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Latest Company Case About Synthesis route of new hypoglycemic drug sitagliptin phosphate
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Synthesis route of new hypoglycemic drug sitagliptin phosphate

 Latest company case about Synthesis route of new hypoglycemic drug sitagliptin phosphate

Sitagliptin phosphate, developed by MSD, was approved by the US FDA for listing in October 2006. It is the first dipeptidyl peptidase IV (DPP-4) inhibitor used to treat type 2 diabetes. The effect of cetagliptin phosphate on type 2 diabetes is very ideal. As a new anti diabetes drug, cetagliptin phosphate is glucose dependent and has moderate hypoglycemic effect. It can increase insulin secretion without hypoglycemia, effectively reduce hunger and other advantages, and has no side effects such as nausea, vomiting, edema and increasing body mass.



Sitagliptin phosphate can enhance the body's ability to reduce excessive blood sugar levels by inhibiting the activity of this enzyme, which relatively increases the levels of naturally occurring intestinal proinsulin, including glucagon like peptide-1 and glucose dependent proinsulin peptide. This triggers the pancreas to increase insulin production and stops glucose production in the liver, ultimately reducing blood sugar concentration. This product is characterized by stimulating insulin secretion, reducing hunger, not increasing weight, nor hypoglycemia and edema. It is suitable for diabetes patients with poor blood sugar control and frequent hypoglycemia.


According to the clinical verification of 552 patients with mild to moderate type 2 diabetes, taking cetagliptin phosphate once a day and 100mg each time can reduce the glycosylated hemoglobin by 0.6% -1.1% after 12 weeks. The incidence of adverse reactions is similar to that of placebo, with the most commonly reported adverse reactions (incidence>5% and higher than placebo) being nasal congestion or runny nose, as well as sore throat, upper respiratory tract infection, and headache. Clinical studies have shown that cetagliptin phosphate, as a single drug, can significantly reduce the level of glycosylated hemoglobin (HbA1c) in patients with type 2 diabetes. When used in combination with metformin or TZDs, it has significant adjunctive therapeutic effect and can target three major defects of type 2 diabetes: insulin resistance, β Cellular dysfunction (reduced insulin release), and α Cellular dysfunction (without inhibiting liver glucose production) plays a role. But it is not suitable for the treatment of type 1 diabetes patients or diabetes ketoacidosis.



Sitagliptin phosphate is used to treat type 2 diabetes. After taking it, many patients can promote the secretion of insulin in the body, control blood sugar, and prevent the recurrence of diabetes. Some patients, after taking it, can promote the speed of cellular and blood metabolism throughout the body, eliminate accumulated toxins and waste, and also improve the sub health symptoms that appear in the body. For consumers who are allergic to this medication during use, it is not advisable to take it as it may cause symptoms such as nausea, vomiting, and dizziness. In severe cases, it can also lead to poisoning and shock. Therefore, it is recommended that consumers carefully read the instructions before taking it, and regularly go to the hospital for examination to pay attention to their physical health.



There are many synthetic routes for sitagliptin, among which the commonly used route is based on 2,4,5-Trifluorophenylacetate acid as the starting material.


Our company can supply the following intermediates. Please feel free to purchase and inquire.

Sitagliptin phosphate monohydrate CAS 654671-77-9

2,4,5-Trifluorophenyl acetic acid CAS 209995-38-0

Meldrum acid CAS 2033-24-1

3-(Trifluoromethyl)-5,6,7,8,-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine HCl CAS 762240-92-6