A kind of synthetic method of 4-tert-butyl-5-ethyl-6-oxyethylene-1,4-oxazepane-4,5-dicarboxylate

A technology of dicarboxylate and oxazepane, applied to 4-tert-butyl-5-ethyl-6-oxyethylene-1,4-oxazepane-4,5-dicarboxylate In the field of synthesis, it can solve the problems of lack of reports and achieve the effects of easy operation, simplified operation process and cheap raw materials
CN105693652BActive Publication Date: 2019-01-08CHANGZHOU HEQUAN PHARMA CO LTD +2
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHANGZHOU HEQUAN PHARMA CO LTD
Publication Date
2019-01-08

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Abstract

The invention relates to a synthesis method of 4-tert-butyl-5-ethyl-6-oxo-1, 4-oxyaza-4, 5-dicarboxylic acid, and solves the technical problems of difficult synthesis operation and expensive raw materials in existing methods. The method includes: reacting 2-benzylaminoethanol as the starting raw material with t-butyloxycarboryl to protect amino to obtain tert-butylbenzyl(2-hydroxyethyl)carbamate, reacting the product with sodium hydride in ice bath, then reacting the reaction product with ethyl bromoacetate to obtain ethyl 2-(2-(benzyl)t-butyloxycarboryl)amine)ethoxy)acetic acid, then removing Boc with a hydrochloric acid ethyl acetate solution to obtain ethyl 2-(2-(benzylamine)ethoxy)acetic acid hydrochloride, and then in the presence of alkali, reacting the ethyl 2-(2-(benzylamine)ethoxy)acetic acid hydrochloride with ethyl bromoacetate to obtain ethyl 2-(benzyl(2-(2-ethoxy-2-oxoethoxy)ethyl)amino)acetic acid, using palladium hydroxide as the catalyst, in the presence of di-tert-butyl carbonate, removing Boc from benzyl with hydrogen to obtain ethyl 2-((t-butyloxycarboryl)(2-(2-ethoxy-2-oxoethoxy)ethyl)amino)acetic acid, and finally under a potassium tert-butoxide alkaline condition and with toluene as the solvent, conducting backflow and ring closing so as to obtain a final compound.
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Description

technical field

[0001] The invention relates to a practical synthesis method of 4-tert-butyl-5-ethyl-6-oxygenide-1,4-oxazepane-4,5-dicarboxylate. Background technique

[0002] 4-tert-butyl-5-ethyl-6-oxyylidene-1,4-oxazepane-4,5-dicarboxylate (CAS No.: 1330763-23-9) is a useful organic Synthetic intermediate, the market sales are good. However, there is a lack of reports on its industrial synthesis methods in the literature, and various derivatives with this compound as the core have important roles in organic synthesis and drug synthesis. Contents of the invention

[0003] The purpose of the present invention is to develop a kind of 4-tert-butyl-5-ethyl-6-oxygenidene-1,4-oxazepane that has raw materials easy to get, easy to operate, easy to control, and high yield. The synthesis method of -4,5-dicarboxylate mainly solves the technical problem that there is no suitable industrial synthesis method at present.

[0004] Technical solution of the present invention: a synthet...

Claims

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