BAZEDOXIFENE ACETATE

Product Name: BAZEDOXIFENE ACETATE
CAS No.: 198481-33-3
Chemical Name: BAZEDOXIFENE ACETATE
Synonyms: Viviant;Way-140424;WAY-TES 424;WAY-TSE-424;Unii-J70472ud3d;3-Oxo Ziprasidone;Badoxifen acetate;Bazedoxifene acetat;Bazedoxifen Acetate;BAZEDOXIFENE ACETATE
CBNumber: CB71011079
Molecular Formula: C32H38N2O5
Formula Weight: 530.67
MOL File: 198481-33-3.mol

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BAZEDOXIFENE ACETATE Property

Melting point:: 174-178°
storage temp.: -20°C
solubility: DMSO: soluble15mg/mL, clear
form: powder
color: white to beige
InChI: InChI=1S/C30H34N2O3.C2H4O2/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31;1-2(3)4/h6-15,20,33-34H,2-5,16-19,21H2,1H3;1H3,(H,3,4)
InChIKey: DGEPGJZKMFNSDD-UHFFFAOYSA-N
SMILES: C(=O)(O)C.C(C1C=CC(OCCN2CCCCCC2)=CC=1)N1C2C=CC(O)=CC=2C(C)=C1C1C=CC(O)=CC=1

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Safety

WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0018
Product name: Bazedoxifene acetate
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $132
Updated: 2024/03/01

Sigma-Aldrich

Product number: PZ0018
Product name: Bazedoxifene acetate
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $537
Updated: 2024/03/01

Cayman Chemical

Product number: 15005
Product name: Bazedoxifene acetate
Purity: ≥98%
Packaging: 5mg
Price: $111
Updated: 2024/03/01

Cayman Chemical

Product number: 15005
Product name: Bazedoxifene acetate
Purity: ≥98%
Packaging: 10mg
Price: $210
Updated: 2024/03/01

Cayman Chemical

Product number: 15005
Product name: Bazedoxifene acetate
Purity: ≥98%
Packaging: 25mg
Price: $493
Updated: 2024/03/01

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BAZEDOXIFENE ACETATE Chemical Properties,Usage,Production

Chemical Properties

Pale Beige Solid

Uses

Bazedoxifene acetate has been used to study its efficacy in inhibiting the interleukin-6 (IL-6)/IL-6R/glycoprotein 130 pathway and its effects on medulloblastoma cells.

Uses

Bazedoxifene Acetate is a nonsteroidal selective estrogen receptor modulator (SERM). Bazedoxifene Acetate is used as an antiosteoporotic.

Biological Activity

bazedoxifene, a novel selective estrogen receptor modulator (serm), has been developed to have favorable effects on bone and the lipid profile while minimizing stimulation of uterine or breast tissues. two large phase iii

Biochem/physiol Actions

Bazedoxifene is a third generation nonsteroidal selective estrogen receptor modulator (SERM), used clinically to treat postmenopausal osteoporosis. Bazedoxifene binds to estrogen receptor-α with IC50 = 26 nM, similar to that of raloxifene, but lower affinity than 17-β estradiol. Bazedoxifene did not stimulate proliferation of MCF-7 cells, instead inhibited 17β -estradiol-induced proliferation with IC50 = 0.19 nM, exhibiting a desirable profile of agonist/antagonist activity.

Clinical Use

The selective estrogen receptor modulator bazedoxifene acetate was approved in Spain for the treatment of osteoporosis in postmenopausal women. The drug was discovered by Wyeth (now Pfizer) and licensed to Almirall. Clinical trials with bazedoxifene along with conjugated estrogens demonstrated significant improvement in bone mineral density and prevented bone loss in postmenopausal women without osteoporosis. It also reduces fracture risks among women with postmenopausal osteroporosis.

Synthesis

Among many syntheses reported for this drug, the most recent process scale synthesis (multi-kg scale) is highlighted and involves the union of azepane ether 9 and indole 12. 4-Hydroxybenzyl alcohol (6) was converted in two steps to chloride 9 (the Scheme). The reaction of 6 with 2-chloroethyl azepane hydrochloride (7) in a biphasic mixture of sodium hydroxide and toluene in the presence of tetrabutylammonium bromide (TBAB) gave the desired intermediate alcohol 8 in 61% yield. Treatment of 8 with thionyl chloride (SOCl2) gave the requisite chloride 9 in 61% yield. The reaction of 2-bromopropiophenone (10) with an excess of 4-benzyloxy aniline hydrochloride (11) in the presence of triethylamine (TEA) in N,N-dimethylformamide (DMF) at elevated temperatures resulted in indole 12 in 65% yield. Alkylation of 12 with benzylchloride 9 in the presence of sodium hydride (NaH) afforded N-alkylated compound 13. The benzyl ether functionalities from compound 13 were removed via hydrogenolysis and subsequently subjected to acidic conditions, providing diol 14 as the hydrochloride salt in 91% yield. The hydrochloride was then exchanged for the acetate via free base preparation with 5% sodium bicarbonate or triethylamine, followed by treatment with acetic acid giving bazedoxifene acetate (II) in 73¨C85% yield.

BAZEDOXIFENE ACETATE Preparation Products And Raw materials

Raw materials

Preparation Products

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BAZEDOXIFENE ACETATE Suppliers

Canada 1 China 181 India 9 United Kingdom 4 United States 20 Global 215

MedChemexpress LLC

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View Lastest Price from BAZEDOXIFENE ACETATE manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD

Product: Bazedoxifene acetate 198481-33-3
Price: US $0.00/g
Min. Order: 1g
Purity: 98%min
Supply Ability: 1000g
Release date: 2021-09-17

PNP Biotech Co. Ltd

Product: Bazedoxifene acetate 198481-33-3
Price: US $0.00/kg
Min. Order: 25kg
Purity: 98%-99%
Supply Ability: Inquiry
Release date: 2022-09-16

Zhuozhou Wenxi import and Export Co., Ltd

Product: BAZEDOXIFENE ACETATE 198481-33-3
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-11

198481-33-3, BAZEDOXIFENE ACETATERelated Search:

5-O-Benzylbazedoxifene 1-[2-[4-(Chloromethyl)phenoxy]ethyl]hexahydro-1H-azepine sodium hexametaphosphate Sodium tripolyphosphate Hyaluronic acid 1-(4-hydroxybenzyl)-2-(4-hydroxyphenyl)-3-Methyl-1H-indol-5-ol Bazedoxifene 4’-β-D-Glucuronide Tolvaptan 1-[4-(2-AZEPAN-1-YL-ETHOXY)-BENZYL]-5-BENZYLOXY-2-(4-BENZYLOXY-PHENYL)-3-METHYL-1H-INDOLE 3-METHYL-5-(PHENYLMETHOXY)-2-[4-(PHENYLMETHOXY)PHENYL]-1H-INDOLE BenzeneMethanol, 4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]- (hydrochloride) 4-[2-(1-AZEPANYL)ETHOXY]BENZYL CHLORIDE HCL 1-[[4-[2-(Hexahydro-1-oxido-1H-azepin-1-yl)ethoxy]phenyl]Methyl]-2-(4-hydroxyphenyl)-3-Methyl-1H-indol-5-ol Bazedoxifene-d4 Acetate Bazedoxifene Bazedoxifene Impurity 8 Flibaserin Bazedoxifene impurity 6

BAZEDOXIFENE ACETATE

1-(p-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol monoacetate (salt)

1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-, monoacetate (salt)

Bazedoxifene acetate [usan]

Unii-J70472ud3d

Viviant

Way-140424

1-((4-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol monoacetate

1-[[4-[2-(Hexahydro-1H-azepin-1-yl)ethoxy]phenyl]Methyl]-2-(4-hydroxyphenyl)-3-Methyl-

WAY-TES 424

1-[4-(2-Azepan-1-yl-ethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate

WAY-TSE-424

3-Oxo Ziprasidone

Bazedoxifene acetat

1-[[4-[2-(Hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate

TSE 424; VIVIANT; WAY-TES 424

1H-Indol-5-ol, 1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-, acetate (1:1)

Bazedoxifene Acetate (TSE-424)

Bazedoxifene (acetate)-B

Bazedoxifene acetateQ: What is Bazedoxifene acetate Q: What is the CAS Number of Bazedoxifene acetate Q: What is the storage condition of Bazedoxifene acetate Q: What are the applications of Bazedoxifene acetate

Badoxifen acetate

Bazedoxifen Acetate

198481-33-3

1984841-33-3

1198481-33-3

C30H34N2O3C2H4O2

Bazedoxifene Acetate

Inhibitors

198481-33-3