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Good Price Purity 99.9%, Empagliflozin Powder
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864070-44-0 Usage

Uses

Empagliflozin is a novel, potent and selective SGLT-2 inhibitor, improves glycaemic control and features of metabolic syndrome in diabetic rats.

Clinical research

FDA approval of empagliflozin(Jardiance) was based on the results of seven clinical trials conducted in nearly 4,500 patients with type 2 diabetes mellitus. Compared to the placebo group, all patients taking empagliflozin(Jardiance) had a significantly lower HbA1c level. The most common adverse reactions are urinary tract infections and female reproductive system infections.
On March 21, 2014, European Medicines Agency (EMA) Commission on Human Medicines recommended the approval of the sodium glucose co-transporter-2 (SGLT2) inhibitor (empagliflozin) for the treatment of adult type 2 diabetes mellitus.
On May 23, 2014, European Medicines Agency (EMA) approved for empagliflozin’s listing in Europe.
On June 16, 2014, the Boehringer-Erya Diabetes Federation released the latest data of empagliflozin Phase II clinical trials at the 74th American Diabetes Association Science Conference (ADA2014). In a two-year study, empagliflozin or glimepiride was used in the treatment of adult patients with type 2 diabetes based on metformin. The results showed that empagliflozin(Jardiance) reduced HbA1c more significantly compared with glimepiride, while the effect of weight and blood pressure treatment are equivalent with glimepiride. Another 52-week study was conducted in patients with type 2 diabetes who were still unable to adequately control blood glucose levels with high doses of insulin (with or without metformin). The results showed that compared with placebo, Jardiance significantly reduced blood glucose levels and weight, and reduced the dose of insulin, with Jardiance or placebo on a daily basis with multiple injections of insulin. In both studies, the safety of empagliflozin was consistent with previous studies.
FDA-related reports write that the drug should not be used in the following types of patients: type 1 diabetes, elevated blood or urine ketones (diabetic ketoacidosis), severe kidney damage, end-stage renal disease or dialysis patients. The most common side effects are urinary tract infections and female genital infections.
Empagliflozin can cause dehydration and lead to decreased blood pressure, resulting in patients with dizziness or fainting and decreased renal function. The risk of older patients, especially those with impaired renal function and diuretics, appears to be greater.
FDA requires Boehring and Eli Lilly to conduct four post-marketing studies: complete ongoing cardiovascular outcome trials, pediatric pharmacokinetics and pharmacodynamics trials, pediatric safety and efficacy trials, toxicity test for the drug (especially effect for renal function, bone and growth and development)

Definition

ChEBI: A C-glycosyl compound consisting of a beta-glucosyl residue having a (4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl group at the anomeric centre. A sodium-glucose co-transporter 2 inhibitor u ed as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Precautions

Do NOT use empagliflozin if:
  • you are allergic to any ingredient in empagliflozin
  • you have type 1 diabetes
  • you have high blood or urine ketone levels (diabetic ketoacidosis)
  • you have severe kidney problems or are on dialysis

References

https://en.wikipedia.org/wiki/Empagliflozin
https://www.drugs.com/cdi/empagliflozin.html

Description

Empagliflozin(trade name Jardiance) is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), and causes sugar in the blood to be excreted by the kidneys and eliminated in urine. On August 1, 2014, the Food and Drug Administration (FDA) officially approved the drug for the treatment of type 2 diabetes, to improve and control blood glucose of adults. Empagliflozin is the third SGLT-2 inhibiting drugs approved by FDA. Another two SGLT-2 inhibitor drugs, canagliflozin and dapagliflozin, belonging to Johnson Pharmaceuticals, AstraZeneca and Bristol-Myers Squibb respectively, are approved by FDA in November 2013 and January 2014 respectively. The new drug Empagliflozin’s application to FDA can be described as twists and turns. In March 2014, due to a large particle contamination incident at the empagliflozin production plant in Boehringer, the application of new drug submitted by the Boehringer-Eli Lilly Alliance was rejected by FDA. In June 2014, after reviewing the summary and material submitted by Boehring in March, confirming that the quality management and compliance system of the Boehring drug production facility was acceptable, FDA withdrew the previously issued warning letter. The Boehringer-Eli Lilly Alliance also filed an application with the FDA on June 17th.

864070-44-0SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

Product name empagliflozin

1.2 Other means of identification

Product number -
Other names X5927

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:864070-44-0 SDS

864070-44-0Synthetic route

C29H32BrClO9

C29H32BrClO9

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With water; potassium hydroxide In acetonitrile at 50 - 60℃; Reagent/catalyst;93.8%
(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-trityl triacetate

(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-trityl triacetate

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With potassium carbonate In tetrahydrofuran at 40 - 45℃;93%
With sodium hydroxide In methanol at 20℃; for 1h;91.7%
With lithium hydroxide In methanol; water at 0 - 5℃; Reagent/catalyst;89.2%
C51H43ClO11

C51H43ClO11

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With sodium methylate In tetrahydrofuran at 40 - 45℃;90%
C43H59ClO11

C43H59ClO11

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With lithium hydroxide In ethanol; water at 40 - 45℃;87%
(2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol
1279691-36-9

(2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With triethylsilane; aluminum (III) chloride In dichloromethane; acetonitrile82.5%
With triethylsilane; aluminum (III) chloride In dichloromethane; acetonitrile at -5 - 10℃; for 2h; Large scale;78%
Stage #1: (2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol With aluminum (III) chloride In dichloromethane; acetonitrile at 5℃; for 0.5h; Large scale;
Stage #2: With triethylsilane In dichloromethane; acetonitrile at 10℃; for 2h; Large scale;
78%
C40H63ClO7Si2

C40H63ClO7Si2

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Stage #1: C40H63ClO7Si2 With tetrabutyl ammonium fluoride In tetrahydrofuran at 60℃; for 6h; Large scale;
Stage #2: With ethanol In toluene at 0 - 75℃; for 2.5h; Large scale;
81%
2,3,4,6-tetra-O-benzyl-1-deoxy-1-((S)-(4-chloro-3-(4-(tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-β-D-glucopyranose

2,3,4,6-tetra-O-benzyl-1-deoxy-1-((S)-(4-chloro-3-(4-(tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-β-D-glucopyranose

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With palladium 10% on activated carbon; hydrogen In methanol at 20℃; for 18h; Reagent/catalyst;80%
(3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran
915095-94-2

(3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran

(3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one
32469-28-6, 55515-28-1, 55515-29-2, 32384-65-9

(3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Stage #1: (3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran With isopropylmagnesium chloride; lithium chloride In tetrahydrofuran at -21 - -15℃; for 1.83333h;
Stage #2: (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one In dichloromethane; acetonitrile at -25 - -13℃; for 2.91667h;
73%
Stage #1: (3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran With isopropylmagnesium chloride; lithium chloride In tetrahydrofuran at -21 - -15℃; for 1.83333h; Industry scale;
Stage #2: (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one In tetrahydrofuran at -25 - -18℃; for 2.91667h; Industry scale;
Stage #3: With citric acid In water at -13 - 19℃; Product distribution / selectivity; Industry scale;
73%
C25H31ClO8

C25H31ClO8

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With triethylsilane; boron trifluoride diethyl etherate In dichloromethane; acetonitrile at -20 - 0℃;71.7%
C23H27ClO8

C23H27ClO8

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With triethylsilane; boron trifluoride diethyl etherate In acetonitrile at 0 - 25℃; Inert atmosphere; Large scale;60%
(2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-hydroxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
864070-37-1

(2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-hydroxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

(R)-tetrahydrofuran-3-yl 4-methylbenzenesulfonate
219823-47-9

(R)-tetrahydrofuran-3-yl 4-methylbenzenesulfonate

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With caesium carbonate In N,N-dimethyl-formamide at 75℃; for 21h;57%
With caesium carbonate In N,N-dimethyl-formamide at 75℃; for 18h;49%
With caesium carbonate In N,N-dimethyl-formamide at 75℃; for 18h;49%
With caesium carbonate at 25 - 40℃;
With caesium carbonate In N,N-dimethyl-formamide at 30 - 45℃; for 24h;0.55 kg
1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-D-glucopyranoside
1417573-74-0

1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-D-glucopyranoside

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With triethylsilane; aluminum (III) chloride In dichloromethane; acetonitrile at 20 - 25℃;57%
methyl-1-C-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl)-D-glucopyranoside
915095-96-4

methyl-1-C-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl)-D-glucopyranoside

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
With triethylsilane; boron trifluoride diethyl etherate In dichloromethane; acetonitrile at -20 - 10℃; for 2h; Product distribution / selectivity;
Multi-step reaction with 3 steps
1: trimethylsilan; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - -30 °C
2: isopropyl alcohol; dichloromethane / 40 - 50 °C
3: ethyl acetate; water / 25 - 50 °C
View Scheme
Multi-step reaction with 3 steps
1: dmap / dichloromethane; pyridine / -5 - 30 °C / Large scale
2: boron trifluoride diethyl etherate; triethylsilane / acetonitrile; water / 0 - 10 °C / Large scale
3: lithium hydroxide / tetrahydrofuran; methanol / 10 - 40 °C
View Scheme
fluorobenzene
462-06-6

fluorobenzene

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: oxalyl dichloride / N,N-dimethyl-formamide / 5 h / 25 - 30 °C
1.2: 6 h / 20 - 30 °C
2.1: potassium tert-butylate / tetrahydrofuran / 4 h / 16 - 25 °C
2.2: 1.83 h / 20 - 21 °C
3.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C
4.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C
4.2: 2.92 h / -25 - -13 °C
View Scheme
Multi-step reaction with 4 steps
1.1: oxalyl dichloride; aluminum (III) chloride / N,N-dimethyl-formamide / 25 - 45 °C / Industry scale
2.1: potassium tert-butylate / tetrahydrofuran / 4 h / 16 - 25 °C / Industry scale
3.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C / Industry scale
3.2: 20 - 51 °C / Industry scale
4.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C / Industry scale
4.2: 2.92 h / -25 - -18 °C / Industry scale
4.3: -13 - 19 °C / Industry scale
View Scheme
Multi-step reaction with 4 steps
1.1: potassium tert-butylate / tetrahydrofuran; tert-butyl alcohol / 1.5 h / 0 - 10 °C / Inert atmosphere; Large scale
2.1: aluminum (III) chloride / ethyl acetate / 9 h / 78 °C / Cooling with ice; Large scale
3.1: n-butyllithium / tetrahydrofuran; toluene; hexane / 3 h / -78 °C / Inert atmosphere; Large scale
3.2: 10 h / 0 - 40 °C / Inert atmosphere; Large scale
4.1: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 2 h / -5 - 10 °C / Large scale
View Scheme
Multi-step reaction with 4 steps
1.1: potassium tert-butylate / tetrahydrofuran / 1 h / 0 - 10 °C / Inert atmosphere; Large scale
2.1: ethyl acetate / 0.5 h / Cooling with ice; Large scale
2.2: 8.5 h / 78 °C / Cooling with ice; Large scale
3.1: n-butyllithium / tetrahydrofuran; toluene / 1 h / -78 °C / Large scale
3.2: 3 h / -78 °C / Large scale
3.3: 10 h / 0 - 40 °C / Large scale
4.1: aluminum (III) chloride / dichloromethane; acetonitrile / 0.5 h / 5 °C / Large scale
4.2: 2 h / 10 °C / Large scale
View Scheme
2-chloro-5-iodobenzoic acid
19094-56-5

2-chloro-5-iodobenzoic acid

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: oxalyl dichloride / N,N-dimethyl-formamide / 5 h / 25 - 30 °C
1.2: 6 h / 20 - 30 °C
2.1: potassium tert-butylate / tetrahydrofuran / 4 h / 16 - 25 °C
2.2: 1.83 h / 20 - 21 °C
3.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C
4.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C
4.2: 2.92 h / -25 - -13 °C
View Scheme
Multi-step reaction with 4 steps
1.1: oxalyl dichloride; aluminum (III) chloride / N,N-dimethyl-formamide / 25 - 45 °C / Industry scale
2.1: potassium tert-butylate / tetrahydrofuran / 4 h / 16 - 25 °C / Industry scale
3.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C / Industry scale
3.2: 20 - 51 °C / Industry scale
4.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C / Industry scale
4.2: 2.92 h / -25 - -18 °C / Industry scale
4.3: -13 - 19 °C / Industry scale
View Scheme
Multi-step reaction with 8 steps
1: oxalyl dichloride; N,N-dimethyl-formamide / fluorobenzene / 2 h / 15 - 25 °C
2: aluminum (III) chloride / 1 h / 0 - 25 °C
3: potassium tert-butylate / tetrahydrofuran / 0.5 h / 7 - 10 °C
4: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 0 - 23 °C
5: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.5 h / -20 - 10 °C
6: hydrogenchloride / isopropyl alcohol / 5 h / 38 - 42 °C / pH 2
7: hydrogenchloride / isopropyl alcohol; methanol
8: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
(2-chloro-5-iodophenyl)(4-fluorophenyl)methanone
915095-86-2

(2-chloro-5-iodophenyl)(4-fluorophenyl)methanone

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: potassium tert-butylate / tetrahydrofuran / 4 h / 16 - 25 °C
1.2: 1.83 h / 20 - 21 °C
2.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C
3.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C
3.2: 2.92 h / -25 - -13 °C
View Scheme
Multi-step reaction with 3 steps
1.1: potassium tert-butylate / tetrahydrofuran / 4 h / 16 - 25 °C / Industry scale
2.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C / Industry scale
2.2: 20 - 51 °C / Industry scale
3.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C / Industry scale
3.2: 2.92 h / -25 - -18 °C / Industry scale
3.3: -13 - 19 °C / Industry scale
View Scheme
Multi-step reaction with 6 steps
1: potassium tert-butylate / tetrahydrofuran / 0.5 h / 7 - 10 °C
2: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 0 - 23 °C
3: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.5 h / -20 - 10 °C
4: hydrogenchloride / isopropyl alcohol / 5 h / 38 - 42 °C / pH 2
5: hydrogenchloride / isopropyl alcohol; methanol
6: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
Multi-step reaction with 6 steps
1: potassium tert-butylate / tetrahydrofuran / 2 - 10 °C
2: sodium tetrahydroborate / ethanol / 20 - 25 °C
3: methanesulfonic acid / 20 - 30 °C
4: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
5: methanesulfonic acid / 20 - 25 °C
6: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 6 steps
1: potassium tert-butylate / tetrahydrofuran / 2 - 10 °C
2: sodium tetrahydroborate / ethanol / 20 - 25 °C
3: triethylamine / dichloromethane / 0 - 35 °C
4: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
5: methanesulfonic acid / 0 - 35 °C
6: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
(S)-(2-chloro-5-iodophenyl)(4-((tetrahydrofuran-3-yl)oxy)phenyl)methanone
915095-87-3

(S)-(2-chloro-5-iodophenyl)(4-((tetrahydrofuran-3-yl)oxy)phenyl)methanone

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C
2.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C
2.2: 2.92 h / -25 - -13 °C
View Scheme
Multi-step reaction with 2 steps
1.1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 18 - 26 °C / Industry scale
1.2: 20 - 51 °C / Industry scale
2.1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.83 h / -21 - -15 °C / Industry scale
2.2: 2.92 h / -25 - -18 °C / Industry scale
2.3: -13 - 19 °C / Industry scale
View Scheme
Multi-step reaction with 5 steps
1: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 0 - 23 °C
2: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.5 h / -20 - 10 °C
3: hydrogenchloride / isopropyl alcohol / 5 h / 38 - 42 °C / pH 2
4: hydrogenchloride / isopropyl alcohol; methanol
5: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
Multi-step reaction with 5 steps
1: sodium tetrahydroborate / ethanol / 20 - 25 °C
2: methanesulfonic acid / 20 - 30 °C
3: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
4: methanesulfonic acid / 20 - 25 °C
5: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 5 steps
1: sodium tetrahydroborate / ethanol / 20 - 25 °C
2: triethylamine / dichloromethane / 0 - 35 °C
3: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
4: methanesulfonic acid / 0 - 35 °C
5: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
(3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran
915095-94-2

(3S)-3-[4-[(2-chloro-5-iodophenyl)methyl]phenoxy]tetrahydrofuran

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.5 h / -20 - 10 °C
2: hydrogenchloride / isopropyl alcohol / 5 h / 38 - 42 °C / pH 2
3: hydrogenchloride / isopropyl alcohol; methanol
4: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
Multi-step reaction with 3 steps
1: lithium chloride; isopropylmagnesium chloride / tetrahydrofuran / -30 - -20 °C / Inert atmosphere; Large scale
2: hydrogenchloride / methanol; water / 4 h / 20 °C / Large scale
3: aluminum (III) chloride; triethylsilane / acetonitrile; dichloromethane
View Scheme
Multi-step reaction with 3 steps
1.1: TurboGrignard / tetrahydrofuran / 1 h / -30 - -20 °C / Inert atmosphere
1.2: 0.5 h / Inert atmosphere
2.1: hydrogenchloride / water / 1 h / 20 - 30 °C
3.1: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile
View Scheme
C35H59ClO8Si4

C35H59ClO8Si4

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: hydrogenchloride / isopropyl alcohol / 5 h / 38 - 42 °C / pH 2
2: hydrogenchloride / isopropyl alcohol; methanol
3: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
C24H29ClO8

C24H29ClO8

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: hydrogenchloride / isopropyl alcohol; methanol
2: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
2-chloro-5-iodobenzoylchloride
281652-58-2

2-chloro-5-iodobenzoylchloride

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1: aluminum (III) chloride / 1 h / 0 - 25 °C
2: potassium tert-butylate / tetrahydrofuran / 0.5 h / 7 - 10 °C
3: aluminum (III) chloride; 1,1,3,3-Tetramethyldisiloxane / toluene / 2.5 h / 0 - 23 °C
4: isopropylmagnesium chloride; lithium chloride / tetrahydrofuran / 1.5 h / -20 - 10 °C
5: hydrogenchloride / isopropyl alcohol / 5 h / 38 - 42 °C / pH 2
6: hydrogenchloride / isopropyl alcohol; methanol
7: aluminum (III) chloride; triethylsilane / dichloromethane; acetonitrile / 0.5 h / 20 - 25 °C
View Scheme
Multi-step reaction with 7 steps
1: aluminum (III) chloride / 25 °C / Inert atmosphere
2: potassium tert-butylate / tetrahydrofuran / 2 - 10 °C
3: sodium tetrahydroborate / ethanol / 20 - 25 °C
4: methanesulfonic acid / 20 - 30 °C
5: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
6: methanesulfonic acid / 20 - 25 °C
7: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 7 steps
1: aluminum (III) chloride / 25 °C / Inert atmosphere
2: potassium tert-butylate / tetrahydrofuran / 2 - 10 °C
3: sodium tetrahydroborate / ethanol / 20 - 25 °C
4: triethylamine / dichloromethane / 0 - 35 °C
5: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
6: methanesulfonic acid / 0 - 35 °C
7: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 8 steps
1: aluminum (III) chloride / chlorobenzene / 1.5 h / 5 °C / Inert atmosphere
2: aluminum (III) chloride / chlorobenzene / 5 - 60 °C / Inert atmosphere
3: 1,1,3,3-tetramethyldisilazane / chlorobenzene / 5.5 h / 5 - 25 °C
4: dmap; triethylamine / dichloromethane / 3 h / 5 - 28 °C
5: n-butyllithium / tetrahydrofuran; toluene; hexane / 4 h / -80 °C / Inert atmosphere; Large scale
6: methanesulfonic acid / tetrahydrofuran; toluene; hexane / 12.5 h / -70 - 30 °C / Inert atmosphere
7: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / 9 h / -30 - -5 °C
8: caesium carbonate / N,N-dimethyl-formamide / 24 h / 30 - 45 °C
View Scheme
(2-chloro-5-bromophenyl)(4-fluorophenyl)methanone
915095-85-1

(2-chloro-5-bromophenyl)(4-fluorophenyl)methanone

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1: potassium tert-butylate / tetrahydrofuran / 2 - 10 °C
2: sodium tetrahydroborate / ethanol / 20 - 25 °C
3: triethylamine / dichloromethane / 0 - 35 °C
4: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
5: methanesulfonic acid / 0 - 35 °C
6: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 7 steps
1.1: potassium carbonate / N,N-dimethyl-formamide / 100 - 110 °C
2.1: aluminum (III) chloride; sodium tetrahydroborate / tetrahydrofuran / 24.5 h / 0 - 60 °C
3.1: n-butyllithium / tetrahydrofuran / 1 h / -80 - -70 °C
3.2: -80 - 0 °C
4.1: sodium tetrahydroborate; cerium(III) chloride heptahydrate / methanol / 2 h / -80 - 70 °C
5.1: acetic acid / water / 100 °C
5.2: 5 h / 0 - 30 °C
6.1: potassium fluoride; trimethylsilyl trifluoromethanesulfonate / acetonitrile / -80 - -70 °C
7.1: potassium hydroxide; water / acetonitrile / 50 - 60 °C
View Scheme
Multi-step reaction with 5 steps
1: potassium tert-butylate / tetrahydrofuran / 2 h / 0 - 10 °C
2: aluminum (III) chloride; potassium borohydride / tetrahydrofuran / 6 h / 20 °C
3: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate / 1,4-dioxane / 8 h / 8 °C / Inert atmosphere
4: tetrakis(triphenylphosphine) palladium(0); potassium dihydrogenphosphate / toluene / 12 h / 105 °C
5: sodium hydroxide / methanol / 1 h / 20 °C
View Scheme
(S)-(5-bromo-2-chlorophenyl)(4-((tetrahydrofuran-3-yl)oxy)phenyl)methanone
915095-84-0

(S)-(5-bromo-2-chlorophenyl)(4-((tetrahydrofuran-3-yl)oxy)phenyl)methanone

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: sodium tetrahydroborate / ethanol / 20 - 25 °C
2: triethylamine / dichloromethane / 0 - 35 °C
3: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
4: methanesulfonic acid / 0 - 35 °C
5: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 3 steps
1.1: potassium borohydride; aluminium trichloride / tetrahydrofuran / 0.5 h / 0 - 20 °C
2.1: TurboGrignard / tetrahydrofuran / -10 - 0 °C / Cooling with ice; Inert atmosphere
2.3: 40 - 50 °C / Inert atmosphere
3.1: lithium hydroxide / ethanol; water / 40 - 45 °C
View Scheme
Multi-step reaction with 3 steps
1.1: potassium borohydride; aluminium trichloride / tetrahydrofuran / 0.5 h / 0 - 20 °C
2.1: TurboGrignard / tetrahydrofuran / 0.5 h / -10 - 0 °C / Cooling with ice; Inert atmosphere
2.2: 40 - 50 °C / Inert atmosphere
3.1: potassium carbonate / tetrahydrofuran / 40 - 45 °C
View Scheme
C17H16BrClO3

C17H16BrClO3

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: triethylamine / dichloromethane / 0 - 35 °C
2: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
3: methanesulfonic acid / 0 - 35 °C
4: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
2-chloro-5-bromobenzaldehyde
189628-37-3

2-chloro-5-bromobenzaldehyde

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
2: triethylamine / dichloromethane / 0 - 35 °C
3: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
4: methanesulfonic acid / 0 - 35 °C
5: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 5 steps
1.1: sodium tetrahydroborate / ethanol / 4 h / 20 °C / Large scale
1.2: pH 4-5 / Cooling with ice; Large scale
2.1: thionyl chloride / 3 h / 70 °C / Large scale
3.1: ethyl acetate / 0.5 h / Cooling with ice; Large scale
3.2: 8.5 h / 78 °C / Cooling with ice; Large scale
4.1: n-butyllithium / tetrahydrofuran; toluene / 1 h / -78 °C / Large scale
4.2: 3 h / -78 °C / Large scale
4.3: 10 h / 0 - 40 °C / Large scale
5.1: aluminum (III) chloride / dichloromethane; acetonitrile / 0.5 h / 5 °C / Large scale
5.2: 2 h / 10 °C / Large scale
View Scheme
(S)-3-(4-bromophenoxy)tetrahydrofuran
857854-82-1

(S)-3-(4-bromophenoxy)tetrahydrofuran

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
2: triethylamine / dichloromethane / 0 - 35 °C
3: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
4: methanesulfonic acid / 0 - 35 °C
5: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
C20H24BrClO3Si

C20H24BrClO3Si

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
2: methanesulfonic acid / 0 - 35 °C
3: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
C17H16ClIO3

C17H16ClIO3

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: triethylamine / dichloromethane / 0 - 35 °C
2: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
3: methanesulfonic acid / 0 - 35 °C
4: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
Multi-step reaction with 4 steps
1: methanesulfonic acid / 20 - 30 °C
2: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
3: methanesulfonic acid / 20 - 25 °C
4: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
C20H24ClIO3Si

C20H24ClIO3Si

empagliflozin
864070-44-0

empagliflozin

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: n-butyllithium / tetrahydrofuran; hexane / -75 - -70 °C / Inert atmosphere
2: methanesulfonic acid / 0 - 35 °C
3: triethylsilane; boron trifluoride diethyl etherate / dichloromethane; acetonitrile / -40 - 20 °C / Inert atmosphere
View Scheme
empagliflozin
864070-44-0

empagliflozin

acetic anhydride
108-24-7

acetic anhydride

(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-trityl triacetate

(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-trityl triacetate

Conditions
ConditionsYield
With pyridine; dmap In dichloromethane at 20℃; for 4h;91%
empagliflozin
864070-44-0

empagliflozin

C23H28O7

C23H28O7

Conditions
ConditionsYield
With ethanol for 0.5h; Reflux; Large scale;90%
empagliflozin
864070-44-0

empagliflozin

(2E)-but-2-enedioic acid
110-17-8

(2E)-but-2-enedioic acid

C23H27ClO7*C4H4O4

C23H27ClO7*C4H4O4

Conditions
ConditionsYield
In methanol for 1.8h; Reflux;90%
empagliflozin
864070-44-0

empagliflozin

citric acid
77-92-9

citric acid

empagliflozin citrate

empagliflozin citrate

Conditions
ConditionsYield
In ethanol for 1.5h; Solvent; Reflux;89%
In methanol for 1.8h; Reflux;85%
empagliflozin
864070-44-0

empagliflozin

L-Pyroglutamic acid
98-79-3

L-Pyroglutamic acid

C23H27ClO7*C5H7NO3

C23H27ClO7*C5H7NO3

Conditions
ConditionsYield
In methanol for 0.833333h;83%
empagliflozin
864070-44-0

empagliflozin

acetic anhydride
108-24-7

acetic anhydride

(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-2-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate

(2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-2-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate

Conditions
ConditionsYield
With potassium carbonate In 1,4-dioxane at 60℃; for 24h;61%

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