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. Synthesis of drugs for diabetes treatment

When preparing the intermediate of vildagliptin, HMDS is used to simultaneously protect the hydroxyl and amino groups:

2. Synthesis of antibiotics

When synthesizing cephalosporin onium salts, HMDS is used to simultaneously protect the carboxyl and amino groups through silanization:

Using hexamethyldisilazane as both the reactant and solvent in the synthesis of amikacin, under appropriate reaction conditions, the reaction time can be shortened from 20 hours to 2 hours, making the process easier to operate, with less solvent usage and environmental friendliness.

3. Synthesis of hepatitis C treatment drugs

In the preparation of the intermediate for the anti-HCV drug sofosbuvir, the carbonyl group in N-benzoylcytosine is first converted to a silyl ether using HMDS, followed by the nucleosylation reaction, thus achieving carbonyl protection:

4. Synthesis of Azvudine, an Anti-HIV and COVID-19 Drug

In the synthesis of Azvudine, starting from the 2'-fluoro-4'-azido uracil nucleoside intermediate, the 4-hydroxyl group of pyrimidine is directly converted to an amino group using HMDS and amide, resulting in the aminolysis product in one step.

In addition to the aforementioned applications as a group protecting agent, HMDS can also serve as a catalyst and an activating group for certain inert groups. For instance, during the preparation of intermediates for the broad-spectrum antiviral drug ribavirin, HMDS can be used to activate the amino group of 1H-l,2,4-triazole-3-carboxamide. The resulting silylated amino-protected intermediate can then undergo further reactions to yield the corresponding intermediate.