Florfenicol intermediate preparation method

Florfenicol intermediate preparation method

The invention discloses a florfenicol intermediate preparation method, which comprises: carrying out a reaction by using D-p-methylsulfonyl phenyl serine ethyl ester as a raw material, and reducing by using sodium borohydride as a reducing agent to obtain D-threon-2-amino-1-p-methylsulfonyl phenyl-1...

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Hauptverfasser: WANG XINGGUO, WANG TONGLONG, LIU JUN, LIAO SHIXUE, WANG QINGWEI
Format: Patent
Sprache:chi ; eng
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator WANG XINGGUO
WANG TONGLONG
LIU JUN
LIAO SHIXUE
WANG QINGWEI
description The invention discloses a florfenicol intermediate preparation method, which comprises: carrying out a reaction by using D-p-methylsulfonyl phenyl serine ethyl ester as a raw material, and reducing by using sodium borohydride as a reducing agent to obtain D-threon-2-amino-1-p-methylsulfonyl phenyl-1, 3-propylene glycol; preparing a cyclization protection reagent 1, 1-trimethyl dichloroorthoacetate from dichloroacetonitrile, methanol and hydrochloric acid; reacting D-threon-2-amino-1-p-methylsulfonyl phenyl-1, 3-propylene glycol with 1, 1-trimethyl dichloroorthoacetate to obtain the florfenicol intermediate D-threon-2-(dichloromethyl)-4, 5-dihydro-5-[4-(methylsulfonyl)-phenyl]-4-oxazole methanol. The method overcomes the defects of the prior art, shortens the reaction time, improves the yield, reduces the production cost, is simple to operate, and is suitable for industrial production. 本发明公开了一种氟苯尼考中间体的制备方法，通过以D-对甲砜基苯丝氨酸乙酯为原料进行反应，利用硼氢化钠作还原剂还原后，得到D-苏式-2-氨基-1-对甲砜基苯基-1，3-丙二醇；通过二氯乙腈、甲醇和盐酸制备环合保护试剂1，1-二氯原乙酸三甲酯；然后将D-苏
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METALLURGY
ORGANIC CHEMISTRY
title Florfenicol intermediate preparation method
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