IP Library Granted Patent US 8,143,435
Granted Patent B2
US 8,143,435 · App. 12/445,105 · Granted Mar 27, 2012

One pot process for the preparation of candesartan

Assignee: Mylan Laboratories Ltd.
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 8,143,435
App. No.
12/445,105
Granted
Mar 27, 2012
Kind
B2
Abstract

Present invention is to provide one pot synthesis of candesartan without isolating the ester intermediate.

Claims (7)

1. A one pot process for the preparation of candesartan (I) comprises: (a) reacting cyanobiphenyl benzimidazole (III) with trialkyltin or triaryltin azide in presence of an organic solvent to form candesartan ethylester (II); and (b) hydrolyzing the candesartan ethylester (II) in situ and without isolation with an alkali followed by in situ treatment with an acid to yield candesartan (I).

2. The process according to claim 1 , wherein the trialkyltin azide or triaryltin azide is trimethyltin azide, tributyltin azide or triphenyltin azide.

3. The process according to claim 2 , wherein the trialkyltin azide or triaryltin azide is tributyltin azide.

4. The process according to claim 1 , wherein organic solvent is o-xylene, toluene, dimethylformamide, or dimethylacetamide.

5. The process according to claim 4 , wherein the organic solvent is o-xylene.

6. The process according to claim 1 , wherein the alkali is sodium hydroxide or potassium hydroxide.

7. The process according to claim 6 , wherein the alkali is sodium hydroxide.

Assignments (4)
CHANGE OF NAME Recorded Jan 12, 2026
From: TIANISH LABORATORIES PRIVATE LIMITED
To: MATRIX PHARMACORP PRIVATE LIMITED
Reel/Frame 074322/0525 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 6, 2024
From: MYLAN LABORATORIES LIMITED
To: TIANISH LABORATORIES PRIVATE LIMITED
Reel/Frame 068861/0150 →
CHANGE OF NAME Recorded Feb 9, 2012
From: MATRIX LABORATORIES LIMITED
To: MYLAN LABORATORIES LIMITED
Reel/Frame 027678/0674 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2010
From: KARUSALA, NAGESWARA RAO; OM, DUTT TYAGI; TUMMALAPALLI, UMA SANKARA SASTRY; BANDARI, MOHAN; GORANTLA, SEETA RAMANJANEYULU
To: MATRIX LABORATORIES LTD.
Reel/Frame 024238/0083 →
Priority Claims (1)
IN 1869/CHE/2006 · Oct 10, 2006 · national
Continuity (1)
Related Publication 20110034701A1 · Feb 10, 2011