IP Library Granted Patent US 9,446,141
Granted Patent B2
US 9,446,141 · App. 14/776,730 · Granted Sep 20, 2016

Methods of producing cancer compounds

Inventors: John K Lynch (Cedarburg, WI); Jeff Hutchison (Sheboygan, WI); Xiong Fu (Superior, CO); Kevin Kunnen (Plymouth, IN)
Assignee: GenSpera, Inc.
A61K47/48246A61K31/365C07C227/02C07C227/18C07C229/08C07C269/04C07C269/06C07C271/22C07D307/93C07K5/06104C07K5/06113
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,446,141
App. No.
14/776,730
Granted
Sep 20, 2016
Kind
B2
Abstract

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

Claims (18)

1. A method of making the compound of Formula 1, having the chemical structure:

which comprises:

(a) reacting the compound of Formula 2, having the chemical structure:

to produce the compound of Formula 3, having the chemical structure of:

and (b) reacting the compound of Formula 3 to obtain the compound of Formula 5, having the chemical structure:

and (c) dissolving the compound of Formula 5 and mixing with trifluoroacetic acid (TFA) to obtain the compound of Formula 6, having the chemical structure of:

and (d) reacting the compound of Formula 6 with the compound of Formula 7, having the chemical structure of:

in a mixture of dimethylformamid (DMF), hydroxybenzoriazole hydrate (HOBt), and 12-ADT-TFA and (e) adding disoprophylethylamine (DIPEA) and (3-Dimethylaminoprophyl) ethylcarbomide hydrochloride (EDC-HCL) to produce the compound of Formula 8, having the chemical structure:

and (f) reacting the compound of Formula 8 to produce the compound of Formula 9, having the chemical structure of:

and (g) purifying the compound of Formula 9 to product the compound of Formula 1.

2. The method of claim 1 , wherein step (a) is performed using sodium ethoxide in ethanol.

3. The method of claim 1 , wherein step (b) is performed using 4-dimethylaminopyridine (4-DMAP), BOC-12-AD, dichloromethane and diisopropylcarbodiimide (DIC).

4. The method of claim 1 , wherein the dissolution in step (c) is performed using dichloromethane (CH 2 Cl 2 ).

5. The method of claim 1 , wherein step (f) is performed using dichloromethane, triethylsilane (Et 3 SiH) and trifluoroacetic acid.

6. The method of any of claim 1 , wherein step (g) is performed using C18 reverse-phase chromatography.

7. The method of claim 6 , wherein step (g) further comprises using a concentration column.

8. The method of claim 1 wherein: step (a) is performed using sodium ethoxide in ethanol; step (b) is performed using 4-dimethylaminopyridine (4-DMAP), the compound of Formula 4, dichloromethane and diisopropylcarbodiimide (DIC); the dissolution step in (c) is performed using dichloromethane (CH 2 Cl 2 ); step (e) is performed using dichloromethane, triethylsilane (Et 3 SiH) and trifluoroacetic acid; and (step (f) is performed using C18 reverse-phase chromatography.

9. The method of claim 8 , wherein step (f) further comprises using a concentration column.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 1, 2022
From: KOREA UNIVERSITY OF MEDIA ARTS INDUSTRY-ACADEMIC COLLABORATION FOUNDATION
To: KOREA UNIVERSITY OF MEDIA ARTS HOLDINGS CO., LTD.
Reel/Frame 060680/0463 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 19, 2015
From: LYNCH, JOHN K; HUTCHISON, JEFF; FU, XIONG; KUNNEN, KEVIN
To: GENSPERA, INC.
Reel/Frame 036606/0015 →
Continuity (2)
Provisional Application 61791909 · Mar 15, 2013
Related Publication 20160030589A1 · Feb 4, 2016