139345-88-3Relevant academic research and scientific papers
A practical procedure for the large-scale preparation of methyl (2R,3S)-3-(4-methoxyphenyl) glycidate, a key intermediate for diltiazem
Furutani, Toshiyuki,Imashiro, Ritsuo,Hatsuda, Masanori,Seki, Masahiko
, p. 4599 - 4601 (2002)
A practical synthesis of methyl (2R,3S)-3-(4- methoxyphenyl)glycidate (-)-2, a key intermediate for diltiazem (1), was developed. Treatment of methyl (E)-4-methoxycinnamate 3 with chiral dioxirane, generated from chiral ketone 4, provided (-)-2 in 77% ee and 89% yield. The crude mixture of (-)-2 and 4 was efficiently separated by the use of novel and simple equipment performing a lipase-catalyzed transesterification and a continuous dissolution and crystallization to furnish the optically pure (-)-2 and recovery of 4 in 74% and 91% yield, respectively.
Process for the preparation of intermediates useful for the synthesis for benzothiazepines
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Page column 3-4, (2008/06/13)
A process for the preparation of the compounds of formula (wherein R has the meanings reported in the specification) by enzymatic transesterification of enantiomeric mixtures is described.These compounds are intermediates useful in the synthesis of Diltiazem.
