Guaiacol

HCID 460CAS 26638-03-9

Basic information

Standard SMILES
COc1ccccc1O
InChIKey
LHGVFZTZFXWLCP-UHFFFAOYSA-N
Molecular formula
C7H8O2
Average molar mass
124.14 g/mol
Monoisotopic mass
124.0524295

Overview

O-methoxyphenol appears as colorless to amber crystals or liquid. Density (of solid) 1.129 g / cm3. Solidifies at 28 °C (82.4 °F), but may remain liquid for a long time even at a much lower temperature. Slightly water soluble. Soluble in aqueous sodium hydroxide. Used medicinally as an expectorant. Used, because of its anti-oxidant properties, as an anti-skinning agent for paints.

Names & identifiers

Preferred name
Guaiacol
IUPAC
2-methoxyphenol
English name
2-Methoxyphenol
Molecular formula
C7H8O2
Molecular weight
124.13722

Names & synonyms

guaiacol2-Methoxyphenol90-05-1o-Methoxyphenol2-Hydroxyanisoleo-GuaiacolGuaiastilPyroguaiac acido-HydroxyanisolePhenol, 2-methoxy-Anastil1-Hydroxy-2-methoxybenzene
Show more names
Pyrocatechol monomethyl etherGuaicolPhenol, o-methoxy-GuaicolinaGuajolGuasolO-Methyl catecholCreodon

Database identifiers

CAS
26638-03-9、90-05-1、9009-62-5
PubChem CID
460
DTXSID
DTXSID0023113
ChEMBL
CHEMBL13766
ChEBI
CHEBI:28591
UNII
6JKA7MAH9C
EC Number
201-964-7、804-496-7
Nikkaji
J3.217D

Properties

Computed structural properties

XLogP
1.3
Topological polar surface area
29.5 Ų
Hydrogen bond donors
1
Hydrogen bond acceptors
2
Rotatable bonds
1
Heavy atoms
9

Experimental & physicochemical properties

Chemical ClassesBiological Agents -> Plant Oils and Extracts
DrugsPharmaceuticals -> Listed in ZINC15
SpringerMaterials Properties13C nuclear magnetic resonance spectrum
FragrancesFragrance Ingredient (Guaiacol) -> IFRA transparency List
LogP · 3 items

log Kow = 1.32

1.32

1.35

Odor · 2 items

Aromatic odor

CHARACTERISTIC SWEET ODOR, SLIGHTLY PHENOLIC

Physicochemical properties

Melting point
32 °C · 32 °C
Boiling point
204 · 204-206 °C
Density
1.1287 g/cm3 · 1.1287 g/cm3(Temp: 21 °C)
pka
9.97 · 9.97±0.10(Predicted)
Symbol(GHS)
7 · GHS07
Signal word
Warning

Safety & regulation

GHS classification

GHS Classification · 6 items

Warning

H302: Harmful if swallowed [Warning Acute toxicity, oral]

P264, P264+P265, P270, P280, P301+P317, P302+P352, P305+P351+P338, P321, P330, P332+P317, P337+P317, P362+P364, and P501 (click each P-code to see the statement)

This chemical does not meet GHS hazard criteria for < 0.1% (1 of 1887) of reports.

Warning

H302 (> 99.9%): Harmful if swallowed [Warning Acute toxicity, oral]

Hazard information

Regulatory Information · 6 items

Chemical: Phenol, 2-methoxy-

Chemical: Beebread

Commission Regulation (EC) No 1565/2000 (Repealed by Com. Implementing Reg. (EU) No 872/2012)

Phenol, 2-methoxy- is listed on the EPA's Chemical Data Reporting (CDR) system. Manufacturers and importers of Phenol, 2-methoxy- are required to report information about their production and use of this chemical to the EPA under the Toxic Substances Control Act (TSCA). (40 eCFR Part 711)

Status: Active Update: 08-09-2020 https://echa.europa.eu/registration-dossier/-/registered-dossier/9979

Guaiacol: Does not have an individual approval but may be used under an appropriate group standard

Fire HazardsThis chemical is combustible. (NTP, 1992)
Fire PotentialThis material is combustible when exposed to heat or flame.
Health Hazards · 1 item

SYMPTOMS: Symptoms of exposure to this compound may include irritation of the skin and eyes, muscular weakness, cardiovascular collapse and paralysis of the vasomotor centers. Ingestion produces burning in the mouth and throat, gastrointestinal distress, tremors and collapse.

Hazards Summary · 1 item

Emergency treatment: Phenol and related agents; [HSDB] May cause skin and eye irritation; Can be absorbed through skin; [CAMEO] Causes somnolence and acts as a general anesthetic; Causes elevation of transaminase enzymes; Mild eye irritant in rabbits; [RTECS] Safe when used as a flavoring agent in food; [JECFA] An irritant; [MSDSonline] See Phenol.

Reactive GroupEthers

Safety & protection

Fire FightingFires involving this material should be controlled using a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)
First Aid · 1 item

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. IMMEDIATELY transport the victim after flushing eyes to a hospital even if no symptoms (such as redness or irritation) develop.

Firefighting HazardsThis material is combustible when exposed to heat or flame. If in the solid form, it is advisable to ground mechanical equipment in contact with dry material to dissipate the potential buildup of static electricity.
Fire Fighting Procedures · 2 items

As with all fires, evacuate personnel to a safe area. Firefighters should use self-contained breathing equipment and protective clothing.

Water spray, dry chemical, carbon dioxide or foam as appropriate for surrounding fire and materials.

Storage ConditionsStore in tight, light-resistant container as defined in the USP-NF. This material should be handled and stored per label instructions to ensure product integrity.
Cleanup Methods · 1 item

Wear approved respiratory protection, chemically compatible gloves and protective clothing. Wipe up spillage or collect spillage using a high efficiency vacuum cleaner. Avoid breathing vapor or dust. Ventilate area and wash spill site. Place spillage in appropriately labelled container for disposal.

Toxicology

Interactions · 2 items

Methoxyphenol has been found to contribute to the carcinogenic effect of tobacco smoke in rats.

Absorption was delayed when ibuprofen and guaiacol administered simultaneously.

Ecotoxicity ValuesEC50; Species: Daphnia magna (Water flea, age 12 hr); Conditions: freshwater, static, 18 °C; Concentration: 25900 ug/L for 48 hr; Effect: intoxication, immobilization /formulation/
Environmental Fate · 3 items

TERRESTRIAL FATE: Based on a classification scheme(1), a Koc value of 40(2), indicates that o-methoxyphenol is expected to have very high mobility in soil(SRC). The pKa of o-methoxyphenol is 9.98(3), indicating that this compound will exist primarily in the undissociated form in the environment(SRC). Volatilization of o-methoxyphenol from moist soil surfaces is expected to be an environmental fate process(SRC) given a Henry's Law constant of 1.2X10-6 atm-cu m/mole(4). o-Methoxyphenol is not expected to volatilize from dry soil surfaces(SRC) based upon a vapor pressure of 0.103 mm Hg at 25 °C(5). Utilizing the Japanese MITI test, 97% of the theoretical BOD was reached in four weeks(6), suggesting that biodegradation may be an important environmental fate process in soil(SRC).

AQUATIC FATE: Based on a classification scheme(1), a Koc value of 40(2) indicates that o-methoxyphenol is not expected to adsorb to suspended solids and sediment(SRC). Volatilization from water surfaces is expected to be an environmental fate process(3) based upon a Henry's Law constant of 1.2X10-6 atm-cu m/mole(4). Using this Henry's Law constant and an estimation method(3), volatilization half-lives for a model river and model lake are 34 and 251 days, respectively(SRC). According to a classification scheme(5), an estimated BCF of 3(SRC), from its log Kow of 1.32(6) and a regression-derived equation(7), suggests the potential for bioconcentration in aquatic organisms is low(SRC). Utilizing the Japanese MITI test, 97% of the theoretical BOD was reached in four weeks(8), suggesting that biodegradation may be an important environmental fate process in water(SRC).

ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), o-methoxyphenol, which has a vapor pressure of 0.103 mm Hg at 25 °C(2), is expected to exist solely as a vapor in the ambient atmosphere. Vapor-phase o-methoxyphenol is degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals(SRC); the half-life for this reaction in air is estimated to be 13 hours(SRC), calculated from its estimated rate constant of 3.2X10-11 cu cm/molecule-sec at 25 °C(3). The sodium salt of o-methoxyphenol absorbs light at wavelengths of 289 nm(4) and therefore o-methoxyphenol may be susceptible to direct photolysis by sunlight(SRC).

Food Survey Values · 2 items

o-Methoxyphenol has been detected in volatile components of popcorn(1), cooked meat (sukiyaki) probably originating from soy sauce(2), fried bacon(3) and roasted filberts(4).

o-Methoxyphenol was detected in a red wine at concentrations of 23.1, 21.8, 17.0, 22.0; 27.3, 28.2; and 46.3 ug/L wine aged 12 months in barrels made of Quercus robur, Q. petrea, Q. pyrenaica, Q. faginea (Spanish oak wood); Q. robur, Q. petaea (French oak wood); and Q. alba (American oak wood), respectively. The concentration in the wine prior to aging as 15.5 ug/L. At 21 months, o-methoxyphenol concentrations were 23.2. 23.9, 20.2, 22.4; 27.6, 27.2; and 42.5 ug/L in barrels made of Q. robur, Q. petrea, Q. pyrenaica, Q. faginea (Spanish oak wood); Q. robur, Q. petaea (French oak wood); and Q. alba (American oak wood), respectively(1).

Adverse EffectsNeurotoxin - Acute solvent syndrome
Effluent Concentrations · 2 items

The concentration range of o-methoxyphenol in the effluent of a paper mill in Ontario, Canada in 1981 was 174-252 ug/L(1). It was detected in a paper mill effluent at Springfield, OR(2) and two other paper mill effluents in the U.S. in the concentration range 170-3,700 ug/L(6). The concentration of o-methoxyphenol in the combined effluent from a straw mill bleaching facility in Copenhagen, Denmark was 9,200 ug/L(3). The compound was also detected in the efflents from the following industries: timber products, leather tanning, pulp and paper, organic and plastic, and rum(4). The concentrations of o-methoxyphenol in a coal gasification condensate were 165-450 mg/L(5).

In surface water adjacent to "Valley of the Drums" site in Louisville, KY, the concentration range of o-methoxyphenol was 1-25 ug/L(2). o-Methoxyphenol was detected at a concentration 0.11 ug/L in the secondary effluent at Fort Polk, LA wastewater treatment facility(3) and in the effluent of a advanced wastewater treatment plant at Pomona, CA(1).

Safety data

Signal word
Warning
Symbol(GHS)
GHS07
Hazard statements
H302-H315-H319
Precautionary statements
P264-P270-P280-P301+P312-P302+P352-P305+P351+P338

Chemistry & industry

Pharmacology

Metabolism/Metabolites · 2 items

Several strains of Aspergillus niger hydroxylated anisole to give o-hydroxyanisole as main product.

o-Methoxyphenol yields 3-methoxycatechol probably in rabbit; yields o-methoxyphenyl sulfate probably in rabbit. o-Methoxyphenol yields catechol in rat; yields 1,2-dimethoxybenzene in mouse, rabbit, guinea pig, and rat. /From table/

Absorption, Distribution and Excretion · 5 items

In rats, guaiacol is rapidly absorbed, being present in the blood 5 minutes after oral administration, and reaching its peak plasma concentration in about 10 minutes. Its elimination from the blood is usually as rapid.

Excreted by rabbits in combined form with sulfate (15%) and glucuronic acid (72%).

Medical experience indicates that toxic quantities can be absorbed through the skin quite readily.

Methoxyphenol largely absorbed from digestive tract and stored in blood, kidneys, and respiratory organs. Excreted by rabbits in combined form with sulfate (15%) and glucuronic acid (72%).

In rats, guaiacol is rapidly absorbed, being present in the blood 5 minutes after oral administration, and reaching its peak plasma concentration in about 10 minutes. Its elimination from the blood is usually as rapid.

Metabolite PathwaysAlkaptonuria

Uses & manufacturing

Uses · 6 items

Naturally occurs in guaiac resin, animal wastes, and essential oils of plants; Used as an antioxidant (for fats, oils, and vitamins), anti-gumming agent in hydrocarbon solvents, anti-skinning agent in surface coatings; flavoring agent, polymerization inhibitor, stimulant expectorant, local anesthetic, and chemical intermediate (medicines, guaiacol compounds, and perfumes); [HSDB]

Painting (Pigments, Binders, and Biocides) [Category: Paint]

Antioxidant; anti-gumming agent in hydrocarbon solvents; anti-skinning agent in surface coatings; chemical intermediate.

Stimulant expectorant, chemical intermediate for other expectorants, eg, guaiacol carbonate; flavoring agent for non-alcoholic beverages and foods; chemical intermediate for papaverine and vanillin.

Methoxyphenol is used in the manufacture of medicines, guaiacol compounds, and perfumes.

Direct-acting or stimulant expectorant

U.S. Imports · 2 items

(1977) 1.32 X 10+8 g (Principal Customs Districts)

(1979) 3.20 X 10+8 g (Principal Customs Districts)

U.S. Production · 6 items

2023: 1,000,000 - <8,500,000 lb

(1977) Probably > 2.27 x 10+6 g

(1979) Probably > 2.27 x 10+6 g

Phenol, 2-methoxy- is listed as a High Production Volume (HPV) chemical (65FR81686). Chemicals listed as HPV were produced in or imported into the U.S. in >1 million pounds in 1990 and/or 1994. The HPV list is based on the 1990 Inventory Update Rule. (IUR) (40 CFR part 710 subpart B; 51FR21438).

Production volumes for non-confidential chemicals reported under the Inventory Update Rule. [Table#4881]

Production volume for non-confidential chemicals reported under the 2006 Inventory Update Rule. Chemical: Phenol, 2-methoxy-. Aggreated National Production Volume: 1 to < 10 million lbs.

Industry UsesIntermediate
Methods of Manufacturing · 4 items

Distillation of wood tar or coal tar; reaction of o-dichlorobenzene with alkali to form catechol, followed by methylation

Guaiacol is prepared by monomethylation of catechol using methyl halides or dimethyl sulfate. Monomethylation of catechol can also be accomplished with methanol in the presence of phosphoric acid, phosphates, or an ion exchanger.

... By mercuric oxide oxidation of lignin; ... by oxidation of anisole with trifluoroperoxyacetic acid; ... from acetovanillone and zinc chloride.

By extracting beechwood creosote with alcoholic potash, washing with ether, crystallizing potash compound from alcohol, and decomposing it with dilute sulfuric acid; also from ortho-anisidine by diazotization and subsequent action of dilute sulfuric acid.

Formulations/PreparationsOral solution: Codeine BP: 7.0 mg/5 mL and Guaiacol (1949) BPC /Boots Company plc/ 75.0 mg/5 mL, Pulmo Bailly (DDD Limited, United Kingdom)

Suppliers50 total

国药集团化学试剂有限公司86-21-63210123 · [email protected]
北京华美互利生物化工010-56205725 · [email protected]
梯希爱(上海)化成工业发展有限公司021-67121386 · [email protected]
上海阿拉丁生化科技股份有限公司400-6206333 13167063860 · [email protected]
山东泰诚生物科技有限公司18769832557 18769832557 · [email protected]

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