- Preparation method of heterobifunctional protein cross-linking agent having hydrazide structure
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The invention relates to the technical field of preparation of compounds, in particular to a preparation method of a heterobifunctional protein cross-linking agent having a hydrazide structure. The method comprises the following steps: enabling maleimide alkyl acid, i.e., a compound A to be subjected to a heating reaction under the action of a solvent and sulfoxide chloride so as to enable a carboxyl group in the structure of the compound A to be converted into acyl chloride; mixing obtained maleimide alkyl acyl chloride with a solvent and various types of compounds B, and performing an acylation reaction under the action of organic or inorganic alkali so as to generate a compound C; and removing a protecting group at the hydrazine end of the compound C under the action of a solvent and acid or alkali so as to obtain maleimide alkyl hydrazide having the hydrazide structure. According to the method involved in the invention, the cheap and readily available maleimide alkyl acid, as a starting raw material, is prepared into the maleimide alkyl hydrazide by three steps of reactions; the yield of a synthetic route is higher; a product is suitable for the research and development and production of an antibody-drug conjugate; and a synthesis method is simple and convenient to operate, safe and controllable, and suitable for industrial production.
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Paragraph 0015
(2019/04/10)
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