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(11beta,17alpha)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid, also known as Prednienic Acid, is a glucocorticoid steroid derived from the androstane class of steroid hormones. It possesses a unique chemical structure with hydroxyl groups at the 11-beta and 17-alpha positions, and a carboxylic acid group at the 17 position. This structure endows it with specific biological activities and makes it a valuable compound for pharmaceutical applications.

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  • (11β,17α)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid

    Cas No: 37927-29-0

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  • 37927-29-0 Structure
  • Basic information

    1. Product Name: (11beta,17alpha)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid
    2. Synonyms: (11beta,17alpha)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid;(17R)-11β,17-Dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid;Δ1-Cortienic acid;Androsta-1,4-diene-17-carboxylic acid, 11,17-dihydroxy-3-oxo-, (11beta,17alpha)-;(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-diMethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid;Prednisolone iMpurity B (carboxylic acid);Prednienic Acid;Prednisolone Impurity B
    3. CAS NO:37927-29-0
    4. Molecular Formula: C20H26O5
    5. Molecular Weight: 346.41744
    6. EINECS: 253-719-9
    7. Product Categories: N/A
    8. Mol File: 37927-29-0.mol
  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: 570.7°Cat760mmHg
    3. Flash Point: 313°C
    4. Appearance: /
    5. Density: 1.33
    6. Vapor Pressure: 2.11E-15mmHg at 25°C
    7. Refractive Index: 1.62
    8. Storage Temp.: Refrigerator
    9. Solubility: DMSO (Slightly), Methanol (Slightly)
    10. PKA: 3.78±0.70(Predicted)
    11. CAS DataBase Reference: (11beta,17alpha)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid(CAS DataBase Reference)
    12. NIST Chemistry Reference: (11beta,17alpha)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid(37927-29-0)
    13. EPA Substance Registry System: (11beta,17alpha)-11,17-dihydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid(37927-29-0)
  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 37927-29-0(Hazardous Substances Data)

37927-29-0 Usage

Uses

Used in Pharmaceutical Industry:
Prednienic Acid is used as a key intermediate in the synthesis of various anti-inflammatory compounds. Its unique structure allows for the creation of macrolactonolides by conjugating Prednienic Acid with macrolides, which are known for their potent anti-inflammatory properties. This application is particularly relevant in the development of new drugs to treat conditions such as arthritis, asthma, and other inflammatory diseases.
Used in Drug Synthesis:
Prednienic Acid serves as a versatile building block for the synthesis of a wide range of steroidal drugs. Its chemical properties make it an ideal candidate for the development of new pharmaceuticals with improved efficacy, reduced side effects, and targeted delivery. This application is crucial in the ongoing efforts to discover and create novel therapeutic agents to address unmet medical needs.

Check Digit Verification of cas no

The CAS Registry Mumber 37927-29-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,7,9,2 and 7 respectively; the second part has 2 digits, 2 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 37927-29:
(7*3)+(6*7)+(5*9)+(4*2)+(3*7)+(2*2)+(1*9)=150
150 % 10 = 0
So 37927-29-0 is a valid CAS Registry Number.
InChI:InChI=1/C20H26O5/c1-18-7-5-12(21)9-11(18)3-4-13-14-6-8-20(25,17(23)24)19(14,2)10-15(22)16(13)18/h5,7,9,13-16,22,25H,3-4,6,8,10H2,1-2H3,(H,23,24)/t13-,14-,15-,16+,18-,19-,20-/m0/s1

37927-29-0SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name (8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-17-carboxylic acid

1.2 Other means of identification

Product number -
Other names Pj 90

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:37927-29-0 SDS

37927-29-0Synthetic route

prednisolon
50-24-8

prednisolon

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Conditions
ConditionsYield
With periodic acid In tetrahydrofuran; methanol at 20℃; for 2h;100%
With sodium periodate; sulfuric acid In methanol; water at 20℃; for 16h; Inert atmosphere;98.8%
With sodium periodate In methanol; water for 0.5h; Heating; Large scale;97%
C20H25BrO5

C20H25BrO5

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Conditions
ConditionsYield
With hydrogenchloride; chromium chloride; mercaptoacetic acid; zinc In ethanol; water at 10 - 30℃; for 0.5h; Temperature; Inert atmosphere;98%
Loteprednol etabonate
82034-46-6

Loteprednol etabonate

A

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

B

17α-ethoxycarbonyloxy-11β-hydroxy-3-oxoandrosta-1,4-diene-17β-carboxylic acid

17α-ethoxycarbonyloxy-11β-hydroxy-3-oxoandrosta-1,4-diene-17β-carboxylic acid

Conditions
ConditionsYield
With heptakis(2,6-di-O-methyl)cyclomaltoheptaose; water at 37℃; Kinetics; Activation energy; Further Variations:; Temperatures; Reagents; Solvents; Hydrolysis;
11α-hydroxy-androsta-1,4-diene-3,17-dione
898-84-0, 96893-16-2, 7801-18-5

11α-hydroxy-androsta-1,4-diene-3,17-dione

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: acetic anhydride; phosphoric acid / dichloromethane / 5 h / 0 - 5 °C / Inert atmosphere
2.1: magnesium; ethylene dibromide / tetrahydrofuran / 1 h / 50 - 60 °C / Inert atmosphere
2.2: 1 h / -5 - 5 °C / Inert atmosphere
3.1: sodium hydrogencarbonate; potassium fluoride / tetrahydrofuran / 0.5 h / 25 °C / Inert atmosphere
3.2: 5 h / 25 °C / Inert atmosphere
4.1: chromium(VI) oxide; sulfuric acid / acetone; water / 0 - 25 °C
5.1: perchloric acid; N-bromoacetamide / acetone / 3.33 h / -5 - 5 °C / Inert atmosphere
6.1: mercaptoacetic acid; chromium chloride; zinc; hydrogenchloride / water; ethanol / 0.5 h / 10 - 30 °C / Inert atmosphere
View Scheme
androsta-1,4,9(11)-triene-3,17-dione
15375-21-0

androsta-1,4,9(11)-triene-3,17-dione

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: magnesium; ethylene dibromide / tetrahydrofuran / 1 h / 50 - 60 °C / Inert atmosphere
1.2: 1 h / -5 - 5 °C / Inert atmosphere
2.1: sodium hydrogencarbonate; potassium fluoride / tetrahydrofuran / 0.5 h / 25 °C / Inert atmosphere
2.2: 5 h / 25 °C / Inert atmosphere
3.1: chromium(VI) oxide; sulfuric acid / acetone; water / 0 - 25 °C
4.1: perchloric acid; N-bromoacetamide / acetone / 3.33 h / -5 - 5 °C / Inert atmosphere
5.1: mercaptoacetic acid; chromium chloride; zinc; hydrogenchloride / water; ethanol / 0.5 h / 10 - 30 °C / Inert atmosphere
View Scheme
C25H38O3Si

C25H38O3Si

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: sodium hydrogencarbonate; potassium fluoride / tetrahydrofuran / 0.5 h / 25 °C / Inert atmosphere
1.2: 5 h / 25 °C / Inert atmosphere
2.1: chromium(VI) oxide; sulfuric acid / acetone; water / 0 - 25 °C
3.1: perchloric acid; N-bromoacetamide / acetone / 3.33 h / -5 - 5 °C / Inert atmosphere
4.1: mercaptoacetic acid; chromium chloride; zinc; hydrogenchloride / water; ethanol / 0.5 h / 10 - 30 °C / Inert atmosphere
View Scheme
C20H26O3

C20H26O3

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: chromium(VI) oxide; sulfuric acid / acetone; water / 0 - 25 °C
2: perchloric acid; N-bromoacetamide / acetone / 3.33 h / -5 - 5 °C / Inert atmosphere
3: mercaptoacetic acid; chromium chloride; zinc; hydrogenchloride / water; ethanol / 0.5 h / 10 - 30 °C / Inert atmosphere
View Scheme
chloro-methylsulfanyl-methane
2373-51-5

chloro-methylsulfanyl-methane

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

methylthiomethyl 11β,17α-dihydroxy-3-oxo-androst-1,4-diene-17β-carboxylate

methylthiomethyl 11β,17α-dihydroxy-3-oxo-androst-1,4-diene-17β-carboxylate

Conditions
ConditionsYield
With triethylamine98%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

chloroformic acid ethyl ester
541-41-3

chloroformic acid ethyl ester

17α-[(ethoxycarbonyl)oxy]-11β-hydroxy-3-oxoandrosta-1,4-diene-17β-carboxylic ethoxycarboxylic anhydride

17α-[(ethoxycarbonyl)oxy]-11β-hydroxy-3-oxoandrosta-1,4-diene-17β-carboxylic ethoxycarboxylic anhydride

Conditions
ConditionsYield
With triethylamine In dichloromethane at 0 - 10℃; for 0.5h; Large scale;96%
With tetra(n-butyl)ammonium hydrogensulfate; sodium hydrogencarbonate In dichloromethane at 20℃; for 3h; Time;90.2%
dichloroacethyl chloride
79-36-7

dichloroacethyl chloride

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

tetra(n-butyl)ammonium hydrogensulfate
32503-27-8

tetra(n-butyl)ammonium hydrogensulfate

17α-dichloroacetoxy-11β-hydroxyandrosta-1,4-diene-3-one-17β-carboxylic acid
199331-37-8

17α-dichloroacetoxy-11β-hydroxyandrosta-1,4-diene-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With sodium hydrogencarbonate In methanol; dichloromethane; water95%
With sodium hydrogencarbonate In methanol; dichloromethane; water95%
With sodium hydrogencarbonate In dichloromethane; water
With sodium hydrogencarbonate In dichloromethane; water
dichloroacethyl chloride
79-36-7

dichloroacethyl chloride

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

17α-dichloroacetoxy-11β-hydroxyandrosta-1,4-diene-3-one-17β-carboxylic acid
199331-37-8

17α-dichloroacetoxy-11β-hydroxyandrosta-1,4-diene-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With potassium hydrogencarbonate In dichloromethane; water for 2h;93%
With potassium hydrogencarbonate In dichloromethane; water for 2.5h;93%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

11β-hydroxy-17-methyl-18-norandrosta-1,4,13(17)-trien-3-one

11β-hydroxy-17-methyl-18-norandrosta-1,4,13(17)-trien-3-one

Conditions
ConditionsYield
With dicyclohexyl-carbodiimide In 1,4-dioxane; acetonitrile for 1h; Ambient temperature;88%
9-deoxo-9a-aza-9a-demethyl-9a-(3-aminopropyl)-9a-homoerythromycin A
92594-46-2

9-deoxo-9a-aza-9a-demethyl-9a-(3-aminopropyl)-9a-homoerythromycin A

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

C60H101N3O16
442638-01-9

C60H101N3O16

Conditions
ConditionsYield
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine In dichloromethane at 0 - 20℃; for 18h; Inert atmosphere;88%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

diisopropyl-carbodiimide
693-13-0

diisopropyl-carbodiimide

(17R)-3'-isopropyl-2'-isopropylimino-11β-hydroxyspiro-3,4'-dione

(17R)-3'-isopropyl-2'-isopropylimino-11β-hydroxyspiro-3,4'-dione

Conditions
ConditionsYield
With copper dichloride In 1,4-dioxane; acetonitrile for 1h; Ambient temperature;86%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

2-(4-methoxyphenoxy)ethylamine
50800-92-5

2-(4-methoxyphenoxy)ethylamine

C29H37NO6

C29H37NO6

Conditions
ConditionsYield
Stage #1: (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 1h; Inert atmosphere;
Stage #2: 2-(4-methoxyphenoxy)ethylamine With triethylamine In N,N-dimethyl-formamide at 60℃; for 1.5h; Inert atmosphere;
75%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

(L)-phenylalanine ethyl ester hydrochloride
3182-93-2

(L)-phenylalanine ethyl ester hydrochloride

ethyl 2-(11β,17α-dihydroxy-3-oxo-androst-1,4-dien-17β-carboxamido)-3-phenylpropionate

ethyl 2-(11β,17α-dihydroxy-3-oxo-androst-1,4-dien-17β-carboxamido)-3-phenylpropionate

Conditions
ConditionsYield
Stage #1: (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid With benzotriazol-1-ol; dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 0 - 8℃; for 16h;
Stage #2: (L)-phenylalanine ethyl ester hydrochloride With triethylamine In N,N-dimethyl-formamide at 0 - 8℃; for 16h;
70%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

diisopropyl-carbodiimide
693-13-0

diisopropyl-carbodiimide

(17R)-3'-isopropyl-11β-hydroxyspiro-2',3,4'-trione

(17R)-3'-isopropyl-11β-hydroxyspiro-2',3,4'-trione

Conditions
ConditionsYield
With water In N,N-dimethyl-formamide for 7h; Ambient temperature;66%
di-p-tolylcarbodiimide
726-42-1

di-p-tolylcarbodiimide

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

11β,17α-dihydroxy-3-oxo-N-p-tolyl-N-(p-tolylaminocarbonyl)androsta-1,4-diene-17-carboxamide

11β,17α-dihydroxy-3-oxo-N-p-tolyl-N-(p-tolylaminocarbonyl)androsta-1,4-diene-17-carboxamide

Conditions
ConditionsYield
With 1,4-diaza-bicyclo[2.2.2]octane In acetonitrile at 80℃; for 1h;63%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

glycine ethyl ester hydrochloride
5680-79-5

glycine ethyl ester hydrochloride

methyl 2-(11β,17α-dihydroxy-3-oxo-androst-1,4-dien-17β-carboxamido)acetate

methyl 2-(11β,17α-dihydroxy-3-oxo-androst-1,4-dien-17β-carboxamido)acetate

Conditions
ConditionsYield
Stage #1: (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid With benzotriazol-1-ol; dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 0 - 8℃; for 16h;
Stage #2: glycine ethyl ester hydrochloride With triethylamine In N,N-dimethyl-formamide at 0 - 8℃; for 16h;
57%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

methyl [4-(3-aminopropoxy)benzoate]
85873-34-3

methyl [4-(3-aminopropoxy)benzoate]

C31H39NO7

C31H39NO7

Conditions
ConditionsYield
Stage #1: (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 1h; Inert atmosphere;
Stage #2: methyl [4-(3-aminopropoxy)benzoate] In N,N-dimethyl-formamide at 60℃; for 2.5h; Inert atmosphere;
54%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

6α,11β,17α-trihydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

6α,11β,17α-trihydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With selenium(IV) oxide In 1,4-dioxane for 12h; Heating;53.9%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

1-(3-aminopropoxy)-3-methoxybenzene
6451-26-9

1-(3-aminopropoxy)-3-methoxybenzene

C30H39NO6

C30H39NO6

Conditions
ConditionsYield
Stage #1: (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid With benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 1h; Inert atmosphere;
Stage #2: 1-(3-aminopropoxy)-3-methoxybenzene With triethylamine In N,N-dimethyl-formamide at 60℃; for 2.5h; Inert atmosphere;
53%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

ethyl β-alaninate hydrochloride
4244-84-2

ethyl β-alaninate hydrochloride

ethyl 3-(11β,17α-dihydroxy-3-oxo-androst-1,4-dien-17β-carboxamido)propionate

ethyl 3-(11β,17α-dihydroxy-3-oxo-androst-1,4-dien-17β-carboxamido)propionate

Conditions
ConditionsYield
Stage #1: (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid With benzotriazol-1-ol; dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 0 - 8℃; for 16h;
Stage #2: ethyl β-alaninate hydrochloride With triethylamine In N,N-dimethyl-formamide at 0 - 8℃; for 16h;
51%
di-p-tolylcarbodiimide
726-42-1

di-p-tolylcarbodiimide

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

(17R)-3'-p-tolyl-11β-hydroxyspiro-2',3,4'-trione

(17R)-3'-p-tolyl-11β-hydroxyspiro-2',3,4'-trione

Conditions
ConditionsYield
With water In N,N-dimethyl-formamide for 168h; Ambient temperature;50%
chloroiodoacetyl chloride
827313-06-4

chloroiodoacetyl chloride

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

17α-chloroiodoacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid
750645-43-3

17α-chloroiodoacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 2.5h;49%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

dicyclohexyl-carbodiimide
538-75-0

dicyclohexyl-carbodiimide

(17R)-3'-cyclohexyl-11β-hydroxyspiro-2',3,4'-trione

(17R)-3'-cyclohexyl-11β-hydroxyspiro-2',3,4'-trione

Conditions
ConditionsYield
With water In N,N-dimethyl-formamide for 7h; Ambient temperature;48%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Trichloroacetyl chloride
76-02-8

Trichloroacetyl chloride

17α-trichloroacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid
750645-44-4

17α-trichloroacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With potassium hydrogencarbonate In dichloromethane; water for 2h;48%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride
25952-53-8

1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride

(17R)-2'-ethylimino-11β-hydroxy-3'-dimethylaminopropylspiro-2',3,4'-trione

(17R)-2'-ethylimino-11β-hydroxy-3'-dimethylaminopropylspiro-2',3,4'-trione

Conditions
ConditionsYield
In N,N-dimethyl-formamide for 3h; Ambient temperature;47%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

dicyclohexyl-carbodiimide
538-75-0

dicyclohexyl-carbodiimide

(17R)-3'-cyclohexyl-2'-cyclohexylimino-11β-hydroxyspiro-3,4'-dione

(17R)-3'-cyclohexyl-2'-cyclohexylimino-11β-hydroxyspiro-3,4'-dione

Conditions
ConditionsYield
With copper dichloride In 1,4-dioxane; acetonitrile for 1h; Ambient temperature;47%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

ethyl iodide
75-03-6

ethyl iodide

ethyl 11β,17α-dihydroxyandrosta-1,4-dien-3-one-17β-carboxylate
182069-13-2

ethyl 11β,17α-dihydroxyandrosta-1,4-dien-3-one-17β-carboxylate

Conditions
ConditionsYield
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 1.5h;45%
formic acid
64-18-6

formic acid

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

17α-formyloxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

17α-formyloxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With acetic anhydride In pyridine for 7h; Heating;39%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

chloroacetyl chloride
79-04-9

chloroacetyl chloride

17α-chloroacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid
750645-47-7

17α-chloroacetoxy-11β-hydroxyandrosta-1,4-dien-3-one-17β-carboxylic acid

Conditions
ConditionsYield
With potassium hydrogencarbonate In dichloromethane; water for 2h;26%
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

Δ1-CA-Me
10486-89-2

Δ1-CA-Me

Conditions
ConditionsYield
In methanol; diethyl ether
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

β‐cyclodextrin
7585-39-9

β‐cyclodextrin

2C42H70O35*C20H26O5

2C42H70O35*C20H26O5

Conditions
ConditionsYield
In water at 25℃; for 168h;
(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid
37927-29-0

(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0 02,7. 011,15]heptadeca-3,6-diene-14-carboxylic acid

cyclomaltooctaose
17465-86-0

cyclomaltooctaose

3C48H80O40*2C20H26O5

3C48H80O40*2C20H26O5

Conditions
ConditionsYield
In water at 25℃; for 168h;

37927-29-0Relevant articles and documents

Preparation method of loteprednol etabonate intermediate

-

Paragraph 0010; 0031; 0036-0037; 0042, (2021/07/14)

The invention provides a preparation method of a loteprednol etabonate intermediate. The preparation method comprises the following steps: carrying out dehydration reaction on 11 alpha-hydroxyl-ADD and a dehydrating agent in an organic solvent to obtain a compound II; carrying out a first addition reaction on the compound II and a halogenating reagent in an organic solvent in the presence of an acid catalyst, and adding a quenching agent to carry out a quenching reaction after the reaction is finished, so as to obtain a compound III; carrying out reduction reaction on the compound III and a metal reducing agent in an organic solvent in the presence of an acid catalyst to obtain a compound IV; carrying out secondary addition reaction on the compound IV and a cyaniding reagent in an organic solvent in the presence of a basic catalyst to obtain a compound V; and carrying out hydrolysis reaction on thecompound V and an acid reagent in an organic solvent to obtain a compound VI, wherein the compound VI is the loteprednol etabonate intermediate. The preparation method saves energy, reduces consumption, and is easy to operate, high in yield and good in purity.

Synthesis method of loteprednol intermediate

-

Paragraph 0012; 0066-0071, (2020/05/08)

The invention provides a preparation method of a loteprednol etabonate intermediate, wherein the method comprises that cheap and accessible 11 alpha-hydroxy-ADD as a starting raw material is subjectedto dehydrating, Grignard reaction, hydrolyzing, oxidizing, bromo-hydroxylating and reducing to obtain 17 beta-carboxylic acid (compound VII). The method has the advantages of easily available initialraw materials, high yield, good purity and stable process.

POTENT SOFT ANTI-INFLAMMATORY CORTICOSTEROID COMPOUNDS AND USES THEROF

-

Paragraph 0070; 0071, (2019/01/08)

Potent soft corticosteroid pharmaceutical compositions comprising them and method for use as anti-inflammatory agents. Also, a method for softening fluticasone propionate and similar corticosteroids to arrive at potent but safer alternatives. The compound S-fluoromethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16a- methyl-3-oxoandrosta-1,4-diene-17β-carbothioate, which is equally potent to but safer than fluticasone, is among those provided. Another compound of particular interest is 2-hydroxyethyl 17α-dichloroacetoxy-6α,9α-difluoro-11β-hydroxy-16β- methyl-3-oxoandrosta-1,4-diene-17β-carboxylate.

A method for synthesizing loteprednol etabonate and a method for synthesizing intermediate (by machine translation)

-

Paragraph 0025; 0027; 0028, (2017/05/05)

The present invention provides a method of synthesizing loteprednol etabonate, comprises the following steps: step 1: to prednisolone as raw material preparation 11 β, 17 α - dihydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid; step 2: adopts the 11 β, 17 α - dihydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid preparation 17 α - ((ethoxy-formyl) oxy) - 11 β - hydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid ethyl carbonic anhydride; step 3: the 17 α - ((ethoxy-formyl) oxy) - 11 β - hydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid ethyl carbonic anhydride adding ethanol into sodium after a period of time by adding chlorine iodine methane then will be chlorine iodine methane. In step 3 can avoid the influence of the introduction of water to the intermediate. (by machine translation)

Loteprednol preparation method and ophthalmic composition of loteprednol

-

Paragraph 0085-0087; 0100-00102; 0115-0117, (2017/09/01)

The present invention relates to a loteprednol preparation method and an ophthalmic composition of loteprednol, particularly to a loteprednol preparation method, which comprises: dissolving a raw material loteprednol in a first organic solvent to obtain a drug-containing solution, adding a second organic solvent to the obtained solution in a dropwise manner under stirring, continuously stirring, filtering, washing the filter cake by using the second organic solvent, and drying the obtained filter cake in a vacuum oven to obtain the product. The invention further provides a loteprednol bulk drug prepared according to the method, an ophthalmic pharmaceutical composition prepared by using the prepared loteprednol as a bulk drug, and uses of the prepared loteprednol in preparation of drugs for treatment or prevention of ocular inflammations or dry eye. The method of the present invention has excellent pharmaceutical properties, wherein the prepared bulk drug and the preparation have excellent stability.

SELECTIVE GLUCOCORTICOID RECEPTOR LIGANDS

-

Page/Page column 34; 38, (2015/06/03)

Described herein are certain steroid derivative compounds, for example of formula (I): wherein X1, X2, X3 L, and Ar are as defined herein, pharmaceutical compositions comprising such compounds, the use of such compounds and compositions to specifically target glucocorticoid action, and the use of such compounds and compositions in the treatment of acute and chronic inflammatory conditions, in particular rheumatoid arthritis, haematological and other malignancies, and for causing immunosuppression in the prevention or treatment of transplant rejection, as well as methods of preparing such compounds.

Macrolactonolides: A novel class of anti-inflammatory compounds

Toma?kovi?, Linda,Komac, Marijana,Makaruha Stegi?, Oresta,Muni?, Vesna,Rali?, Jovica,Stani?, Barbara,Banjanac, Mihailo,Markovi?, Stribor,Hrva?i?, Bo?ka,?ip?i? Paljetak, Hana,Padovan, Jasna,Glojnari?, Ines,Erakovi? Haber, Vesna,Mesi?, Milan,Mer?ep, Mladen

, p. 321 - 332 (2013/02/23)

A new concept in design of safe glucocorticoid therapy was introduced by conjugating potent glucocorticoid steroids with macrolides (macrolactonolides). These compounds were synthesized from various steroid 17β-carboxylic acids and 9a-N-(3-aminoalkyl) derivatives of 9-deokso-9a-aza-9a-homoeritromicin A and 3-descladinosyl-9-deokso-9a-aza-9a-homoeritromicin A using stable alkyl chain. Combining property of macrolides to preferentially accumulate in immune cells, especially in phagocyte cells, with anti-inflammatory activity of classic steroids, we designed molecules which showed good anti-inflammatory activity in ovalbumin (OVA) induced asthma in rats. The synthesis, in vitro and in vivo anti-inflammatory activity of this novel class of compounds are described.

Etiprednol dicloacetate, a new soft glucocorticoid drug candidate. Development of chemistry

Csanadi,Horvath,Szekeres,Hasko,Ila,Ivanics,Patthy,Salat,Seres,Pallagi,Toth,Szederkenyi,Konya,Tegdes,Bodor,Zubovics, Zoltan

, p. 349 - 359 (2007/10/03)

During development of chemistry of the soft drug candidate etiprednol dicloacetate (BNP-166) 1) optimization studies on the three-step chemical synthesis resulted in a process that could be scaled-up to the kg level, 2) the impurity profile was determined, 3) synthetic routes were developed for the preparation of the radiolabeled target compound, and 4) a series of hydroxylated metabolites was prepared.

Effect of cyclodextrins on the solubility and stability of a novel soft corticosteroid, loteprednol etabonate

Bodor, Nicholas,Drustrup,Wu

, p. 206 - 209 (2007/10/03)

To increase the aqueous solubility and stability of the soft corticosteroid loteprednol etabonate (LE), drug complexation using various cyclodextrins (CDs), such as γ-cyclodextrin (γ-CD), 2-hydroxypropyl-β- cyclodextrin (HPBCD), maltosyl-β-cyclodextrin (MBCD), mixture of glucosyl/maltosyl-α-, β-, and γ-cyclodextrin (GMCD), and heptakis (2,6-di- O-methyl)-β-cyclodextrin (DMCD), were attempted. The solubilizing and stabilizing effects of CD by itself or combined with various co-solvents were also investigated. Micronized (5 micron) LE was mixed in various aqueous CD or CD with cosolvent solutions. After equilibration and filtration at 23 °C, the solubility of LE was determined by HPLC. Subsequently, the stability of LE in the solutions was also determined by following the LE concentration change in the solution for an appropriate period. CD complexation significantly increased the aqueous solubility and stability of LE. The increase in solubility displayed a concentration dependency on CDs (0-50%). Among the five CDs used, DMCD showed the highest effects on the solubility (4.2-18.3 mg/ml in 10-50% DMCD) and stability (t90 > 4 years at 4 °C, when LE 0.5 mg/ml was dissolved in 10% DMCD solution) of LE. By adding co- solvents, such as glycerol, propylene glycol (PG), polyvinyl alcohol (PVA), and polyvinylpyrrolidone (PVP-10), the solubility of LE in DMCD solutions was further increased. Degradation of LE to the corresponding metabolites, Δ1- cortienic acid etabonate (AE) and Δ1-cortienic acid (A), in aqueous CD solutions appeared to be a predicted, two-step kinetics. Differential Scanning Calorimetry (DSC) was used to assist explaining the solubilizing and stabilizing activity differences between CDs. LE/CD mixture or lyophilized LE/CD complex was scanned at a rate of 20 °C/min. The exothermic peak found in the DSC diagram with LE/DMCD sample, but not with LE/HPBCD samples, suggests a stronger complex formed between LE and DMCD, resulting in higher solubility and stability of LE in DMCD than in HPBCD.

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