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filingDate 2022-06-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c96c03b784cf17ab0e9495ebaa6b8d57
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publicationDate 2022-08-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-114874156-A
titleOfInvention A kind of method for synthesizing diltiazem intermediate (2S)-cis-hydroxylactam
abstract The invention relates to a method for synthesizing a diltiazem intermediate (2S)-cis-hydroxylactam. The synthesis method firstly uses p-methoxybenzaldehyde and methyl chloroacetate as reaction substrates to prepare a racemic epoxy ester intermediate , under the action of esterase, the intermediate of racemic epoxy ester is enzymatically resolved to obtain the intermediate of L-epoxy ester, and then the ring-opening addition is carried out between the intermediate of L-epoxy ester and o-aminothiophenol The ring-opening addition reaction product is obtained, and under the action of methanesulfonic acid, the ring-opening addition reaction product will undergo ring-closing condensation to obtain a crude product (2S)-cis-hydroxylactam, and finally refined with methanol to obtain a diltiazem intermediate (2S) ‑cis‑hydroxylactam pure product. The invention has simple synthetic route, high raw material utilization rate, low production cost, and is suitable for mass production, provides a new way for the synthesis of diltiazem intermediate (2S)-cis-hydroxylactam, and has strong industrial application prospects .
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