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Improve the efficiency of drug synthesis|Group protecting agent XY-602

Release Time:2023-02-01 14:46:49      Number of clicks:377

In the  drug synthesis,  it is usually  necessary to use a group protecting agent to protect the undesired functional group to form a derivative, and then restore it to the original functional group after reaching the expected structure to improve the reaction efficiency. Hexamethyldisilazane (HMDS), as a common protective agent of silylated groups, is widely used in antibiotic synthesis and the synthesis of therapeutic drugs such as hepatitis, tumor, cardiovascular and cerebrovascular diseases.  Let's  introduce the application of our product hexamethyldisilazane,XY-602, in drug synthesis.

1、糖尿病治疗药物的合成

制备维格列汀中间体时,采用HMDS同时保护羟基和氨基:

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2、抗生素的合成

合成头孢烯类鎓盐化合物时,采用HMDS同时对羧基和氨基进行硅烷化保护:

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以六甲基二硅氮烷作为阿米卡星合成时的反应物及溶剂,适当反应条件下,反应时间由20小时缩短至2小时,易于操作,溶剂使用量少,环境友好。

3、丙肝治疗药物的合成

在制备抗丙肝病毒药物索非布韦中间体时,先用HMDS将N-苯甲酰基胞嘧啶中的羰基转化为硅醚,再继续进行核苷化反应,从而实现羰基的保护:

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4、抗艾滋病毒及新冠病毒药物阿兹夫定的合成

在阿兹夫定的合成中,以2’-氟-4’-叠氮基尿嘧啶核苷中间体为原料,采用HMDS和酰胺直接将嘧啶4位羟基转换成氨基,一步得到胺解产物。

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除了上述在基团保护剂方面的应用外,HMDS还可以用作催化剂以及某些惰性基团的活化基团。例如在制备广谱抗病毒药物利巴韦林中间体时,可先用HMDS活化1H-l,2,4-三唑-3-甲酰胺的氨基,所得硅烷化保护氨基的中间体继续反应得到相应中间体。

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