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Alogliptin benzoate manufacturer Alogliptin benzoate low price Alogliptin benzoate high quality
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High quality Alogliptin benzoate Cas 850649-62-6 with best price and good service
Specification
Items |
Specification |
Result |
Assay |
≥99% |
99.6% |
Appearance |
White crystalline powder |
White crystalline powder |
Loss on drying |
≤0.5% |
0.2% |
Heavy metals |
≤10ppm |
<10ppm |
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Product information
Alogliptin benzoate Basic information |
Pharmacological effects Detection method - high performance liquid chromatography (HPLC) method Pharmacokinetics Safety Alogliptin benzoate compound medicines |
Product Name: | Alogliptin benzoate |
Synonyms: | ALOGLIPTIN BENZOATE;2-[[6-[(3R)-3-Amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile benzoate;2-[[6-[(3R)-3-aMino-1-piperidinyl]-3,4-dihydro-3-Methyl-2,4-dioxo-1(2H)-pyriMidinyl]Methyl]-Benzonitrile Monobenzoate;SYR 322;Nesina;2-[6-[3(R)-AMinopiperidin-1-yl]-3-Methyl-2,4-dioxo-1,2,3,4-tetrahydropyriMidin-1-ylMethyl]benzonitrile benzoate;(R)-2-((6-(3-aMinopiperidin-1-yl)-3-Methyl-2,4-dioxo-3,4-dihydropyriMidin-1(2H)-yl)Methyl)benzonitrile benzoate;2-[6-[3(R)-AMinopiperidin-1-yl]-3-Methyl-2,4-dioxo-1,2,3,4-tetrahydropyriMidin-1-ylMethyl]benzonitrile benzoate Monobenzoate |
CAS: | 850649-62-6 |
MF: | C18H21N5O2.C7H6O2 |
MW: | 461.519 |
EINECS: | |
Product Categories: | Final material;Inhibitors |
Mol File: | 850649-62-6.mol |
Alogliptin benzoate Usage And Synthesis |
Type 2 diabetes drugs | Alogliptin benzoate is a kind of serine protease dipeptidyl peptidase IV (DPP-IV) inhibitor developed by the Takeda Company (Japan). This product can maintain the in vivo level of glucagon-like (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) levels, stimulating the secretion of insulin, and thus playing a hypoglycemic effect. A randomized, placebo-controlled clinical trial results have showed that compared to placebo, the Alogliptin monotherapy can significantly improve the glycemic control in patients with type 2 diabetes without increasing the incidence of hypoglycemia as well as with a good tolerance. Alogliptin and its pharmaceutical composition are orally effective specific DPP-IV inhibitor following the emergence of sitagliptin and vildagliptin, providing a new and important treatment option for type 2 diabetes patients and have a wide range of application prospects. Alogliptin benzoate is officially marketed at the beginning of 2014, and is the first batch of type 2 diabetes drugs with confirmed cardiovascular safety approve in China, providing more and better choices for the treatment of type 2 diabetes. |
Pharmacological effects | Incretin is the postprandial peptide hormone produced in gastrointestinal tract and can promote the islet β cells to secrete insulin. It includes glucagon-like peptide -1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), secreted by the L cells in the ileum and colon and K cells in the duodenum, respectively. GLP-1 and GIP, as an active hormone, can be released into the blood circulation within a few minutes after food intake and further quickly degraded and inactivated by serine protease DPP-4. The in vivo postprandial incretin levels of patients of type 2 diabetes was significantly reduced, thereby preventing the inactivation of incretin to increase the duration of action for effectively lowering blood sugar. Alogliptin benzoate, as a kind of DPP-4 inhibitors, can increase the in vivo GLP-1 level via selective inhibition of DPP-4 and reduction of the inactivation of GLP-1, and thus reducing blood sugar. When the blood sugar to normal levels, they will not continue to play a hypoglycemic effect, so it can also effectively reduce the risk of hypoglycemia. Additionally, DPP-4 inhibitors can also delay gastric emptying and increase satiety, suppress appetite, and help the patients lose weight. Therefore, these drugs, while effectively reducing the blood sugar, can also reduce the risk of hypoglycemia and weight gain, further overcoming the obstacles for patients to reach standard indicators levels , bringing new hope for the treatment of diabetes. |
Synthetic method |
(1) Take 6-chloro-3-methyl uracil as a starting material; it has the alkylation reaction with 2-bromomethyl-benzonitrile under alkaline conditions, and further has substitution reaction with (R) -3- aminopiperidine di-hydrochloride to give (R) -2 - [(6- (3- amino-piperidin-1-yl) -3-methyl-2,4-dioxo-3,4-dihydro-pyrimidin-1 ( 2H)-yl) methyl] benzonitrile (A01), and then obtain the alogliptin benzoate salt through reaction with benzoic acid. This method has a total absorption rate being 56.1% with many advantages such as easy available raw materials, mild reaction condition, high purity product, less kinds of reagent, etc., This method is more suitable for industrial production. |
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