IP Library Granted Patent US 8,871,932
Granted Patent B2
US 8,871,932 · App. 13/860,262 · Granted Oct 28, 2014

Process for the preparation of tadalafil

Inventors: Dattatray Bapuso Patil (Kolhapur, IN); Killol Patel (Junagadh, IN); Ashok Prasad (New Delhi, IN); Mohan Prasad (Gurgaon, IN)
Assignee: Ranbaxy Laboratories Limited
C07D471/14C07D471/12C07D471/04
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Quick Facts
Patent No.
US 8,871,932
App. No.
13/860,262
Granted
Oct 28, 2014
Kind
B2
Abstract

The present invention relates to a process for the preparation of tadalafil of Formula I, comprising reacting a D-tryptophan compound of Formula III with piperonal in sulfolane.

Claims (12)

1. A process for the preparation of tadalafil of Formula I

wherein the process comprises:

a) reacting a D-tryptophan compound of Formula III or a pharmaceutically acceptable salt thereof

 with a compound of Formula IV

 in the presence of sulfolane to obtain a cis-intermediate compound of Formula II;

b) optionally isolating the cis-intermediate compound of Formula II;

c) reacting the cis-intermediate compound of Formula II with a compound of Formula V

 in the presence of a base to obtain a compound of Formula VI;

d) reacting the compound of Formula VI with a compound of Formula VII; and

H 3 C—NH 2   Formula VII

e) isolating tadalafil of Formula I.

2. The process according to claim 1 , wherein step a) is carried out at a temperature of 50° C. to 100° C.

Assignments (2)
MERGER Recorded Jan 13, 2016
From: RANBAXY LABORATORIES LIMTED
To: SUN PHARMACEUTICAL INDUSTRIES LIMITED
Reel/Frame 037513/0475 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 29, 2013
From: PATIL, DATTATRAY B.; PATEL, KILLOL; PRASAD, ASHOK; PRASAD, MOHAN
To: RANBAXY LABORATORIES LIMITED
Reel/Frame 030307/0597 →
Priority Claims (1)
IN 1402/DEL/2007 · Jun 29, 2007 · national
Continuity (2)
Division 12666606
Related Publication 20140142309A1 · May 22, 2014