Practical Asymmetric Synthesis of (+)-erythro Mefloquine Hydrochloride

A highly enantioselective and cost efficient process for the synthesis of (+)-erythro mefloquine has been developed. The key step is an enantioselective reduction of pyridyl ketone KI using transfer hydrogenation with formic acid as the hydrogen source. The ratio of formic acid to NEt3 was found to...

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Bibliographic Details
Published inOrganic process research & development Vol. 16; no. 3; pp. 461 - 463
Main Authors Hems, William P, Jackson, William P, Nightingale, Peter, Bryant, Rob
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 16.03.2012
Amer Chemical Soc
Subjects
Chemistry
Chemistry, Applied
Chemistry, Organic
Physical Sciences
Science & Technology
TRANSFER HYDROGENATION
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Summary:A highly enantioselective and cost efficient process for the synthesis of (+)-erythro mefloquine has been developed. The key step is an enantioselective reduction of pyridyl ketone KI using transfer hydrogenation with formic acid as the hydrogen source. The ratio of formic acid to NEt3 was found to be very important to achieving a highly efficient process.
ISSN:1083-6160
1520-586X
DOI:10.1021/op200354f