IP Library Granted Patent US 10,633,412
Granted Patent B2
US 10,633,412 · App. 16/051,409 · Granted Apr 28, 2020

Preparation of bile acids and intermediates thereof

Inventors: Achampeta Rathan Prasad (Hyderabad, IN); Roy A. Swaringen, Jr. (Durham, NC); John Gregory Reid (Groton, MA); Robert M. Moriarty (Michiana Shores, IN); Akhila Kumar Sahoo (Hyderbad, IN)
Assignee: Allergan Sales, LLC
C07J9/005C07J1/00C07J1/0011C07J9/00C07J13/00C07J13/007C07J75/00
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Quick Facts
Patent No.
US 10,633,412
App. No.
16/051,409
Granted
Apr 28, 2020
Kind
B2
Abstract

Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

Claims (23)

1. A composition comprising a compound of formula 1.0:

and a hydrogenation catalyst.

2. The composition of claim 1 , further comprising a solvent.

3. The composition of claim 1 , wherein the hydrogenation catalyst comprises Pd/C.

4. The composition of claim 2 , wherein the solvent is DMF.

5. A composition comprising a compound of formula 1.0:

and a compound of formula 1.1:

6. A composition comprising a compound of formula 1.3:

and a two carbon olefination reagent.

7. The composition of claim 6 , further comprising a solvent.

8. The composition of claim 6 , wherein the olefination reagent is Ph 3 PCH 2 CH 3 + Br.

9. A composition comprising a compound of formula 1.3:

and a compound of formula 1.5:

10. A composition comprising a compound of formula 1.8:

wherein R is alkyl and P is a protecting group, and

an oxidizing agent.

11. The composition of claim 10 , wherein the composition further comprises a solvent.

12. The composition of claim 10 , wherein —OP is —OAc and —CO 2 R is —CO 2 Me.

13. A composition comprising a compound of formula 2.0

wherein R is alkyl and P is a protecting group, and a reducing agent.

14. The composition of claim 13 , wherein the composition further comprises a solvent.

15. The composition of claim 13 , wherein the reducing agent is lithium tri-tert-butoxyaluminum hydride.

16. The composition of claim 13 , wherein —OP is —OAc and —CO 2 R is —CO 2 Me.

Assignments (2)
MERGER AND CHANGE OF NAME Recorded Oct 8, 2019
From: KYTHERA BIOPHARMACEUTICALS, LLC; ALLERGAN SALES, LLC
To: ALLERGAN SALES, LLC
Reel/Frame 050657/0443 →
CHANGE OF NAME Recorded Oct 4, 2019
From: KYTHERA BIOPHARMACEUTICALS, INC.
To: KYTHERA BIOPHARMACEUTICALS, LLC
Reel/Frame 050638/0057 →
Priority Claims (1)
GB 0807615.0 · Apr 25, 2008 · national
Continuity (6)
Division 14696204 · Apr 24, 2015
Division 13752175 · Jan 28, 2013
Continuation 13010727 · Jan 20, 2011
Division 12613969 · Nov 6, 2009
Continuation 12153446 · May 16, 2008
Related Publication 20190048037A1 · Feb 14, 2019