IP Library › Granted Patent US 11,040,974
Granted Patent B2
US 11,040,974 · App. 16/832,067 · Granted Jun 22, 2021

Crystalline linagliptin intermediate and process for preparation of linagliptin

Inventors: Venkata Raghavendracharyulu Palle (Hyderabad, IN); Shanmughasamy Rajmahendra (Chennai, IN); Dharshan Jakkali Chandregowda (Chikkamagaluru, IN); Thangarasu Ponnusamy (Coimbatore, IN)
Assignee: BIOCON LIMITED
C07D473/04C07B2200/13
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 11,040,974
App. No.
16/832,067
Granted
Jun 22, 2021
Kind
B2
Abstract

The present invention provides novel crystalline forms B1 & B2 of linagliptin intermediate of structural formula V and methods for production of novel crystalline form of linagliptin intermediate represented by the following structural formula V.

Claims (20)

1. A crystalline form B1 of Linagliptin intermediate of formula V,

characterised by an XPRD pattern in accordance with FIG. 1 .

2. The crystalline form B1 of Linagliptin intermediate of formula V, of claim 1 having prominent peaks at 3.14±0.2, 6.31±0.2, 8.34±0.2, 10.93±0.2, 13.75±0.2 & 14.46±0.2 degrees 2θ.

3. The crystalline form B1 of Linagliptin intermediate of formula V, of claim 1 having DSC endotherms at 53.87 & 162.97° C.

4. The process for preparation of crystalline form B1 of Linagliptin intermediate of formula V, of claim 1 comprising following steps of:

a. Heating crude linagliptin intermediate of formula V in a solvent,

b. Adding a suitable anti-solvent to the reaction mass of above step at elevated temperature,

c. Heating the reaction mass to an elevated temperature,

d. Reaction mass was cooled and isolated the crystalline form of Linagliptin intermediate of formula V.

5. The process for preparation of claim 4 , wherein solvent is acetonitrile.

6. The process for preparation of claim 4 , wherein anti-solvent is water.

7. A crystalline form B2 of Linagliptin intermediate of formula V,

characterised by an XPRD pattern in accordance with FIG. 4 .

8. The crystalline form B2 of Linagliptin intermediate of formula V, of claim 7 having prominent peaks at 3.43±0.2, 8.10±0.2, 9.96±0.2 & 17.02±0.2 degrees 2θ.

9. The crystalline form B2 of Linagliptin intermediate of formula V, of claim 7 having a DSC endotherm at 168.69° C.

10. The process for preparation of crystalline form B2 of Linagliptin intermediate of formula V, of claim 7 comprising following steps of:

a. Treating crude linagliptin intermediate of formula V with preheated solvent,

b. Adding an anti-solvent to the reaction mass of above step,

c. Heating the reaction mass to an elevated temperature,

d. Reaction mass was cooled and isolated the crystalline form of Linagliptin intermediate of formula V.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2020
From: PALLE, VENKATA RAGHAVENDRACHARYULU; RAJMAHENDRA, SHANMUGHASAMY; CHANDREGOWDA, DHARSHAN JAKKALI; PONNUSAMY, THANGARASU
To: BIOCON LIMITED
Reel/Frame 053072/0227 →
Priority Claims (1)
IN 201741034292 · Sep 27, 2017 · national
Continuity (2)
Continuation PCTIB2018057484 · Sep 27, 2018
Related Publication 20200354363A1 · Nov 12, 2020