IP Library Granted Patent US 10,286,504
Granted Patent B2
US 10,286,504 · App. 15/914,597 · Granted May 14, 2019

Synthesis of paracetamol (acetaminophen) from biomass-derived p-hydroxybenzamide

Inventors: John Ralph (Madison, WI); Steven Karlen (Verona, WI); Justin Mobley (Cottage Grove, WI)
Assignee: Wisconsin Alumni Research Foundation
B23P19/04B60K3/02B60K15/03006B60L11/1816B60L11/1827B60L11/1838B60L11/1851B60L11/1881C07C213/02C07C231/10G05D23/1904H01M8/04925H01M8/10H01M16/006B60K2015/03019B60K2015/03026C07B2200/09H01M2220/20H01M2250/20Y02B90/12Y02T10/7005Y02T90/32
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Quick Facts
Patent No.
US 10,286,504
App. No.
15/914,597
Granted
May 14, 2019
Kind
B2
Abstract

Disclosed is a method to make N-acetyl-p-aminophenol. The method includes steps for converting biomass-derived p-hydroxybenzoates to p-hydroxybenzamide, then to p-aminophenol; and then N-acetylating the p-aminophenol.

Claims (35)

1. A method to make N-acetyl-p-aminophenol, the method comprising:

(a) converting p-hydroxybenzamide to p-aminophenol; and then

(b) N-acetylating at least a portion of the p-aminophenol to yield N-acetyl-p-aminophenol.

2. The method of claim 1 , wherein, step (a) comprises contacting the p-hydroxybenzamide with a hypohalite salt to cause a Hofmann-style rearrangement reaction, thereby yielding p-aminophenol.

3. The method of claim 1 , wherein step (b) comprises contacting the p-aminophenol with acetic anhydride and water for a time and at a temperature to yield N-acetyl-p-aminophenol.

4. The method of claim 1 , wherein, step (a) comprises contacting the p-hydroxybenzamide with a hypohalite salt to cause a Hofmann-style rearrangement reaction, thereby yielding p-aminophenol; and

step (b) comprises contacting the p-aminophenol with acetic anhydride and water for a time and at a temperature to yield N-acetyl-p-aminophenol.

5. The method of claim 4 , wherein step (a) is conducted in an alkaline aqueous or non-aqueous solvent, at a pH from about 10 to about 14, a temperature from about 20° C. to about 100° C., and for a time of from about 30 minutes to about 24 h.

6. The method of claim 4 , wherein step (b) is conducted at a temperature of from about 100° C. to about 150° C.

7. The method of claim 4 , wherein step (a) is conducted in an alkaline aqueous or non-aqueous solvent, at a pH from about 10 to about 14, a temperature from about 20° C. to about 100° C., and for a time of from about 30 minutes to about 24 h; and

step (b) is conducted at a temperature of from about 100° C. to about 150° C.

8. A method to make N-acetyl-p-aminophenol, the method comprising:

(a) providing p-hydroxybenzamide derived from p-hydroxybenzoate esters derived from biomass;

(b) converting at least a portion of the p-hydroxybenzamide to p-aminophenol; and then

(c) N-acetylating at least a portion of the p-aminophenol to yield N-acetyl-p-aminophenol.

9. The method of claim 8 , wherein, step (b) comprises contacting the p-hydroxybenzamide with a hypohalite salt to cause a Hofmann-style rearrangement reaction, thereby yielding p-aminophenol.

10. The method of claim 8 , wherein step (c) comprises contacting the p-aminophenol with acetic anhydride and water for a time and at a temperature to yield N-acetyl-p-aminophenol.

11. The method of claim 8 , wherein, step (b) comprises contacting the p-hydroxybenzamide with a hypohalite salt to cause a Hofmann-style rearrangement reaction, thereby yielding p-aminophenol; and

step (c) comprises contacting the p-aminophenol with acetic anhydride and water for a time and at a temperature to yield N-acetyl-p-aminophenol.

12. The method of claim 11 , wherein step (b) is conducted in an alkaline aqueous or non-aqueous solvent, at a pH from about 10 to about 14, a temperature from about 20° C. to about 100° C., and for a time of from about 30 minutes to about 24 h.

13. The method of claim 11 , wherein step (c) is conducted at a temperature of from about 100° C. to about 150° C.

14. The method of claim 11 , wherein step (b) is conducted in an alkaline aqueous or non-aqueous solvent, at a pH from about 10 to about 14, a temperature from about 20° C. to about 100° C., and for a time of from about 30 minutes to about 24 h; and

step (c) is conducted at a temperature of from about 100° C. to about 150° C.

15. A method to make N-acetyl-p-aminophenol from lignin, the method comprising:

(a) performing an ammonia fiber expansion process reaction or an extractive ammonia process reaction on lignin to yield p-hydroxybenzamide;

(b) converting at least a portion of the p-hydroxybenzamide from step (a) to p-aminophenol; and then

(c) N-acetylating at least a portion of the p-aminophenol from step (b) to yield N-acetyl-p-aminophenol.

16. The method of claim 15 , wherein, step (b) comprises contacting the p-hydroxybenzamide with a hypohalite salt to cause a Hofmann-style rearrangement reaction, thereby yielding p-aminophenol.

17. The method of claim 15 , wherein step (c) comprises contacting the p-aminophenol with acetic anhydride and water for a time and at a temperature to yield N-acetyl-p-aminophenol.

18. The method of claim 15 , wherein, step (b) comprises contacting the p-hydroxybenzamide with a hypohalite salt to cause a Hofmann-style rearrangement reaction, thereby yielding p-aminophenol; and

step (c) comprises contacting the p-aminophenol with acetic anhydride and water for a time and at a temperature to yield N-acetyl-p-aminophenol.

19. The method of claim 18 , wherein step (b) is conducted in an alkaline aqueous or non-aqueous solvent, at a pH from about 10 to about 14, a temperature from about 20° C. to about 100° C., and for a time of from about 30 minutes to about 24 h.

20. The method of claim 18 , wherein step (c) is conducted at a temperature of from about 100° C. to about 150° C.

21. The method of claim 18 , wherein step (b) is conducted in an alkaline aqueous or non-aqueous solvent, at a pH from about 10 to about 14, a temperature from about 20° C. to about 100° C., and for a time of from about 30 minutes to about 24 h; and

step (c) is conducted at a temperature of from about 100° C. to about 150° C.

Assignments (2)
CONFIRMATORY LICENSE Recorded Apr 17, 2019
From: UNIVERSITY OF WISCONSIN-MADISON
To: UNITED STATES DEPARTMENT OF ENERGY
Reel/Frame 048922/0899 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 8, 2018
From: RALPH, JOHN; KARLEN, STEVEN; MOBLEY, JUSTIN
To: WISCONSIN ALUMNI RESEARCH FOUNDATION
Reel/Frame 046328/0247 →
Continuity (2)
Provisional Application 62468420 · Mar 8, 2017
Related Publication 20180258030A1 · Sep 13, 2018