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、糖尿病治療藥物的合成
制備維格列汀中間體時(shí),采用HMDS同時(shí)保護(hù)羥基和氨基:
2、抗生素的合成
合成頭孢烯類鎓鹽化合物時(shí),采用HMDS同時(shí)對(duì)羧基和氨基進(jìn)行硅烷化保護(hù):
以六甲基二硅氮烷作為阿米卡星合成時(shí)的反應(yīng)物及溶劑,適當(dāng)反應(yīng)條件下,反應(yīng)時(shí)間由20小時(shí)縮短至2小時(shí),易于操作,溶劑使用量少,環(huán)境友好。
3、丙肝治療藥物的合成
在制備抗丙肝病毒藥物索非布韋中間體時(shí),先用HMDS將N-苯甲?;奏ぶ械聂驶D(zhuǎn)化為硅醚,再繼續(xù)進(jìn)行核苷化反應(yīng),從而實(shí)現(xiàn)羰基的保護(hù):
4、抗艾滋病毒及新冠病毒藥物阿茲夫定的合成
在阿茲夫定的合成中,以2’-氟-4’-疊氮基尿嘧啶核苷中間體為原料,采用HMDS和酰胺直接將嘧啶4位羥基轉(zhuǎn)換成氨基,一步得到胺解產(chǎn)物。
除了上述在基團(tuán)保護(hù)劑方面的應(yīng)用外,HMDS還可以用作催化劑以及某些惰性基團(tuán)的活化基團(tuán)。例如在制備廣譜抗病毒藥物利巴韋林中間體時(shí),可先用HMDS活化1H-l,2,4-三唑-3-甲酰胺的氨基,所得硅烷化保護(hù)氨基的中間體繼續(xù)反應(yīng)得到相應(yīng)中間體。
Previous:Innovative Phenyl Solutions | Phenyl Chlorosilane series
Next:"Battle for Thirty Years" | Annual fun sports meeting |
Return list |