: as well as new forms of the inhibitor.

Claims (11)

1. A process of preparing a compound of Formula Ia:

comprising reacting a compound of Formula Ib:

with a strong base in the presence of a solvent component, wherein the compound of Formula Ib is present in a composition comprising the compound of Formula Ib and the compound of Formula Ia prior to said reacting of said compound of Formula Ib with said strong base.

2. The process of claim 1 , wherein the strong base is an alkoxide base.

3. The process of claim 1 , wherein the strong base is an alkali metal C 1-6 alkoxide.

4. The process of claim 1 , wherein the strong base is potassium tert-butoxide.

5. The process of claim 1 , wherein the compound of Formula Ia is prepared as a compound of Formula II:

6. The process of claim 1 , wherein the solvent component comprises isopropyl alcohol.

7. The process of claim 1 , wherein the solvent component comprises isopropyl alcohol and tetrahydrofuran.

8. The process of claim 1 , wherein the reacting of the composition with the strong base is conducted at a temperature of about room temperature.

9. The process of claim 1 , wherein about 0.05 to about 0.15 equivalents of strong base is used based on 1 equivalent of the compound of Formula Ib.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2021
From: INCYTE CORPORATION
To: INCYTE CORPORATION; INCYTE HOLDINGS CORPORATION
Reel/Frame 058815/0857 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 19, 2015
From: ZHOU, JIACHENG; LIU, PINGLI; CHEN, SHILI; WU, YONGZHONG; WANG, DENGJIN; JIA, ZHONGJIANG; QIAO, LEI; FRIETZE, WILLIAM; XIA, MICHAEL; DAI, YINGRUI
To: INCYTE CORPORATION
Reel/Frame 035948/0070 →