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2135-17-3

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2135-17-3 Usage

Description

Flumethasone is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic, and vasoconstrictive properties. It functions as an agonist of glucocorticoid and mineralocorticoid receptors, exhibiting significant anti-inflammatory activity. Flumethasone is a white solid that is insoluble in water, and its mechanism of action involves inhibiting arachidonic acid's role in the biosynthesis of prostaglandins and leukotrienes.
Used in Veterinary Practice:
Flumethasone is used as an anti-inflammatory glucocorticoid for a variety of animals, helping to combat inflammatory symptoms caused by pathogens and aiding in the understanding of inflammatory mechanisms. It is also utilized to investigate novel techniques for detecting and quantifying steroid compounds within muscles.
Used in Skin Condition Treatment:
Flumethasone is used as a topical anti-inflammatory corticosteroid for the treatment of various skin conditions, including contact dermatitis, atopic dermatitis, eczema, psoriasis, diaper rash, bug bites, and other inflammation-related skin disorders.
Used in Otitis Externa and Otomycosis Treatment:
In combination with Clioquinol, Flumethasone is used as a corticosteroid for the treatment of otitis externa and otomycosis, showing a potency 420 times that of cortisone in an animal model for anti-inflammatory activity.
Used in Cortisol Assays:
Flumethasone pivalate, a topical difluorinated corticosteroid ester, is used in cortisol assays to study early porcine conceptus development, providing insights into the role of corticosteroids in early embryonic development.
Used in Cardiac Regeneration Research:
Flumethasone has been shown to impair cell cycle re-entry of cardiac cells and cardiac regeneration in zebrafish, indicating its potential use in research related to cardiac regeneration and the study of the effects of corticosteroids on heart tissue recovery post-injury.

Biological Activity

Flumethasone pivalate is a glucocorticoid receptor agonist used in studies on plasma transcortin binding. It binds to the nucleus causing a variety of genetic activations and repressions. The anti-inflammatory action of flumethasone is thought to involve lipocortins and phospholipase A2 inhibitory proteins, which results in the inhibition of arachidonic acid and the control of prostaglandin and leukotriene biosynthesis. Flumethasone suppresses the immune system due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.

Originator

Locacorten,Ciba,W. Germany,1964

Manufacturing Process

To approximately 1.3 g of hydrogen fluoride contained in a polyethylene bottle and maintained at -60°C was added 2.3 ml of tetrahydrofuran and then a solution of 500 mg (0.0012 mol) of 6α-fluoro-9β,11β-epoxy-16α-methyl- 17α,21-dihydroxy-1,4-pregnadiene-3,20-dione-21-acetate in 2 ml of methylenechloride. The steroid solution was rinsed in with an additional 1 ml of methylene chloride. The light red colored solution was then kept at approximately -30°C for 1 hour and at -10°C for 2 hours. At the end of this period it was mixed cautiously with an excess of cold sodium bicarbonate solution and the organic material extracted with the aid of additional methylene chloride. The combined extracts were washed with water, dried over anhydrous sodium sulfate and concentrated to approximately 35 ml. The solution was chromatographed over 130 g of Florisil anhydrous magnesium silicate. The column was developed with 260 ml portions of hexanes (Skellysolve B) containing increasing proportions of acetone. There was thus eluted 6α,9α-difluoro-11β,17α,21-trihydroxy-16α-methyl-1,4-pregnadiene- 3,20-dione 21-acetate which was freed of solvent by evaporation of the eluate fractions.

Therapeutic Function

Glucocorticoid, Antiinflammatory

Veterinary Drugs and Treatments

Flumethasone injection (Flucort?) is labeled in horses as indicated for: 1) Musculoskeletal conditions due to inflammation, where permanent structural changes do not exist, such as bursitis, carpitis, osselets and myositis. Following therapy an appropriate period of rest should be instituted to allow a more normal return to function of the affected part. 2) In allergic states such as hives, urticaria and insect bites. Flumethasone injection (Flucort?) is labeled in dogs as indicated for: 1) Musculoskeletal conditions due to inflammation of muscles or joints and accessory structures, where permanent structural changes do not exist, such as arthritis, osteoarthritis, the disc syndrome and myositis. In septic arthritis appropriate antibacterial therapy should be concurrently administered. 2) In certain acute and chronic dermatoses of varying etiology to help control the pruritus, irritation and inflammation associated with these conditions. The drug has proven useful in otitis externa in conjunction with topical medication for similar reasons. 3) In allergic states such as hives, urticaria and insect bites. 4) Shock and shock-like states, by intravenous administration. Flumethasone injection (Flucort?) is labeled in cats as indicated for certain acute and chronic dermatoses of varying etiology to help control the pruritus, irritation and inflammation associated with these conditions. Glucocorticoids have been used in an attempt to treat practically every malady that afflicts man or animal, but there are three broad uses and dosage ranges for use of these agents. 1) Replacement of glucocorticoid activity in patients with adrenal insufficiency, 2) as an antiinflammatory agent, and 3) as an immunosuppressive. Among some of the uses for glucocorticoids include treatment of: endocrine conditions (e.g., adrenal insufficiency), rheumatic diseases (e.g., rheumatoid arthritis), collagen diseases (e.g., systemic lupus), allergic states, respiratory diseases (e.g., asthma), dermatologic diseases (e.g., pemphigus, allergic dermatoses), hematologic disorders (e.g., thrombocytopenias, autoimmune hemolytic anemias), neoplasias, nervous system disorders (increased CSF pressure), GI diseases (e.g., ulcerative colitis exacerbations), and renal diseases (e.g., nephrotic syndrome). Some glucocorticoids are used topically in the eye and skin for various conditions or are injected intra-articularly or intra-lesionally. The above listing is certainly not complete.

Check Digit Verification of cas no

The CAS Registry Mumber 2135-17-3 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 2,1,3 and 5 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 2135-17:
(6*2)+(5*1)+(4*3)+(3*5)+(2*1)+(1*7)=53
53 % 10 = 3
So 2135-17-3 is a valid CAS Registry Number.
InChI:InChI=1/C22H28F2O5/c1-11-6-13-14-8-16(23)15-7-12(26)4-5-19(15,2)21(14,24)17(27)9-20(13,3)22(11,29)18(28)10-25/h4-5,7,11,13-14,16-17,25,27,29H,6,8-10H2,1-3H3/t11-,13?,14?,16+,17+,19+,20+,21+,22+/m1/s1

2135-17-3SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 15, 2017

Revision Date: Aug 15, 2017

1.Identification

1.1 GHS Product identifier

Product name flumethasone

1.2 Other means of identification

Product number -
Other names flumetasone

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:2135-17-3 SDS

2135-17-3Synthetic route

C24H30F2O5

C24H30F2O5

flumetasone
2135-17-3

flumetasone

Conditions
ConditionsYield
With monoperoxyphthalic acid In dichloromethane; ethyl acetate at 27℃;93%
flumethasone pivalate
2002-29-1

flumethasone pivalate

flumetasone
2135-17-3

flumetasone

Conditions
ConditionsYield
With Curvularia lunata In water at 30℃; for 72h; Yield given;
4,6 alpha,9 alpha-trifluoro-11 beta,17 alpha-dihydroxy-16 alpha-methyl-3-oxoandrosta-1,4-diene

4,6 alpha,9 alpha-trifluoro-11 beta,17 alpha-dihydroxy-16 alpha-methyl-3-oxoandrosta-1,4-diene

A

4,6 alpha,9 alpha-trifluoro-11 beta-hydroxy-16 alpha-methyl-3-oxo-17 alpha-propionyloxyandrosta-1,4-diene

4,6 alpha,9 alpha-trifluoro-11 beta-hydroxy-16 alpha-methyl-3-oxo-17 alpha-propionyloxyandrosta-1,4-diene

B

flumetasone
2135-17-3

flumetasone

Conditions
ConditionsYield
With pyridine In propionic acid anhydride
Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: potassium carbonate; water / methanol / 10 h
2: hydrogen fluoride / 5 h / -15 - -10 °C
View Scheme
epoxyparamethasone

epoxyparamethasone

flumetasone
2135-17-3

flumetasone

Conditions
ConditionsYield
With hydrogen fluoride at -15 - -10℃; for 5h;
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β,17α-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carboxylic acid
28416-82-2

6α,9α-difluoro-11β,17α-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-carboxylic acid

Conditions
ConditionsYield
With water; periodic acid In tetrahydrofuran at 20℃; for 1h;100%
With periodic acid In tetrahydrofuran; water at 0 - 20℃; for 2h;99.12%
With periodic acid In tetrahydrofuran; water at 0 - 20℃; for 5.75h;98%
2-(triphenylmethylthio)ethanoic acid
34914-36-8

2-(triphenylmethylthio)ethanoic acid

flumetasone
2135-17-3

flumetasone

flumethasone 2-(tritylmercapto)acetate

flumethasone 2-(tritylmercapto)acetate

Conditions
ConditionsYield
With dmap In dichloromethane at 20℃;98%
flumetasone
2135-17-3

flumetasone

C22H27BrF2O4

C22H27BrF2O4

Conditions
ConditionsYield
With pyridine; N-Bromosuccinimide; sulfur dioxide at 20℃; for 1h;97.3%
flumetasone
2135-17-3

flumetasone

6α,9-difluoro-11β,21-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione
2607-06-9

6α,9-difluoro-11β,21-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione

Conditions
ConditionsYield
With trimethylsilyl iodide In acetonitrile at -20℃; for 2h; Inert atmosphere;93%
flumetasone
2135-17-3

flumetasone

Triethyl orthopropionate
115-80-0

Triethyl orthopropionate

6α,9α-difluoro-11β,17,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione cyclic 17,21-(ethyl orthopropionate)
22593-09-5

6α,9α-difluoro-11β,17,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione cyclic 17,21-(ethyl orthopropionate)

Conditions
ConditionsYield
With toluene-4-sulfonic acid In N,N-dimethyl-formamide; toluene at 20℃; for 2h;90%
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β-hydroxy-16α-methylandrosta-1,4-diene-3,17-dione
25256-97-7

6α,9α-difluoro-11β-hydroxy-16α-methylandrosta-1,4-diene-3,17-dione

Conditions
ConditionsYield
In acetonitrile for 1h; Irradiation;50 % Turnov.
flumetasone
2135-17-3

flumetasone

A

6α,9α-difluoro-11β-hydroxy-16α-methylandrosta-1,4-diene-3,17-dione
25256-97-7

6α,9α-difluoro-11β-hydroxy-16α-methylandrosta-1,4-diene-3,17-dione

B

6α,9α-difluoro-11β,17α,21-trihydroxy-16α-methyl-1,5-cyclopregna-3-ene-2,20-dione
389119-99-7

6α,9α-difluoro-11β,17α,21-trihydroxy-16α-methyl-1,5-cyclopregna-3-ene-2,20-dione

Conditions
ConditionsYield
In acetonitrile Quantum yield; Further Variations:; irradiation wavelength; UV-irradiation;
In acetonitrile Quantum yield; Further Variations:; irradiation wavelength; Irradiation;
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β,17α,21-trihydroxy-16α-methyl-1,5-cyclopregna-3-ene-2,20-dione
389119-99-7

6α,9α-difluoro-11β,17α,21-trihydroxy-16α-methyl-1,5-cyclopregna-3-ene-2,20-dione

Conditions
ConditionsYield
In acetonitrile for 2.5h; Irradiation;60 % Turnov.
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β,21-dihydroxy-16α-methyl-17α-propionyloxypregna-1,4-diene-3,20-dione
22593-10-8

6α,9α-difluoro-11β,21-dihydroxy-16α-methyl-17α-propionyloxypregna-1,4-diene-3,20-dione

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 90 percent / TsOH / dimethylformamide; toluene / 2 h / 20 °C
2: 96 percent / aq. AcOH / methanol / 0.5 h / Heating
View Scheme
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β,21-dihydroxy-16α-methyl-17α-propionyloxypregn-4-ene-3,20-dione
193408-56-9

6α,9α-difluoro-11β,21-dihydroxy-16α-methyl-17α-propionyloxypregn-4-ene-3,20-dione

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: 90 percent / TsOH / dimethylformamide; toluene / 2 h / 20 °C
2: 96 percent / aq. AcOH / methanol / 0.5 h / Heating
3: 85 percent / H2 / (Ph3P)3RhCl / ethanol / 60 h / 760.05 Torr
View Scheme
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β-hydroxy-21-methylsulfonyloxy-16α-methyl-17α-propionyloxypregna-1,4-diene-3,20-dione
64272-25-9

6α,9α-difluoro-11β-hydroxy-21-methylsulfonyloxy-16α-methyl-17α-propionyloxypregna-1,4-diene-3,20-dione

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: 90 percent / TsOH / dimethylformamide; toluene / 2 h / 20 °C
2: 96 percent / aq. AcOH / methanol / 0.5 h / Heating
3: 100 percent / pyridine / 2 h
View Scheme
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β-hydroxy-21-methylsulfonyloxy-16α-methyl-17α-propionyloxypregn-4-ene-3,20-dione
193408-57-0

6α,9α-difluoro-11β-hydroxy-21-methylsulfonyloxy-16α-methyl-17α-propionyloxypregn-4-ene-3,20-dione

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: 90 percent / TsOH / dimethylformamide; toluene / 2 h / 20 °C
2: 96 percent / aq. AcOH / methanol / 0.5 h / Heating
3: 85 percent / H2 / (Ph3P)3RhCl / ethanol / 60 h / 760.05 Torr
4: 100 percent / pyridine / 2 h
View Scheme
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β-hydroxy-16α-methyl-21-(2-oxotetrahydrofuran-3-ylsulfanyl)-17α-propionyloxypregna-1,4-diene-3,20-dione

6α,9α-difluoro-11β-hydroxy-16α-methyl-21-(2-oxotetrahydrofuran-3-ylsulfanyl)-17α-propionyloxypregna-1,4-diene-3,20-dione

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: 90 percent / TsOH / dimethylformamide; toluene / 2 h / 20 °C
2.1: 96 percent / aq. AcOH / methanol / 0.5 h / Heating
3.1: 100 percent / pyridine / 2 h
4.1: NaH / tetrahydrofuran / 0.5 h / 0 °C
4.2: 17 percent / tetrahydrofuran / 22 h / 0 - 21 °C
View Scheme
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β-hydroxy-16α-methyl-21-(2-oxotetrahydrofuran-3-ylsulfanyl)-17α-propionyloxypregn-4-ene-3,20-dione

6α,9α-difluoro-11β-hydroxy-16α-methyl-21-(2-oxotetrahydrofuran-3-ylsulfanyl)-17α-propionyloxypregn-4-ene-3,20-dione

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: 90 percent / TsOH / dimethylformamide; toluene / 2 h / 20 °C
2.1: 96 percent / aq. AcOH / methanol / 0.5 h / Heating
3.1: 85 percent / H2 / (Ph3P)3RhCl / ethanol / 60 h / 760.05 Torr
4.1: 100 percent / pyridine / 2 h
5.1: NaH / tetrahydrofuran / 0.5 h / 0 °C
5.2: 43 percent / tetrahydrofuran / 22 h / 0 - 21 °C
View Scheme
trimethyl ortho-4-bromobutanoate
55444-67-2

trimethyl ortho-4-bromobutanoate

flumetasone
2135-17-3

flumetasone

C27H35BrF2O6
1207376-56-4

C27H35BrF2O6

Conditions
ConditionsYield
toluene-4-sulfonic acid In N,N-dimethyl-formamide at 20℃; for 72h;
methanesulfonyl chloride
124-63-0

methanesulfonyl chloride

flumetasone
2135-17-3

flumetasone

2-[(1R,2S,8S,10S,11S,13R,14R,15S,17S)-1,8-difluoro-14,17-dihydroxy-2,13,15-trimethyl-5-oxotetracyclo[8.7.0.02'7.011,15]heptadeca-3,6-dien-14-yl]-2-oxoethyl methanesulfonate
2414-34-8

2-[(1R,2S,8S,10S,11S,13R,14R,15S,17S)-1,8-difluoro-14,17-dihydroxy-2,13,15-trimethyl-5-oxotetracyclo[8.7.0.02'7.011,15]heptadeca-3,6-dien-14-yl]-2-oxoethyl methanesulfonate

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 20℃;
With pyridine at 0℃; for 2h;
flumetasone
2135-17-3

flumetasone

C29H31F2NO4S2
1345277-64-6

C29H31F2NO4S2

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C
2: potassium carbonate / acetone / Reflux
View Scheme
flumetasone
2135-17-3

flumetasone

C61H101F2N3O16

C61H101F2N3O16

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: periodic acid / 1,4-dioxane; water / 2 h / 20 °C
2: triethylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 18 h / 0 - 20 °C / Inert atmosphere
View Scheme
flumetasone
2135-17-3

flumetasone

C53H87F2N3O13
442638-54-2

C53H87F2N3O13

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: periodic acid / 1,4-dioxane; water / 2 h / 20 °C
2: triethylamine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 18 h / 0 - 20 °C / Inert atmosphere
View Scheme
C12H24N4O2
1281702-63-3

C12H24N4O2

flumetasone
2135-17-3

flumetasone

A

C34H50F2N4O6

C34H50F2N4O6

B

C46H72F2N8O7

C46H72F2N8O7

Conditions
ConditionsYield
With acetic acid In ethanol; water at 70℃; for 0.5h;
flumetasone
2135-17-3

flumetasone

6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(propionyloxy)androsta-1,4-diene-17β-carboxylic acid
65429-42-7

6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(propionyloxy)androsta-1,4-diene-17β-carboxylic acid

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: sodium periodate / water; tetrahydrofuran / 2 h / 25 - 30 °C
2.1: triethylamine / acetone / 3 h / 0 - 5 °C
2.2: 2.5 h / 40 - 45 °C
View Scheme
Multi-step reaction with 2 steps
1.1: periodic acid / water; tetrahydrofuran / 2 h / 0 - 10 °C
2.1: triethylamine / acetone / 1 h / 0 - 10 °C
2.2: 2 h
View Scheme
flumetasone
2135-17-3

flumetasone

17β-[(N,N-dimethylcarbamoyl)thio]formyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-one androstone-1,4-diene
105638-31-1

17β-[(N,N-dimethylcarbamoyl)thio]formyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-one androstone-1,4-diene

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: sodium periodate / water; tetrahydrofuran / 2 h / 25 - 30 °C
2.1: triethylamine / acetone / 3 h / 0 - 5 °C
2.2: 2.5 h / 40 - 45 °C
3.1: sodium iodide; triethylamine / tetrahydrofuran / 4 h / 70 - 75 °C
View Scheme
Multi-step reaction with 3 steps
1.1: periodic acid / water; tetrahydrofuran / 2 h / 0 - 10 °C
2.1: triethylamine / acetone / 1 h / 0 - 10 °C
2.2: 2 h
3.1: sodium iodide; triethylamine / tetrahydrofuran / 16 h / 20 °C
View Scheme
flumetasone
2135-17-3

flumetasone

17-propionate carbothioic acid
80474-45-9

17-propionate carbothioic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: sodium periodate / water; tetrahydrofuran / 2 h / 25 - 30 °C
2.1: triethylamine / acetone / 3 h / 0 - 5 °C
2.2: 2.5 h / 40 - 45 °C
3.1: sodium iodide; triethylamine / tetrahydrofuran / 4 h / 70 - 75 °C
4.1: morpholine / 3 h / 20 °C
View Scheme
Multi-step reaction with 4 steps
1.1: periodic acid / water; tetrahydrofuran / 2 h / 0 - 10 °C
2.1: triethylamine / acetone / 1 h / 0 - 10 °C
2.2: 2 h
3.1: sodium iodide; triethylamine / tetrahydrofuran / 16 h / 20 °C
4.1: calcium hydroxide / methanol / 24 h / 25 - 30 °C
View Scheme
flumetasone
2135-17-3

flumetasone

flixotide
80474-14-2

flixotide

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sodium periodate / water; tetrahydrofuran / 2 h / 25 - 30 °C
2.1: triethylamine / acetone / 3 h / 0 - 5 °C
2.2: 2.5 h / 40 - 45 °C
3.1: sodium iodide; triethylamine / tetrahydrofuran / 4 h / 70 - 75 °C
4.1: morpholine / 3 h / 20 °C
5.1: potassium carbonate / acetone / 0.5 h / 20 °C
5.2: 0 - 5 °C
View Scheme

2135-17-3Relevant articles and documents

Synthesis method of steroid corticosteroid 21-hydroxyl side chain

-

Paragraph 0042-0044, (2020/03/06)

The invention belongs to the technical field of steroid hormone preparation, and particularly relates to a synthesis method of a steroid corticosteroid 21-hydroxyl side chain. The synthesis method comprises the step that a compound I reacts with a peroxide to obtain a compound II. The reaction route is as follows. (Please see the specification for the reaction route.) According to the synthesis method, the 21-hydroxysteroid compound is obtained from a 20-alkenyl steroid compound substrate by a one-pot method. Compared with a previous construction method, the step is the shortest, conditions are simpler, and the highest efficiency is achieved.

Ring opening and fluoridation method and device of steroidal epoxy compound

-

Paragraph 0038; 0039; 0041, (2017/07/22)

The invention discloses a method of preparing a compound II, which is as shown as the following reaction formula as shown in the specification. A 9 alpha-fluorine-11 beta -hydroxyl steroidal compound II is prepared via epoxy compound ring opening and fluoridation of a steroidal epoxy compound I by taking hydrogen fluoride as a fluorination reagent in a solvent consisting of arene and water. In the formula, R is CH3, CH2OH or CH2OAc; R1 is OH; R2 is alpha-CH3 or beta-CH3; and R3 is F or H. A continuous reaction device as shown in Figure 1 can be used in the method.

Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor

-

, (2008/06/13)

Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.

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