IP Library Granted Patent US 9,822,064
Granted Patent B2
US 9,822,064 · App. 15/232,590 · Granted Nov 21, 2017

Methods of producing cancer treating compounds

Inventors: John K Lynch (Cedarburg, WI); Jeff Hutchison (Sheboygan, WI); Xiong Fu (Superior, CO); Kevin Kunnen (Plymouth, IN)
Assignee: Inspyr Therapeutics, Inc.
C07C227/16A61K31/365A61K47/48246C07C227/02C07C227/18C07C229/08C07C269/04C07C269/06C07C271/22C07D307/93C07K5/06104C07K5/06113
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Quick Facts
Patent No.
US 9,822,064
App. No.
15/232,590
Granted
Nov 21, 2017
Kind
B2
Abstract

Provided herein are methods of making the compound of Formula I: and certain intermediates involved in such process.

Claims (19)

1. A method of producing the compound of Formula 14

where n is an integer greater than 2, the method comprising esterify, by acid catalysis with acetyl chloride in methanol, the compound of Formula 15

to form the compound of Formula 16

react the compound of Formula 16 with Boc 2 O to form the compound of Formula 17

and

hydrolyze the compound of Formula 17 with NaOH to form the compound of Formula 14.

2. The method of claim 1 , wherein the compound of Formula 14 is Boc-12-AD (4)

3. The method of claim 1 , wherein the reaction with Boc 2 O with the compound of Formula 16 is in CH 2 Cl 2 in the presence of dimethylaminopyridine and a tertiary amine base.

4. The method of claim 3 , wherein the tertiary amine base is triethylamine.

5. The method of claim 1 , wherein the yield of the compound of Formula 14 is at least 97%.

6. A method of producing Boc-12-AD, having Formula

the method comprising esterify, by acid catalysis with acetyl chloride in methanol, 12-AD, having Formula 10

to form the compound of Formula 11

react the compound of formula 11 with Boc 2 O to form the compound of Formula 12

and

hydrolyze the compound of Formula 12 with NaOH to form the compound of Formula 4.

7. The method of claim 6 , wherein the reaction with Boc 2 O with the compound of Formula 11 is in CH 2 Cl 2 in the presence of dimethylaminopyridine and triethylamine.

8. The method of claim 1 , wherein the compound of Formula 14 comprises essentially no dimer impurities.

9. The preparation of claim 8 , wherein the compound is Boc-12-AD, having Formula 4.

Assignments (2)
CHANGE OF NAME Recorded Oct 13, 2016
From: GENSPERA, INC.
To: INSPYR THERAPEUTICS, INC.
Reel/Frame 040350/0234 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 25, 2016
From: LYNCH, JOHN K; HUTCHISON, JEFF; FU, XIONG; KUNNEN, KEVIN
To: GENSPERA, INC.
Reel/Frame 039850/0281 →
Continuity (3)
Division 14776730
Provisional Application 61791909 · Mar 15, 2013
Related Publication 20160347706A1 · Dec 1, 2016