The preparation method of protease inhibitor
A protease inhibitor, slow technology, applied in the field of preparation of protease inhibitors, can solve the problem of few preparation methods, and achieve the effect of high purity
Active Publication Date: 2020-09-15
泉州易初生物医药科技有限公司
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Problems solved by technology
However, there are few methods for the preparation of the substance
Method used
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[0026] The implementation of the present invention will be described in detail below in conjunction with specific examples, so as to fully understand and implement the process of how to apply technical means to solve technical problems and achieve technical effects in the present invention.
[0027] Unless otherwise specified, the technical means used in the examples are conventional means well known to those skilled in the art, and the reagents and products used are also commercially available. The sources, trade names and, where necessary, listing of constituents of reagents used are indicated the first time they appear.
[0028] Embodiments of the invention are:
[0029] refer to figure 1 , the preparation method of protease inhibitor, is characterized in that, comprises following processing step:
[0030] (1) Preparation of 3,5-dichlorobenzylthiophenol:
[0031] In a dry reaction bottle, add dimethyl sulfoxide (20ml), and mix trichlorobenzene (2g), benzyl mercaptan (1.3...
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The invention relates to a Grp94-specific Hsp-90 inhibitor and provides a preparation method for a protease inhibitor to fill in gaps in the prior art. The preparation method comprises the following treatment steps: putting anhydrous dimethyl formamide into a three-necked flask, and then under the protection of nitrogen, adding 3,5-dichlorothiophenol at first, carrying out stirring to completely dissolve 3,5-dichlorothiophenol, then slowly adding sodium hydride, and carrying out a stirring reaction at room temperature for 1 h; then adding 8-bromo-9-(3-isopropylamino)-n-propyl adenine while stirring, slowly increasing a temperature to 150 DEG C after completion of the addition, and carrying out a reflux reaction for 6 h; and carrying out cooling to room temperature after completion of the reaction, slowly adding a reaction solution into water, quenching unreacted sodium hydride, carrying out extraction with a mixed solution of dichloromethane / methanol, washing an organic phase with saturated brine and a saturated ammonium chloride solution several times, then carrying out extraction with saturated sodium bicarbonate multiple times, and successively carrying out drying with anhydrousmagnesium sulfate, rotary evaporation and purification with column chromatographic column.
Description
technical field [0001] The invention relates to a Grp94-specific Hsp-90 inhibitor, in particular to a preparation method of a protease inhibitor. Background technique [0002] Grp-specific inhibitors are a very popular novel inhibitor of proteases. Grp (glucose regulated proteins) is a kind of stress protein distributed in the cavity of the endoplasmic reticulum. Its main members are Grp78 and Grp94. They participate in the folding of nascent peptide chains during protein synthesis and perform the function of molecular chaperones. Molecular chaperones play an important role in cellular function by ensuring proper folding of proteins after synthesis and their refolding under conditions of deformation stress. Molecular chaperones are an important part of the cellular response to stress. In addition, by regulating the Properly folded, chaperones play important roles in regulating cellular functions such as cell proliferation and apoptosis. Heat shock proteins (Hsp) are a clas...
Claims
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IPC IPC(8): C07D473/34
CPCC07D473/34
Inventor 陈艳辉
Owner 泉州易初生物医药科技有限公司