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[3-(Aminomethyl)-oxetan-3-yl] p-methoxybenzyl carbamate p-chlorobenzoate synthetic method

A technology for p-methoxybenzyl ester and oxetane, which is applied in the field of pharmaceutical synthesis and can solve problems such as explosion, difficulty in post-processing, and inapplicability to scale-up production.

Active Publication Date: 2020-03-03
SHANGHAI ARK BIOSCI CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the synthesis route disclosed in this patent, liquid ammonia is used for substitution reaction to introduce primary amino groups into molecular fragments, but because liquid ammonia will pollute the environment and post-processing is difficult, and the substitution reaction needs to be carried out in a high-pressure reactor at 25°C There is a risk of explosion at ~30°C, so it is not suitable for industrial scale-up production

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  • [3-(Aminomethyl)-oxetan-3-yl] p-methoxybenzyl carbamate p-chlorobenzoate synthetic method

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Embodiment Construction

[0032] The synthetic method of [3-(aminomethyl)-oxetan-3-yl] carbamic acid p-methoxybenzyl p-chlorobenzoate provided by the invention, concrete reaction scheme is as follows:

[0033]

[0034] In conjunction with the above-mentioned reaction scheme, specifically comprise the following steps:

[0035] First perform step a, using a cyclic imide group to replace the bromine group of compound 1 to generate compound 2, and the cyclic imide group is phthalimide, succinimide, maleimide Any of the salts of imines. Specifically, the purpose of this step is to convert the bromoalkyl group on compound 1 into a protective imide group. The compound 1 is an intermediate in the synthesis process, which can be obtained by combining the technical solutions provided in patent WO2015110446A1. More specifically, phthalimide, succinimide, and maleimide can be used in actual reactions to form potassium salts through potassium carbonate. Those skilled in the art understand that the step a is co...

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Abstract

The invention provides a method for synthesizing p-methoxybenzyl [3-(aminomethyl)-oxetane-3-yl]carbamate p-chlorobenzoate. The method comprises the following steps: a, preparing a compound 2 from a cyclic imido group substituted compound 1, wherein the cyclic imido group is any one of phthalimide, succimide and maleimide; b, carrying out an amination reaction on a primary amine and the compound 2to generate a compound 3; and c, reacting the compound 3 with 4-chlorobenzoic acid to obtain a compound 4. A reaction route is shown in the description. The synthesis method is friendly to the environment, and is suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of medicine synthesis, in particular to a method for synthesizing [3-(aminomethyl)-oxetan-3-yl]carbamate p-methoxybenzyl p-chlorobenzoate. Background technique [0002] Patent WO2015110446 A1 discloses a synthesis method of [3-(aminomethyl)-oxetan-3-yl]carbamic acid p-methoxybenzyl ester p-chlorobenzoate. In the synthesis route disclosed in this patent, liquid ammonia is used for substitution reaction to introduce primary amino groups into molecular fragments, but because liquid ammonia will pollute the environment and post-processing is difficult, and the substitution reaction needs to be carried out in a high-pressure reactor at 25°C There is a risk of explosion at ~30°C, so it is not suitable for industrial scale-up production. Contents of the invention [0003] For the technical defect that prior art exists, the invention provides a kind of [3-(aminomethyl)-oxetane-3-yl] the synthetic method of p-methoxybenzyl ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/08
CPCC07D305/08
Inventor 许庆彭程骆玉美姚二东冯二龙
Owner SHANGHAI ARK BIOSCI CO LTD
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