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A method for synthesizing 3-methyloxetane-3-(4-nitrophenyl) carbonate

A technology of methyloxetane and nitrophenyl, which is applied in the field of scalable synthesis of 3-methyloxetane-3-yl carbonate, can solve the difficult separation of intermediates, yield, and Applicable to industrial scale-up production and other issues, to achieve a wide range of industrial application prospects and market value, easy operation, and the effect of improving efficiency

Active Publication Date: 2020-11-27
SHANGHAI LINKCHEM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The two-step preparation method of 3-methyloxetan-3-yl (4-nitrophenyl) carbonate (2) disclosed in the patent document (WO2015142714A1) has the problem that the intermediate is not easy to separate and the yield is low, so it is not applicable for industrial scale-up production

Method used

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  • A method for synthesizing 3-methyloxetane-3-(4-nitrophenyl) carbonate
  • A method for synthesizing 3-methyloxetane-3-(4-nitrophenyl) carbonate
  • A method for synthesizing 3-methyloxetane-3-(4-nitrophenyl) carbonate

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Embodiment 1

[0022] 3-Methyloxetan-3-yl (4-nitrophenyl) carbonate synthesis, the synthetic route is:

[0023]

[0024] The synthesis steps are:

[0025] Add 400g of anhydrous tetrahydrofuran and 200g of compound A into a dry 5L three-necked reaction flask, turn on mechanical stirring, pump air to replace the nitrogen three times, cool the reaction solution to -30°C, and keep it for half an hour, slowly add the compound A to the tetrahydrofuran solution Add 1.02L of methylmagnesium bromide B with a concentration of 3M dropwise, and keep the system temperature at -20°C. After the dropwise addition, keep the system temperature at -20°C for half an hour. Under the protection of nitrogen, slowly add 560g of compound C, and keep the system temperature At -15°C, keep the temperature of the system at -20°C and stir for 1 hour after the addition of the feed, spot the plate to detect the completion of the reaction, add saturated ammonium chloride to quench the reaction, extract with saturated sal...

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Abstract

The invention discloses a method for efficiently synthesizing 3-methyl cyclobutane-3-yl-(4-nitrobenzophenone) carbonic ester. The synthetic route is as shown in the specification. The method comprisesthe following synthesis steps: 1, reacting a compound A and a compound B; and 2, adding a compound C into the reaction system of the step 1, and reacting, thereby obtaining the compound 2. The methodfor efficiently synthesizing 3-methyl cyclobutane-3-yl-(4-nitrobenzophenone) carbonic ester, disclosed by the invention, can be applied to industrial enlarged production. According to the process disclosed by the invention, cheap and relatively stable and efficient methyl magnesium bromide is adopted as a raw material, and by virtue of the one-step reaction, the reaction efficiency is greatly improved. Moreover, the method is simple in process, cheap and readily available in raw materials, easy and convenient to operate and extremely suitable for industrial large production, and has very wideindustrial application prospects and market value.

Description

technical field [0001] The invention relates to the field of synthesis of pharmaceutical intermediates, in particular to a method capable of enlarging and synthesizing 3-methyloxetan-3-yl (4-nitrophenyl) carbonate. Background technique [0002] Nicotinamide phosphoribosyltransferase (NAMPT) inhibitors are newly discovered small molecule compounds for treating tumors, such as compound 1, which is a lead compound with excellent anticancer effects. And 3-methyloxetan-3-yl (4-nitrophenyl) carbonate (2) is an important pharmaceutical intermediate for the synthesis of compound 1 (J.Med.Chem.2016,59,8345–8368 ). [0003] [0004] The two-step preparation method of 3-methyloxetan-3-yl (4-nitrophenyl) carbonate (2) disclosed in the patent document (WO2015142714A1) has the problem that the intermediate is not easy to separate and the yield is low, so it is not applicable for industrialized scale-up production. Contents of the invention [0005] Aiming at the problems existing ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/08
CPCC07D305/08
Inventor 陆茜匡逸崔晓展
Owner SHANGHAI LINKCHEM TECH CO LTD
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