3-Chloro-2-methoxyphenylboronic acid

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3-Chloro-2-methoxyphenylboronic acid Basic information
Product Name:3-Chloro-2-methoxyphenylboronic acid
Synonyms:3-Chloro-2-methoxybenzeneboronicacid;3-Chloro-2-methoxybenzeneboronic acid 99%;Boronic acid, (3-chloro-2-methoxyphenyl)- (9CI);Boronic acid, B-(3-chloro-2-methoxyphenyl)-;3-Chloro-2-methoxyphenylboronic acid (contains varying amounts of Anhydride);3-Chloro-2-methoxyphenylboronic acid
CAS:179898-50-1
MF:C7H8BClO3
MW:186.4
EINECS:
Product Categories:Boronic Acid;API intermediates
Mol File:179898-50-1.mol
3-Chloro-2-methoxyphenylboronic acid Structure
3-Chloro-2-methoxyphenylboronic acid Chemical Properties
Boiling point 356.9±52.0 °C(Predicted)
density 1.32±0.1 g/cm3(Predicted)
storage temp. under inert gas (nitrogen or Argon) at 2-8°C
pka7.58±0.58(Predicted)
form solid
color Off-white
Safety Information
HS Code 2931900090
MSDS Information
3-Chloro-2-methoxyphenylboronic acid Usage And Synthesis
Uses3-Chloro-2-methoxyphenylboronic Acid is a reagent used in the synthesis of a selective 17β-HSD1 inhibitor in the therapeutic treatment of endometriosis.
Synthesis
1-Bromo-3-chloro-2-methoxybenzene

174913-10-1

Triisopropyl borate

5419-55-6

3-CHLORO-2-METHOXYPHENYLBORONIC ACID

179898-50-1

General procedure for the synthesis of 3-chloro-2-methoxyphenylboronic acid from 1-bromo-3-chloro-2-methoxybenzene and triisopropyl borate: 1-bromo-3-chloro-2-methoxybenzene (113.2 g, 426.4 mmol) was dissolved in tetrahydrofuran (1000 mL), and cooled to -78°C. At the same temperature 1.7 M tertiary-butyllithium (t-BuLi) was added slowly to a tert-butyl lithium (t-BuLi) ) to a hexane solution (251.7 mL, 426.4 mmol). The reaction mixture was stirred at -78°C for 1 h. Triisopropyl borate (B(OiPr)3) (113.2 mL, 852.4 mmol) was added, followed by gradual warming of the reaction mixture to room temperature and continued stirring for 3 hours. Upon completion of the reaction, 2 N aqueous hydrochloric acid (800 mL) was added to the mixture and stirred at room temperature for 1.5 hours. The resulting precipitate was collected by filtration, washed sequentially with water and ether and dried under vacuum. The crude product was recrystallized by a solvent mixture of chloroform and ethyl acetate and dried to give 3-chloro-2-methoxyphenylboronic acid as a white solid (89.6 g, 91% yield; Mass Spectrometry (MS): [M + H]+ = 230.

References[1] Patent: KR2018/10165, 2018, A. Location in patent: Paragraph 0207-0210
3-Chloro-2-methoxyphenylboronic acid Preparation Products And Raw materials
Raw materials1-Bromo-3-chloro-2-methoxybenzene-->Triisopropyl borate-->Trimethyl borate-->Water-->Tetrahydrofuran-->tert-Butyllithium-->Hydrochloric acid
Tag:3-Chloro-2-methoxyphenylboronic acid(179898-50-1) Related Product Information
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