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Sale API Exemestane/Aromasin 107868-30-4 Fast Delivery
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Exemestane(Aromasin) CAS NO.107868-30-4 Factory High Quality
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Exemestane 99% USP
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107868-30-4 Usage

Uses

Labeled Exemestane, intended for use as an internal standard for the quantification of Exemestane by GC- or LC-mass spectrometry.

Uses

An antineoplastic (hormonal)

Brand name

Aromasin (Pharmacia& Upjohn).

Indications and Usage

Exemestane is an irreversible steroid aromatase inhibitor. Its structure is similar to that of aromatase’s natural substrate, androstenedione, and acts as a pseudosubstrate. Postmenopausal women’s estrogen is mainly converted from androgen (produced by the adrenal cortex) by aromatase in the surrounding tissue. This drug irreversibly binds with the active site on aromatase to deactivate it, thus dramatically lower estrogen levels in the blood circulation of postmenopausal women. By inhibiting aromatase to lower estrogen levels, it can be used to treat hormone-dependent breast cancer in postmenopausal women. Exemestane is suitable for treating advanced breast cancer in naturally or artificially postmenopausal women that has not responded well to tamoxifen treatment. It is also suitable for treating estrogen and progesterone receptor positive postmenopausal advanced breast cancer, and it can also be used to treat metastasized breast cancer and as adjuvant therapy for early breast cancer.

Definition

ChEBI: A 17-oxo steroid that is androsta-1,4-diene-3,17-dione in which the hydrogens at position 6 are replaced by a double bond to a methylene group. A selective inhibitor of the aromatase (oestrogen synthase) system, it is used in the treatment of advanced brea t cancer.

Drug interactions

1. This drug cannot be used in combination with estrogen-based drugs to avoid counteracting its medicinal effects. 2. Exemestane is mostly metabolized by CYP3A4, but when used in combination with a strong CYP3A4 inhibitor (Ketoconazole), its pharmacokinetics do not exhibit any change. This is because the inhibitor does not seem to affect the drug’s pharmacokinetics, but it is also possible that the known CYP3A4 inducer lowers the blood concentration of Exemestane.

Originator

Farmitalia Carlo Erba (Italy)

General Description

Exemestane, 6-methylenandrosta-1,4-diene-3,17-dione (Aromasin), is the first steroid-basedaromatase inhibitor approved for the treatment of breastcancer in the United States. It is a mechanism-based inactivatorthat irreversibly inhibits the enzyme. Plasma estrogenlevels are reduced by 85% to 95% within 2 to 3 days, and effectslast 4 to 5 days. Exemestane does not inhibit any of themajor cytochromes P450 and has essentially no interactionwith steroid receptors, with only a very weak affinity for theAR. The 17β-hydroxyexemestane reduction product, however,has much higher affinity for the AR than the parent(still several fold less than DHT, 0.28% for parent vs. 30%for metabolite). The clinical significance of the affinity islikely minimal because of the low levels of the metaboliteproduced.

Contradictions

1. Not to be used by patients allergic to this drug. 2. Not to be used by pregnant women, breastfeeding women, and children.

Chemical Properties

white to light yellow crystal powder

Clinical Research

For patients resistant to tamoxifen, 25mg of Exemestane, qd, can achieve an objective efficacy rate of 15-28% and a median continuation period of 69-76 weeks. Exemestane is superior to Megestrol, and it can extend the disease progression time. For patients who have worsened conditions following Megestrol treatment, Exemestane can still achieve an objective efficacy rate of 11-13%. A daily 25mg dose of Exemestane has an objective efficacy rate of 6.6% on patients who have not responded to non-steroidal aromatase inhibitors, and the two drugs are not cross-resistant.

Warnings and precautions

1. Premenopausal women usually do not use Exemestane. 2. Patients with moderate to severe liver or renal failure should use with caution. Exceeding the recommended dosage of Exemestane may increase the occurrence of nonfatal adverse effects. 3. FDA labeled this drug’s pregnancy safety as level D. 4. Elderly patients do not require any special precautions.

Uses

antiinfective

Manufacturing Process

0.50 g of 6-methylenandrost-4-ene-3,17-dione and 0.57 g of dichlorodicyanobenzoquinone were refluxed in 20 ml of anhydrous dioxane for about 15 hours. To remove the DDQ the suspension was filtered through alumina. After evaporation of the solvent the residue was dissolved in ethyl acetate, the organic layer washed with water, dried over sodium sulfate and the solvent removed under vacuum. The crude product was chromatographed on silica gel using hexane/ethyl acetate to yield 0.25 g of pure 6- methylenandrosta-1,4-diene-3,17-dione, m.p. 188-191°C, λmax 247 nm (ε 13.750).

Side effects

Adverse effects include nausea, dryness, constipation, diarrhea, dizziness, insomnia, rash, fatigue, fever, swelling, pain, vomiting, abdominal pain, increased appetite, weight gain, etc. Additionally, some literature reports cases of hypertension, depression, anxiety, difficulty breathing, coughing, etc. There may also be decreases lymph cell amounts, abnormalities in liver function indicators (such as alanine aminotransferase), etc.

Therapeutic Function

Antineoplastic

Pharmacokinetics

This drug has no noticeable effect on adrenal corticosteroids biosynthesis. Even when its concentration is over 600 times the concentration required to inhibit aromatase, it still has no noticeable effect the other enzymes in the corticosteroid production pathway. This drug is absorbed quickly when taken orally and will affect food absorption. Its oral bioavailability is 42%. Postmenopausal women have a higher absorption rate than healthy test subjects. Patients reach peak blood concentration 2-4 hours after intake, and the peak lasts for an average of 1.2 hours, which is 2.9 hours shorter than healthy subjects. It mainly binds to Α1-acid glycoprotein and protein, and its overall binding rate to protein is 90%. It is mainly metabolized by the liver, the metabolite is inactive 17-Hydrecoxetron, and its clearing half-life is 24 hours. It is mostly excreted through urine and feces, which both account for 42% of the consumed amount.

Description

Exemestane was launched in US and other countries for the treatment of estrogendependent tumors and postmenopausal breast cancer. It is a novel steroidal compound structurally related to the natural substrate for the biosynthesis of estrogen, androstanedione, and can be synthesized by methylidenation of androsta-1, 4-dien- 17beta-ol-3-one in 6 position then oxidation of the alcohol function. Exemestane is an irreversible inactivator of the aromatase enzyme system, so inducing in vivo a dose-related sustained suppression of serum estrogen and minimal endocrine activity. It is the first steroidal representative of the third-generation of orally active aromatase inhibitors with a highly potent and selective mechanism of action, displaying good tolerability and safety profile. In rats with DMBA-induced mammary tumors, 10 to 100 mglkg of exemestan administered po twice-daily for 4 weeks resulted in 76 to 88% regression. In women failing anti-estrogen therapy with tamoxifen, this agent has demonstrated high activity in locally advanced or metastatic disease. In addition, it may also have potential for breast cancer prevention.

Hazard

A reproductive hazard.
InChI:InChI=1/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14?,15?,16?,19-,20+/m1/s1

107868-30-4 Well-known Company Product Price

Brand (Code)Product description CAS number Packaging Price Detail
Sigma-Aldrich (PHR1634)  Exemestane  (pharmaceutical secondary standard; traceable to USP) 107868-30-4 PHR1634-1G 1,027.26CNY Detail
Sigma-Aldrich (Y0001747)  Exemestane  European Pharmacopoeia (EP) Reference Standard 107868-30-4 Y0001747 1,880.19CNY Detail
Sigma-Aldrich (Y0001756)  Exemestane for system suitability  European Pharmacopoeia (EP) Reference Standard 107868-30-4 Y0001756 1,880.19CNY Detail
USP (1269050)  Exemestane  United States Pharmacopeia (USP) Reference Standard 107868-30-4 1269050-150MG 4,326.66CNY Detail
Sigma (PZ0006)  Exemestane  ≥98% (HPLC) 107868-30-4 PZ0006-5MG 1,115.01CNY Detail

107868-30-4SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 20, 2017

Revision Date: Aug 20, 2017

1.Identification

1.1 GHS Product identifier

Product name exemestane

1.2 Other means of identification

Product number -
Other names 6-methylenandrosta-1,4-diene-3,17-dione

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:107868-30-4 SDS

107868-30-4Synthetic route

17β-hydroxy-6-methylen- androsta-1,4-dien-3-one
122370-91-6

17β-hydroxy-6-methylen- androsta-1,4-dien-3-one

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With Jones reagent In acetone at -20℃; Jones oxidation; Inert atmosphere;100%
With jones reagent In acetone at -20℃; for 0.25h;85%
With Jones reagent In acetone at 0℃; Product distribution / selectivity;
6α-hydroxymethylandrosta-1,4-diene-3,17-dione
933455-74-4

6α-hydroxymethylandrosta-1,4-diene-3,17-dione

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
Stage #1: 6α-hydroxymethylandrosta-1,4-diene-3,17-dione With methanesulfonyl chloride; triethylamine In dichloromethane at 0 - 30℃;
Stage #2: With methanol; potassium hydroxide at 40 - 50℃;
90%
17-hydroxyimino-6-methylenandrosta-1,4-diene-3-one

17-hydroxyimino-6-methylenandrosta-1,4-diene-3-one

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With toluene-4-sulfonic acid In water; acetone at 25 - 30℃; for 10h; Solvent; Reagent/catalyst; Temperature; Jones Oxidation; Inert atmosphere;88.2%
6-methylene-androst-4-ene 3,17-dione
19457-55-7

6-methylene-androst-4-ene 3,17-dione

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With N,O-Bis(trimethylsilyl)trifluoroacetamide; chloranil; trifluorormethanesulfonic acid In toluene at 108 - 110℃; for 0.75h; Product distribution / selectivity; Heating / reflux;81.8%
With trifluorormethanesulfonic acid; N,O-Bis(trimethylsilyl)trifluoroacetamide; chloranil In toluene Inert atmosphere; Reflux;81%
With tert-butyldimethylsilyl chloride; 2,3-dicyano-5,6-dichloro-p-benzoquinone In 1,4-dioxane at 0 - 20℃;30.2%
methanol
67-56-1

methanol

6β-hydroxymethylandrosta-1,4-diene-3,17-dione
121021-51-0

6β-hydroxymethylandrosta-1,4-diene-3,17-dione

A

(6S,8R,9S,10R,13S,14S)-6-(methoxymethyl)-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione

(6S,8R,9S,10R,13S,14S)-6-(methoxymethyl)-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione

B

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With hydrogenchloride at 20℃; for 24h;A 8%
B 60%
6-Methylen-4-androsten-3,17-dion
19457-55-7, 51154-17-7

6-Methylen-4-androsten-3,17-dion

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With 1-hydroxy-3H-benz[d][1,2]iodoxole-1,3-dione In dimethyl sulfoxide; toluene at 85℃; for 48h; Inert atmosphere; Large scale;56.7%
Androsta-1,4-diene-3,17-dione
897-06-3

Androsta-1,4-diene-3,17-dione

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: 20 h / Heating
2: 1.10 g / benzene; ethanol; H2O / 5 h / 20 °C
3: 60 percent / conc. HCl / 24 h / 20 °C
View Scheme
Multi-step reaction with 3 steps
1.1: hydroxylamine hydrochloride; sodium acetate / water; ethanol / 6 h / Inert atmosphere; Reflux
2.1: N,N-dimethylammonium chloride / i-Amyl alcohol / 2 h / Inert atmosphere; Reflux
2.2: 15 h / 140 °C
3.1: toluene-4-sulfonic acid / water; acetone / 10 h / 25 - 30 °C / Inert atmosphere
View Scheme
Multi-step reaction with 4 steps
1: orthoformic acid triethyl ester; toluene-4-sulfonic acid / tetrahydrofuran / 12 h / 40 - 45 °C / Large scale
2: tetrahydrofuran; ethanol / 10 h / 40 - 45 °C / Large scale
3: hydrogenchloride / tetrahydrofuran; ethanol / 1 h / Large scale
4: 1-hydroxy-3H-benz[d][1,2]iodoxole-1,3-dione / dimethyl sulfoxide; toluene / 48 h / 85 °C / Inert atmosphere; Large scale
View Scheme
1α,3-dipyrrolidinylandrosta-3,5-dien-17-one
67737-88-6

1α,3-dipyrrolidinylandrosta-3,5-dien-17-one

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 1.10 g / benzene; ethanol; H2O / 5 h / 20 °C
2: 60 percent / conc. HCl / 24 h / 20 °C
View Scheme
1-dehydrotestosterone
846-48-0

1-dehydrotestosterone

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 1.) Me2NH*HCl / 1.) isoamyl alcohol, reflux, 2 h, 2.) isoamyl alcohol, reflux, 15 h
2: 85 percent / Jones reagent / acetone / 0.25 h / -20 °C
View Scheme
C21H28O5S
861395-77-9

C21H28O5S

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With potassium hydroxide In methanol; dichloromethane; water at 25℃; Heating / reflux;
pyrographite
7440-44-0

pyrographite

6-methylene-androst-4-ene 3,17-dione
19457-55-7

6-methylene-androst-4-ene 3,17-dione

tert-butyl alcohol
75-65-0

tert-butyl alcohol

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With selenium(IV) oxide In ethyl acetate
6-hydroxymethyl-androsta-1,4-diene-3,17-dione

6-hydroxymethyl-androsta-1,4-diene-3,17-dione

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With toluene-4-sulfonic acid In toluene at 80 - 90℃; under 315 Torr; for 4h; Purification / work up;
With toluene-4-sulfonic acid In toluene at 90℃; for 3h; Purification / work up;
With camphor-10-sulfonic acid In toluene at 90℃; for 7h; Purification / work up;
With (1S)-10-camphorsulfonic acid In ethyl acetate at 70 - 80℃; for 32h; Purification / work up;
Stage #1: 6-hydroxymethyl-androsta-1,4-diene-3,17-dione With pyridine; p-toluenesulfonyl chloride at 0℃; for 48h;
Stage #2: With potassium hydroxide In methanol; water at 65℃; for 2h; Purification / work up;
dehydroepiandrosterone
53-43-0

dehydroepiandrosterone

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: toluene / 1 h / 120 °C / Inert atmosphere
1.2: 0.33 h / 20 °C / Inert atmosphere
1.3: 3 h / 20 °C / Inert atmosphere
2.1: orthoformic acid triethyl ester; toluene-4-sulfonic acid / ethanol; tetrahydrofuran / 3 h / 40 °C
2.2: 4 h / 40 °C
3.1: Arthrobacter simplex ATCC6946 culture / aq. buffer / 33 °C / Microbiological reaction
View Scheme
3-Aethoxy-androstadien-(3,5)-on-(17)
972-46-3

3-Aethoxy-androstadien-(3,5)-on-(17)

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: tetrahydrofuran; ethanol / 10 h / 40 - 45 °C / Large scale
2: hydrogenchloride / tetrahydrofuran; ethanol / 1 h / Large scale
3: 1-hydroxy-3H-benz[d][1,2]iodoxole-1,3-dione / dimethyl sulfoxide; toluene / 48 h / 85 °C / Inert atmosphere; Large scale
View Scheme
6-methyleneandrostenediol ketal

6-methyleneandrostenediol ketal

exemestane
107868-30-4

exemestane

Conditions
ConditionsYield
With toluene-4-sulfonic acid In tetrahydrofuran; water at 20 - 25℃; for 10h; Inert atmosphere;
exemestane
107868-30-4

exemestane

FCE27353
184972-12-1

FCE27353

Conditions
ConditionsYield
With 3-chloro-benzenecarboperoxoic acid In dichloromethane for 48h; Ambient temperature;80%
exemestane
107868-30-4

exemestane

C20H24N6O2

C20H24N6O2

Conditions
ConditionsYield
With copper(l) iodide; tert-Butyl peroxybenzoate; trimethylsilylazide In acetonitrile at 50℃; for 6h; Reagent/catalyst; Solvent; Schlenk technique; Inert atmosphere; Green chemistry;75%
exemestane
107868-30-4

exemestane

A

6α-methylandrost-4-ene-3,17-dione
2241-94-3

6α-methylandrost-4-ene-3,17-dione

B

C20H30O2

C20H30O2

C

6β-methylandrost-4-ene-3,17-dione
5696-36-6

6β-methylandrost-4-ene-3,17-dione

Conditions
ConditionsYield
With diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate; 5%-palladium/activated carbon In ethanol for 18h; Reflux; stereoselective reaction;A n/a
B 62%
C n/a
formaldehyd
50-00-0

formaldehyd

exemestane
107868-30-4

exemestane

C21H24O2

C21H24O2

Conditions
ConditionsYield
With N,N-dimethylammonium chloride In ethanol at 78℃; for 3h; Temperature; Mannich Aminomethylation;54.1%
4-Fluorobenzenesulfonyl chloride
349-88-2

4-Fluorobenzenesulfonyl chloride

exemestane
107868-30-4

exemestane

(6S,8R,9S,10R,13S,14S)-6-(((4-fluorophenyl)sulfonyl)methyl)-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione

(6S,8R,9S,10R,13S,14S)-6-(((4-fluorophenyl)sulfonyl)methyl)-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione

Conditions
ConditionsYield
With fac-tris(2-phenylpyridinato-N,C2')iridium(III); tris-(trimethylsilyl)silane In acetonitrile at 20℃; for 16h; Irradiation; diastereoselective reaction;50%
exemestane
107868-30-4

exemestane

A

6-methylandrosta-1,4,6-trien-17β-ol

6-methylandrosta-1,4,6-trien-17β-ol

B

17β-hydroxy-6-methylen- androsta-1,4-dien-3-one
122370-91-6

17β-hydroxy-6-methylen- androsta-1,4-dien-3-one

Conditions
ConditionsYield
With sodium tetrahydroborate; acetic acid; trifluoroacetic acid In dichloromethane; acetonitrile at 20℃; for 11h; Inert atmosphere;A 11.3 mg
B 39%
Bromotrifluoromethane
75-63-8

Bromotrifluoromethane

exemestane
107868-30-4

exemestane

A

C21H25F3O3

C21H25F3O3

B

C21H25F3O3

C21H25F3O3

Conditions
ConditionsYield
With cobalt(II) tetrafluoroborate hexahydrate; N-isopropyl-N,2-dimethylpropan-2-amine In water; N,N-dimethyl-formamide; acetonitrile at 65℃; for 24h; Sealed tube;A 30%
B 33%
Bromotrifluoromethane
75-63-8

Bromotrifluoromethane

exemestane
107868-30-4

exemestane

A

C21H25F3O3

C21H25F3O3

B

C21H25F3O3

C21H25F3O3

Conditions
ConditionsYield
With cobalt(II) tetrafluoroborate hexahydrate; N-isopropyl-N,2-dimethylpropan-2-amine In N,N-dimethyl-formamide; acetonitrile at 65℃; for 24h;A 30%
B 33%
nitromethane
75-52-5

nitromethane

exemestane
107868-30-4

exemestane

6α-(2-Nitroethyl)androsta-1,4-dien-3,17-dion
911856-13-8

6α-(2-Nitroethyl)androsta-1,4-dien-3,17-dion

Conditions
ConditionsYield
With sodium ethanolate In ethanol for 22h; Michael addition; Heating;32%
exemestane
107868-30-4

exemestane

A

6α-spirooxiranandrosta-1,4-diene-3,17-dione

6α-spirooxiranandrosta-1,4-diene-3,17-dione

B

6α-spirooxiranandrosta-1,4-diene-3,17-dione

6α-spirooxiranandrosta-1,4-diene-3,17-dione

Conditions
ConditionsYield
With formic acid; dihydrogen peroxide In dichloromethane at 20℃; for 96h;A 21%
B 76.1 mg
L-Cysteine
52-90-4

L-Cysteine

exemestane
107868-30-4

exemestane

6-methylcysteinylandrosta-1,4-diene-3,17-dione

6-methylcysteinylandrosta-1,4-diene-3,17-dione

Conditions
ConditionsYield
With potassium hydroxide In methanol at 20℃; for 24h; Inert atmosphere;13%
exemestane
107868-30-4

exemestane

1α,2α-epoxy-6-methylenandrost-4-ene-3,17-dione

1α,2α-epoxy-6-methylenandrost-4-ene-3,17-dione

Conditions
ConditionsYield
With dihydrogen peroxide; sodium hydroxide In methanol; water at 0 - 20℃; for 24.5h;11%
exemestane
107868-30-4

exemestane

diethyl malonate
105-53-3

diethyl malonate

Diethyl-2-(3,17-dioxoandrosta-1,4-dien-6β-ylmethyl)-malonat

Diethyl-2-(3,17-dioxoandrosta-1,4-dien-6β-ylmethyl)-malonat

Conditions
ConditionsYield
With sodium In ethanol for 7h; Michael addition; Heating;6%
exemestane
107868-30-4

exemestane

6α-(2-Oxoethyl)androsta-1,4-dien-3,17-dion
911856-14-9

6α-(2-Oxoethyl)androsta-1,4-dien-3,17-dion

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: 32 percent / NaOEt / ethanol / 22 h / Heating
2.1: KOH / methanol / 3 h / 20 °C
2.2: 31 percent / aq. H2SO4 / methanol / 4 h / cooling
View Scheme
exemestane
107868-30-4

exemestane

Dimethyl-4-[(3,17-dioxoandrosta-1,4-dien-6α-yl)methyl]-2,6-dimethyl-3,5-pyridindicarboxylat

Dimethyl-4-[(3,17-dioxoandrosta-1,4-dien-6α-yl)methyl]-2,6-dimethyl-3,5-pyridindicarboxylat

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: 32 percent / NaOEt / ethanol / 22 h / Heating
2.1: KOH / methanol / 3 h / 20 °C
2.2: 31 percent / aq. H2SO4 / methanol / 4 h / cooling
3.1: 58 percent / acetic acid / 22 h / 20 - 60 °C
4.1: 87 percent / CAN / acetone; H2O / 0.5 h
View Scheme
exemestane
107868-30-4

exemestane

Dimethyl-4-[(3,17-dioxoandrosta-1,4-dien-6α-yl)methyl]-2,6-dimethyl-1,4-dihydro-3,5-pyridindicarboxylat
911856-15-0

Dimethyl-4-[(3,17-dioxoandrosta-1,4-dien-6α-yl)methyl]-2,6-dimethyl-1,4-dihydro-3,5-pyridindicarboxylat

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: 32 percent / NaOEt / ethanol / 22 h / Heating
2.1: KOH / methanol / 3 h / 20 °C
2.2: 31 percent / aq. H2SO4 / methanol / 4 h / cooling
3.1: 58 percent / acetic acid / 22 h / 20 - 60 °C
View Scheme
exemestane
107868-30-4

exemestane

6-Hydroxymethylexemestane

6-Hydroxymethylexemestane

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 80 percent / 50percent m-chloroperbenzoic acid / CH2Cl2 / 48 h / Ambient temperature
2: 38 percent / 20percent aq. HClO4 / tetrahydrofuran / 3 h / Ambient temperature
View Scheme
exemestane
107868-30-4

exemestane

6α/β-hydroxy-6α/β-hydroxymethylandrosta-1,4-diene-3,17-dione

6α/β-hydroxy-6α/β-hydroxymethylandrosta-1,4-diene-3,17-dione

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 80 percent / 50percent m-chloroperbenzoic acid / CH2Cl2 / 48 h / Ambient temperature
2: 42 percent / 20percent aq. HClO4 / tetrahydrofuran / 3 h / Ambient temperature
View Scheme

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