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Dapagliflozin propanediol monohydrate

Dapagliflozin propanediol monohydrate Structure
Dapagliflozin propanediol monohydrate structure
CAS No.
960404-48-2
Chemical Name:
Dapagliflozin propanediol monohydrate
Synonyms
Dapagliflozin propylene glycolate hydrate;Dapagliflozin propanediol hydrate;Forxiga;(2S,3R,4R,5S,6R)-2-(4-CHLORO-3-(4-ETHOXYBENZYL)PHENYL)-6-(HYDROXYMETHYL)TETRAHYDRO-2H-PYRAN-3,4,5-TRIOL COMPOUND WITH (S)-PROPANE-1,2-DIOL (1:1) HYDRATE;CS-1307;Dapaglilozin;Enzymes Pepsase;Dapagliflozin Hydrate;Dapagliflozin SC crystal;Dapagliflozin Impurity 67
CBNumber:
CB62705080
Molecular Formula:
C24H33ClO8
Molecular Weight:
484.97
MDL Number:
MFCD28167768
MOL File:
960404-48-2.mol
Last updated:2025-04-30 17:58:12
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Dapagliflozin propanediol monohydrate Properties

Melting point 74 - 78°C
storage temp. -20°C Freezer
solubility Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form Solid
color White to Off-White
optical activity [α]/D +17 to +25, c =1.0 in chloroform-d
FDA UNII 887K2391VH
UNSPSC Code 41116107
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338

Dapagliflozin propanediol monohydrate price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC D185398 DapagliflozinPropanediolHydrate 960404-48-2 100mg $640 2021-12-16 Buy
Biosynth Carbosynth MD45346 Dapagliflozin propanediol monohydrate 960404-48-2 250mg $750 2021-12-16 Buy
AK Scientific 9589AF Dapagliflozin((2S)-1,2-propanediol,hydrate) 960404-48-2 10g $1157 2021-12-16 Buy
Biosynth Carbosynth MD45346 Dapagliflozin propanediol monohydrate 960404-48-2 50mg $250 2021-12-16 Buy
Biosynth Carbosynth MD45346 Dapagliflozin propanediol monohydrate 960404-48-2 100mg $400 2021-12-16 Buy
Product number Packaging Price Buy
D185398 100mg $640 Buy
MD45346 250mg $750 Buy
9589AF 10g $1157 Buy
MD45346 50mg $250 Buy
MD45346 100mg $400 Buy

Dapagliflozin propanediol monohydrate Chemical Properties,Uses,Production

Description

Dapagliflozin propanediol monohydrate is the first approved sodium-glucose cotransporter protein 2 (SGLT2) inhibitor. It is indicated for the treatment of type 2 diabetes. When combined with diet and exercise in adults, dagliflozin helps improve glycaemic control by inhibiting glucose reabsorption in the proximal tubules of renal units and causing glycosuria. Dagliflozin can be given alone or in combination with insulin or other oral hypoglycaemic agents as adjunctive therapy.
Dagliflozin was originally approved by the FDA on 8 January 2014 for use in combination with diet and exercise to improve glycemic control in adults with type 2 diabetes. It was later approved in April 2021 to reduce the risk of declining kidney function, kidney failure, cardiovascular death and hospitalisation for heart failure in adults with chronic kidney disease.

Uses

Dapagliflozin Propanediol Hydrate is an SGLT2 inhibitor, which can be used for the treatment of diabetes.

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 chloride. 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 methanesulfonic 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 lithium hydroxide gave dapagliflozin in quantitative yield, and upon treatment with propanediol in water, dapagliflozin propanediol hydrate (X) was produced.

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.

Synthesis_960404-48-2

Dapagliflozin propanediol monohydrate Preparation Products And Raw materials

Raw materials

Preparation Products

Dapagliflozin propanediol monohydrate Suppliers

Global( 313)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Rochi Pharmaceutical Co.,Ltd. 		21-38751876 +8615000076078 info@rochipharma.com China 431 58
Hebei Chuanghai Biotechnology Co., Ltd 		+8615531157085 abby@chuanghaibio.com China 8808 58
Hebei Mujin Biotechnology Co.,Ltd 		+86 13288715578 +8613288715578 sales@hbmojin.com China 12798 58
Hebei Chuanghai Biotechnology Co,.LTD 		+86-13131129325 sales1@chuanghaibio.com China 5868 58
Henan Fengda Chemical Co., Ltd 		+86-371-86557731 +86-13613820652 info@fdachem.com China 20232 58
Hangzhou Hyper Chemicals Limited 		+86-0086-57187702781 +8613675893055 info@hyper-chem.com China 295 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 		+86-18600796368 +86-18600796368 sales@sjar-tech.com China 485 58
Shanghai Daken Advanced Materials Co.,Ltd 		+86-371-+86-371-66670886 info@dakenam.com China 19841 58
Beijing Cooperate Pharmaceutical Co.,Ltd 		010-60279497 sales01@cooperate-pharm.com CHINA 1803 55
Shanghai Time Chemicals CO., Ltd. 		+86-021-57951555 +8617317452075 jack.li@time-chemicals.com China 1803 55
Supplier Advantage
Shanghai Rochi Pharmaceutical Co.,Ltd. 		58
Hebei Chuanghai Biotechnology Co., Ltd 		58
Hebei Mujin Biotechnology Co.,Ltd 		58
Hebei Chuanghai Biotechnology Co,.LTD 		58
Henan Fengda Chemical Co., Ltd 		58
Hangzhou Hyper Chemicals Limited 		58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 		58
Shanghai Daken Advanced Materials Co.,Ltd 		58
Beijing Cooperate Pharmaceutical Co.,Ltd 		55
Shanghai Time Chemicals CO., Ltd. 		55

View Lastest Price from Dapagliflozin propanediol monohydrate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Dapagliflozin ((2S)-1,2-propanediol, hydrate) pictures 2025-04-30 Dapagliflozin ((2S)-1,2-propanediol, hydrate)
960404-48-2
 US $37.00-56.00 / mg 99.39% 10g TargetMol Chemicals Inc.
Dapagliflozin propanediol monohydrate pictures 2025-04-30 Dapagliflozin propanediol monohydrate
960404-48-2
 US $0.00-0.00 / kg 1kg 98 1000 Wuhan Circle Star Chem-medical Technology Co.,Ltd
Dapagliflozin propanediol monohydrate pictures 2025-04-30 Dapagliflozin propanediol monohydrate
960404-48-2
 US $0.00-0.00 / kg 1kg 99% 2500kg Wuhan Biocar Pharmacy CO.,Ltd.

Dapagliflozin propanediol monohydrate Spectrum

Dapagliflozin propanediol monohydrate(960404-48-2)1HNMR

960404-48-2(Dapagliflozin propanediol monohydrate)Related Search:

Dapagliflozin Impurity 4 (Mixture of Diastereomers) Dapagliflozin Impurity D Dapagliflozin Impurity 1 Dagliflozin (S)-propylene glycol hydrate (2R,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxyMethyl)tetrahydro-2H-pyran-3,4,5-triol
Ortho-Isomer of Dapagliflozin 4,4'-dichloro-3,3'-bis(4-ethoxybenzyl)-1,1'-biphenyl Dapagliflozin Impurity 21 Dapagliflozin Open Ring Dapagliflozin Impurity G
4,4''-Diethoxybenzil 2-Propanone, 1-(2-hydroxypropoxy)- (9CI) Dapagliflozin Impurity 46 (2,5-dibromophenyl)(4-ethoxyphenyl)methanone Dapagliflozin Impurity (MW:423Da)
(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3- (4-methoxybenzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4- hydroxybenzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate Dapagliflozin Impurity 28

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Dapagliflozin (S)-Propylene Glycol Hydrate Dag column net a water glycol Dapagliflozin,(2S)-1,2-propanediol, hydrate (1:1:1) Dapagliflozin ((2S)-1,2-propanediol, hydrate)###461432-26-8###Dapagliflozin Dapagliflozin ((2S)-1,2-propanediol, hydrate) BMS 512148 (2S)-1,2-propanediol CS-1307 Dapragliflozin Propanediol Monohydrate (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-glucitol compound with (2S)-1,2-Propanediol (1:1), Monohydrate (9CI) (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl Dapagliflozin Impurity 67 BMS-512148 (2S)-1,2-propanediol, hydrate Enzymes Pepsase Dapagliflozin (API) (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-glucitol, compounded with (2S)-1,2-propanediol, hydrate (1:1:1) Dapagliflozin propanediol hydrate Dapagliflozin propylene glycolate hydrate Forxiga (2S,3R,4R,5S,6R)-2-(4-CHLORO-3-(4-ETHOXYBENZYL)PHENYL)-6-(HYDROXYMETHYL)TETRAHYDRO-2H-PYRAN-3,4,5-TRIOL COMPOUND WITH (S)-PROPANE-1,2-DIOL (1:1) HYDRATE (2S)-propane-1,2-diol (2S,3R,4R,5S,6R)-2-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-6-(hydroxymethyl)oxane-3,4,5-triol hydrate Dapaglilozin Dapagliflozin Hydrate Dapagliflozin Monohydrate In-House Dapagliflozin SC crystal (2S,3R,4R,5S,6R)-2-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (S)-propane-1,2-diol hydrate Dapagliflozin ((2S)-1,2-propanediol, hydrate), 10 mM in DMSO Dapagliflozin propanediol monohydrate - Bio-X ? 960404-48-2 496040-08-2 C21H25ClO6C3H8O2H2O C24H35ClO9 C3H8O2C21H25ClO6H2O API 960404-48-2