- An improved method of preparing Anritsu tezosentan
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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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- Process Research for (+)-Ambrisentan, an Endothelin-A Receptor Antagonist
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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.
- Feng, Wei-Dong,Zhuo, Song-Ming,Yu, Jun,Zhao, Chuan-Meng,Zhang, Fu-Li
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p. 1200 - 1207
(2018/09/06)
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- Process for the Preparation of an Endothelin Receptor Antagonist
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The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.
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- PROCESS FOR THE PREPARATION OF AN ENDOTHELIN RECEPTOR ANTAGONIST
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The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.
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- Synthesis of (+)-ambrisentan via chiral ketone-catalyzed asymmetric epoxidation
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The synthesis of optically pure (+)-ambrisentan has been achieved from 3,3-diphenylacrylate in four steps with 53% overall yield and >99% ee at the >100 g scale without column purification. The chiral epoxide intermediate was prepared via asymmetric epoxi
- Peng, Xianyou,Li, Peijun,Shi, Yian
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p. 701 - 703
(2012/03/26)
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- Improved Process For The Preparation Of Endothelin Receptor Antagonists
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The present invention relates to improved processes for the preparation of Endothelin receptor antagonists, their salts and intermediates.
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- IMPROVED PROCESS FOR THE PREPARATION OF ENDOTHELIN RECEPTOR ANTAGONISTS
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The present invention relates to improved processes for the preparation of Endothelin receptor antagonists, their salts and intermediates.
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Page/Page column 21
(2010/08/05)
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- METABOLITES AND DERIVATIVES OF AMBRISENTAN
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The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is -H or -OCH3; R2is-H, lower alkyl (e.g. C1-C4 alkyl) or glyco
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Page/Page column 24-25
(2009/03/07)
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- Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists
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A novel class of endothelin-A receptor ligands was discovered by high-throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compounds are endothelin-A-selective, are orally available, and show a long duration of action.
- Riechers, Hartmut,Albrecht, Hans-Peter,Amberg, Willi,Baumann, Ernst,Bernard, Harald,B?hm, Hans-Joachim,Klinge, Dagmar,Kling, Andreas,Müller, Stefan,Raschack, Manfred,Unger, Liliane,Walker, Nigel,Wernet, Wolfgang
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p. 2123 - 2128
(2007/10/03)
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