Identification | Back Directory | [Name]
4-[2-(1-AZEPANYL)ETHOXY]BENZYL CHLORIDE HCL | [CAS]
223251-25-0 | [Synonyms]
Bazedoxifene intermediate Landiolol Impurity 13 Heoxalate -[2-(1-AZEPANYL)ETHOXY]BENZYL CHLORIDE HCL 4-[2-(1-AZEPANYL)ETHOXY]BENZYL CHLORIDE HCL 1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane HCI 1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane HCl 1-{2-[4-(Chloromethyl)phenoxy]ethyl}azepane hydrochloride (1:1) 1-{2-[4-(Chloromethyl)phenoxy]ethyl}azepane hydrochloride (1... 1-[2-[4-(ChloroMethyl)phenoxy]ethyl]hexahydro-1H-azepine hydrochloride 1-(2-(4-(chloromethyl)phenoxy)ethyl)azepane Hydrochloride(For export only) 1-[2-[4-(chloromethyl)phenoxy]ethyl]hexahydro-1H-Azepine hydrochloride (1:1) 1H-Azepine, 1-[2-[4-(chloroMethyl)phenoxy]ethyl]hexahydro-, hydrochloride (1:1) 1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane hydrochlorideQ: What is
1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane hydrochloride Q: What is the CAS Number of
1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane hydrochloride Q: What is the storage condition of
1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane hydrochloride Q: What are the applications of
1-(2-(4-(Chloromethyl)phenoxy)ethyl)azepane hydrochloride | [EINECS(EC#)]
695-296-7 | [Molecular Formula]
C15H23Cl2NO | [MDL Number]
MFCD11865353 | [MOL File]
223251-25-0.mol | [Molecular Weight]
304.26 |
Hazard Information | Back Directory | [Uses]
1-[2-[4-(Chloromethyl)phenoxy]ethyl]hexahydro-1H-azepine Hydrochloride is a useful synthetic intermediate in the synthesis of Bazedoxifene (B129250); a nonsteroidal selective estrogen receptor modulator (SERM). Also used as an antiosteoporotic. | [Synthesis]
S4: (4-(2-(Azepan-1-yl)ethoxy)phenyl)methanol (561 g) obtained from step S3 was dissolved in 1.2 L of tetrahydrofuran and cooled to 0 °C. Thionyl chloride (320 g) was added slowly and dropwise under stirring, keeping the reaction temperature not exceeding 55 °C, and the reaction was gradually warmed up at this temperature for 6 hours. Upon completion of the reaction, about 600 mL of solvent was removed by distillation. To the residue was added 300 mL of ethyl acetate, the mixture was cooled to 0 °C and stirred for 30 minutes. It was subsequently filtered and the solid was washed with 300 mL of ethyl acetate. The resulting solid was dried to give 1-(2-(4-(chloromethyl)phenoxy)ethyl)azepane hydrochloride (619 g) in 90% yield and 99% HPLC purity. | [References]
[1] Patent: CN107400087, 2017, A. Location in patent: Paragraph 0045 [2] Patent: WO2011/22596, 2011, A2. Location in patent: Page/Page column 4; 24 [3] Patent: WO2011/22596, 2011, A2. Location in patent: Page/Page column 22; 23 [4] Angewandte Chemie - International Edition, 2013, vol. 52, # 22, p. 5795 - 5798 [5] Angew. Chem., 2013, p. 5999 |
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