3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester CAS 287944-16-5

Introduction:Basic information about 3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester CAS 287944-16-5, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester Basic information

Product Name:3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester
Synonyms:2H-Pyran, 3,6-dihydro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-;4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-2h-pyran, 95%;3,6-Dihydro-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-2H-pyran;2-(3,6-dihydro-2H-pyran-4-yl)-4,4,5,5-tetraMethyl-1,3,2-dioxaborolane;3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester;3,6-Dihydro-2H-pyran-4-bo...;3,6-Dihydro-4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-;3,6-Dihydro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2H-pyran, 2-(3,6-Dihydro-2H-pyran-4-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
CAS:287944-16-5
MF:C11H19BO3
MW:210.08
EINECS:
Product Categories:Boronate Esters;Boronic Acids and Derivatives;Chemical Synthesis;Heteroaryl Boronate Esters;Organometallic Reagents;Organoborons;Organic boronic acid
Mol File:287944-16-5.mol

3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester Chemical Properties

Melting point 63-67℃
Boiling point 238.6±50.0 °C(Predicted)
density 1.01±0.1 g/cm3(Predicted)
storage temp. 2-8°C
form Solid
color White to off-white
Water Solubility Slightly soluble in water.
Sensitive Moisture Sensitive
InChIInChI=1S/C11H19BO3/c1-10(2)11(3,4)15-12(14-10)9-5-7-13-8-6-9/h5H,6-8H2,1-4H3
InChIKeyDOSGEBYQRMBTGS-UHFFFAOYSA-N
SMILESC1OCC=C(B2OC(C)(C)C(C)(C)O2)C1

Safety Information

Hazard Codes Xn
Risk Statements 22
Safety Statements 20-35
WGK Germany 3
HS Code 29349990
Storage Class11 - Combustible Solids
Hazard ClassificationsAcute Tox. 4 Oral

3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester Usage And Synthesis

UsesIt plays an important role as intermediate for organic synthesis agrochemical, pharmaceutical and dyestuff field.
Uses3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester can be used:
  • To prepare 1,2-dihydro-2-oxopyridine based endocannabinoid system (ECS) modulators.
  • As an intermediate in the synthesis of embryonic ectoderm development (EED) inhibitors.
  • To prepare pyrrolotriazine based IRAK4 inhibitors.

Synthesis

73183-34-3

188975-30-6

287944-16-5

To a 250 mL round-bottomed flask, a solution of 3,6-dihydro-2H-pyran-4-trifluoromethanesulfonate (2.7 g, 11.6 mmol), PdCl2(dppf) (440 mg, 0.6 mmol), and potassium acetate (3 g, 36 mmol) was added to a solution of dioxane (20 mL), which was subsequently displaced three times with argon to remove air. The reaction mixture was stirred at 80 °C overnight. Upon completion of the reaction, it was cooled to room temperature and filtered through a short column containing diatomaceous earth to remove solid impurities. The filtrate was concentrated under reduced pressure and the residue was purified by column chromatography (eluent: 10% dichloromethane solution of hexane) to give the final white solid product 3,6-dihydro-2H-pyran-4-boronic acid pinacol ester (2 g, 81% yield).

References[1] Patent: WO2008/153858, 2008, A1. Location in patent: Page/Page column 307
[2] Patent: US2012/316147, 2012, A1. Location in patent: Page/Page column 32
[3] Patent: WO2012/168350, 2012, A1. Location in patent: Page/Page column 76; 77
[4] ACS Medicinal Chemistry Letters, 2016, vol. 7, # 7, p. 666 - 670
[5] Patent: US2008/318935, 2008, A1. Location in patent: Page/Page column 65

3,6-Dihydro-2H-pyran-4-boronic acid pinacol ester Preparation Products And Raw materials

Raw materials1,3,2-Dioxaborolane, 4,4,5,5-tetramethyl-2-[1-methylene-3-(2-propen-1-yloxy)propyl]--->Bis(pinacolato)diboron-->Pinacol-->4-BROMO-3,6-DIHYDRO-2H-PYRAN-->Trimethyl borate-->3,6-DIHYDRO-2H-PYRAN-4-YL TRIFLUORO-METHANESULFONATE-->Potassium Acetate-->1,4-Dioxane
Preparation Products2-FLUORO-3-(TETRAHYDRO-2H-PYRAN-4-YL)-PYRIDINE-->4-(3-bromophenyl)-3,6-dihydro-2H-Pyran
3,6-DICHLORO-2-HYDROXY BENZOIC ACID CAS 3401-80-7
3,6-Dihydro-3-methyl-N-nitro-2H-1,3,5-oxadiazin-4-amine CAS 153719-38-1
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