GODTFREDSEN, SVEN ERIK,KARPINSKI, PIOTR,FENG, LILI,SUTTON, PAUL ALLEN,PRASHAD, MAHAVIR,GIRGIS, MICHAEL J
申请号：
NZ60062606
公开号：
NZ600626A
申请日:
2006.11.08
申请国别(地区):
NZ
年份:
2013
代理人:
摘要：
ABSTRACT - 600626 The disclosure relates to a method of preparing a dual-acting compound having the sum formula [S)-N-valeryl-N-{ [2-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl} -valine) ((2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester]Na1-3 x H20 in the solid form and in the form of a supramolecular complex, wherein x is 0 to 3, wherein the compound is not Trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3-methyl-2-(pentanoyl{ 2"-(tetrazol-5-ylate)biphenyl-mylmethyl} amino)butyrate]hemipentahydratethe, wherein said method comprising the steps of: (i) dissolving (S)-N-valeryl-N-{ [2-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl} -valine (an angiotensin receptor antagonist commonly known as valsartan) and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester (a neutral endopeptidase inhibitor) in a suitable solvent such as acetone (ii) dissolving a basic compound of Na in a suitable solvent, wherein the basic compound of Na is NaOH, Na2CO3, NaHCO3, NaOMe, NaOAc or NaOCHO (iii) combining the solutions obtained in steps (i) and (ii) (iv) precipitation of the solid, and drying same to obtain the dual-acting compound or alternatively obtaining the dual-acting compound by exchanging the solvent(s) employed in steps (i) and (ii) by (iva) evaporating the resulting solution to dryness (va) re-dissolving the solid in a suitable solvent such as acetone (via) precipitation of the solid and drying same to obtain the dual-acting compound.
