Abstract: A novel cost effective process for the synthesis of phosphate salts of 1-(9H-carbazol-4yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-propan-2-ol, (carvedilol phosphate) of formula (II) with high yields and purity is disclosed. More particularly, the invention discloses a process for preparation of crystalline phosphate salts of carvedilol using various phosphate forming reagents such as phosphorous pentoxide, polyphosphoric acid, dipotassium hydrogen phosphate, ammonium dihydrogen ortho phosphate, and sodium dihydrogen ortho phosphate in solvents selected from Acetonitrile, acetone and tetrahydrofuran. The solvents used to prepare solvates of carvedilol dihydrogen phosphate are methanol, ethanol and isopropyl alcohol.
Type:
Grant
Filed:
November 7, 2007
Date of Patent:
August 17, 2010
Assignee:
Wanbury Limited
Inventors:
Shankar Sanganbhatla, Jitendra Pandurang Suryavanshi, Alam Sayyed Zahid
Abstract: Disclosed herein is crystalline carvedilol dihydrogen phosphate monohydrate having high aqueous solubility and the process for preparation thereof. The invention further discloses methods for treating hypertension, congestive heart failure and angina in a mammal, using pharmaceutical compositions comprising the compound of invention.
Abstract: Disclosed herein is crystalline carvedilol dihydrogen phosphate monohydrate having high aqueous solubility and the process for preparation thereof. The invention further discloses methods for treating hypertension, congestive heart failure and angina in a mammal, using pharmaceutical compositions comprising the compound of invention.
Abstract: A novel cost effective process for the synthesis of phosphate salts of 1-(9H-carbazol-4yloxy)-3-[[2-(2-methoxyphenoxy)ethyl] amino]-propan-2-ol, (carvedilol phosphate) of formula (II) with high yields and purity is disclosed. More particularly, the invention discloses a process for preparation of crystalline phosphate salts of carvedilol using various phosphate forming reagents such as phosphorous pentoxide, polyphosphoric acid, dipotassium hydrogen phosphate, ammonium dihydrogen ortho phosphate, and sodium dihydrogen ortho phosphate in solvents selected from Acetonitrile, acetone and tetrahydrofuran. The solvents used to prepare solvates of carvedilol dihydrogen phosphate are methanol, ethanol and isopropyl alcohol.
Type:
Application
Filed:
November 7, 2007
Publication date:
November 20, 2008
Applicant:
Wanbury Limited
Inventors:
Shankar Sanganbhatla, Jitendra Pandurang Suryavanshi, Alam Sayyed Zahid