Dapagliflozin Propanediol Monohydrate; CAS 960404 -48-2

Colour
White
Shelf Life
2-3 Years
Lead Time
5-7 Working Days
Transport
Air/Express/Sea
MOQ
10g
Site Audit
Available
Certificates
ISO9001/SGS
Stocks
in Stock
Package
1kg/5kg/10kg/25kg
Purity
99%
Samples
Available
Transport Package
Drum/Bottle/Bags
Trademark
Yunbang
Origin
China
Reference Price
Please contact us for quote

Product Description

Dapagliflozin propanediol monohydrate;CAS 960404-48-2
 
Dapagliflozin Propanediol Monohydrate; CAS 960404-48-2
 
Dapagliflozin propanediol monohydrate Chemical Properties
 
Safety Information
 
MSDS Information
 
 
Dapagliflozin propanediol monohydrate Usage And Synthesis
Definition ChEBI: A hydrate that consists of dapagliflozin compounded with (S)-propylene glycol and hydrate in a (1:1:1) ratio. Used to improve glycemic control, along with diet and exercise, in adults with type 2 diabetes.
Clinical Use The most likely process-scale synthesis has been described in a literature publication and patent, and this is summarized in the scheme below. The synthesis began with global silylation glucolactone 63 to form tetrasiloxide 64. In parallel, commercial 5-bromo-2-chlorobenzoyl acid (65) was converted to the corresponding acid chloride with oxalyl ch loride. Subsequently, this acid chloride was subjected to Friedel-Crafts acylation with ethyl phenyl ether ("phenetole") in the presence of aluminum trichloride at low temperature to give benzophenone 66 in 91% yield. Next, the carbonyl functionality within 66 was removed upon treatment with triethylsilane and boron trifluoride-etherate, producing 5-bromo-2-chloro- 4'-ethoxydiphenylmethane 67 in 75% yield as the aglycon partner. Aryl bromide 67 was subjected to lithium halogen exchange conditions and subsequent exposure to lactone 64, which gave a mixture of lactols which were then immediately subjected to metha nesulfonic acid to provide glucol 68 in 85% yield. The anomeric methoxy group of 68 was reduced with triethylsilane and boron trifluoride-etherate followed by peracetylation to deliver α-C-glycoside tetra-acetate 69 in 55% (two steps) after recrystalliaztion in ethanol. Hydrolysis of polyacetate 69 with lithi m hydroxide gave dapagliflozin in quantitative yield, and upon treatment with propanediol in water, dapagliflozin propanediol hydrate (X) was produced.
Chemical Synthesis Dapagliflozin propanediol hydrate, an orally active sodium glucose cotransporter type 2 (SGLT-2) inhibitor, was developed by Bristol-Myers Squibb (BMS) and AstraZeneca for the once-daily treatment of type 2 diabetes. As opposed to competitor SGLT-2 inhibitors, dapagliflozin was not associated with renal toxicity or long-term deterioration of renal function in phase III clinical trials. The drug exhibits excellent SGLT2 potency with more than 1200 fold selectivity over the SGLT1 enzyme.
 
Dapagliflozin Propanediol Monohydrate; CAS 960404-48-2 Dapagliflozin Propanediol Monohydrate; CAS 960404-48-2 Dapagliflozin Propanediol Monohydrate; CAS 960404-48-2 Dapagliflozin Propanediol Monohydrate; CAS 960404-48-2
Company Informations:

Hunan Yunbang Pharmaceutical Co., Ltd. ( Yunbangpharm) located in Changsha High-tech Industrial Park, Hunan. It is a high-tech enterprise specializing in the research and development, production and sales of Pharmaceutical raw materials, Pharmaceutical intermediates(API) and Fine chemicals. Based in China, Yunbangpharm has been providing suitable solutions for many domestic,foreign pharmaceutical companies and traders. Excellent quality, good reputation and authentic price have won the praise of the majority of customers.
The company adheres to the corporate tenet of "We do not produce medicines, but help pharmaceutical companies make good medicines".

We can provide customers with customized processing, research and development services;
We can develop high-end Pharmaceutical and chemical products with high technical difficulties,high barriers and unique production processes;
We can provide 100 grams Grade, kilograms, and hundred kilograms of raw material pharmaceutical intermediates and other products.
We can perform -100°C to 300°C reaction.

R&D strength is the company's core competitiveness.Yunbangpharm has maintains a good cooperation relationship with many Universities and Research institutes locally, which can quickly transform R&D results into industrial production.

Our goal : To achieve the integrated upgrade of P harmaceutical intermediates, raw materials and high-end chemical products, adhere to "serving pharmaceutical companies, creating our brands" to provide customers with high-quality and low-cost pharmaceutical and chemical products, realizing Win-win cooperation and common development.

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