Pharmaceutical intermediates Gliclazide CAS 21187-98-4

CAS:21187-98-4

MF: C15H21N3O3S

MW:323.41

EINECS:244-260-5

Specification: 99% min Gliclazide

Sample:Gliclazide Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:White

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Gliclazide Usage and Synthesis.

Gliclazide has a stronger effect, and its mechanism is to act selectively on pancreatic β-cells to promote insulin secretion and increase insulin release after glucose intake, so that hepatic glucose production and output are suppressed.

It has a hypoglycaemic effect on adult-type diabetics and has the effect of reducing cholesterol accumulation and decreasing the plasma concentration of aortic glycerol triphosphate and fatty acids, so gliclazide can not only treat diabetic metabolic disorders, but also prevent diabetic microvascular pathology, improve retinopathy and renal function.

Uses and functions of Gliclazide.

Hypoglycaemic agents for the treatment of non-insulin-dependent diabetes mellitus

For adults with type 2 diabetes mellitus, diabetes mellitus with obesity or with vascular disease

Pharmacological Effect of Gliclazide.

1. Hypoglycaemic effect: This product is the second generation of oral sulfonylurea hypoglycaemic drugs, and its effect is more than 10 times stronger than that of methylbutylurea.

The mechanism of action is to stimulate the release of insulin from pancreatic β-cells, so that excessive blood glucose decreases. This may be due to the fact that sulfonylureas bind to the receptors on the surface of β-cells and increase their activation, as well as increase the sensitivity of peripheral target tissues to insulin.

2. Decrease platelet aggregation and adhesion and prevent fibrin deposition on microvessels.

3. Reduce cholesterol accumulation, reduce arterial plasma concentrations of glycerol triphosphate and fatty acids.

The three actions, in addition to the treatment of diabetic metabolic disorders, but also to prevent diabetic complications - vascular, retinal, renal function of the occurrence and development of lesions.

Synthesis method of Bulk Gliclazide.

Cyclopentane phthalic anhydride is used as raw material, ammoniated to obtain cyclopentane phthalimide, catalytically reduced by LiAlH4, KBH4/ZnCl2 or platinum black to obtain azabicyclo, and then nitrosation and zinc powder reduction to obtain N-amino-3-azabicyclo［3,3,O］octane hydrochloride, and finally condensed with p-toluene sulphonyl urea to obtain gliclazide.