Process Research for (+)-Ambrisentan, an Endothelin-A Receptor Antagonist
An efficient and robust synthetic route to (+)-ambrisentan ((+)-AMB) was designed by recycling the unwanted isomer from the resolution mother liquors. The racemization of AMB in the absence of either acid or base in the given solvents was reported. The recovery process was developed to produce racemates with purities over 99.5%. The mechanism of the formation of the process-related impurities of (+)-AMB is also discussed in detail. (+)-AMB was obtained in 47% overall yield with >99.5% purity and 99.8% e.e. by chiral resolution with only one recycling of the mother liquors on a 100-g scale without column purification.
An improved method of preparing Anritsu tezosentan
The invention belongs to the field of chemical synthesis, and discloses an improved method used for preparing ambrisentan. According to the improved method, 2-hydroxy-3-methoxy-3,3-diphenylpropionic ester and 4,6-dimethyl-2-methylsulfonylpyrimidine are su
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(2019/05/04)
PROCESS FOR THE PREPARATION OF HIGHLY PURE AMBRISENTAN
The present invention relates to an improved and novel process for the preparation of highly pure (>99.8%) (+)-2(S)-(4,6-dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid (Ambrisentan) of formula (I).
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Paragraph 0065; 0066
(2013/03/26)
A PROCESS FOR THE PREPARATION OF HIGHLY PURE AMBRISENTAN
The present invention relates to an improved and novel process for the preparation of highly pure (>99.8 %) (+)-2(S)-(4,6-dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid (Ambrisentan) of formula (I).
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Page/Page column 11
(2011/10/10)
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