公开(公告)号：EP2215083A2

公开(公告)日：2010-08-11

申请号：EP07870533.2

申请日：2007-12-07

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, bandi ,  RATHNAKAR REDDY, kura ,  RAJI REDDY, rapolu ,  MURALIDHARA REDDY, dasari ,  RAMAKRISHNA REDDY, matta

IPC分类号： C07D403/10

CPC分类号： C07D403/10 ,  C07D235/02

摘要： The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield.

公开(公告)号：EP2057144A2

公开(公告)日：2009-05-13

申请号：EP06809939.9

申请日：2006-09-01

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, bandi ,  RATHNAKAR REDDY, kura ,  RAJI REDDY, rapolu ,  MURALIDHARA REDDY, dasari ,  SUBASH CHANDER REDDY, kesireddy

IPC分类号： C07D401/12

CPC分类号： C07D231/14

摘要： The present invention discloses novel and stable polymorphs of rimonabant, its hydrates and solvates, to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention further discloses novel and stable amorphous form of rimonabant, process for its preparation and a pharmaceutical composition comprising it. The present invention also provides an improved process for preparation of rimonabant crystalline Form II. Thus, for example, rimonabant is dissolved in methylene dichloride, stirred for 10 minutes at 25 - 30
o C and then distilled off the solvent under vacuum at 40
o C. The resulting residue is stirred with water and the separated solid is collected at 25 - 30
o C to give a stable crystalline rimonabant hydrate.