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2210-74-4 Usage

Chemical Properties

White Crystalline Solid

Flammability and Explosibility

Nonflammable

Check Digit Verification of cas no

The CAS Registry Mumber 2210-74-4 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 2,2,1 and 0 respectively; the second part has 2 digits, 7 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 2210-74:
(6*2)+(5*2)+(4*1)+(3*0)+(2*7)+(1*4)=44
44 % 10 = 4
So 2210-74-4 is a valid CAS Registry Number.
InChI:InChI=1/C10H12O3/c1-11-9-4-2-3-5-10(9)13-7-8-6-12-8/h2-5,8H,6-7H2,1H3

2210-74-4 Well-known Company Product Price

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  • Detail
  • Alfa Aesar

  • (H61777)  Glycidyl 2-methoxyphenyl ether, 98%   

  • 2210-74-4

  • 5g

  • 565.0CNY

  • Detail
  • Alfa Aesar

  • (H61777)  Glycidyl 2-methoxyphenyl ether, 98%   

  • 2210-74-4

  • 25g

  • 2545.0CNY

  • Detail
  • USP

  • (1598755)  Ranolazine Related Compound A  United States Pharmacopeia (USP) Reference Standard

  • 2210-74-4

  • 1598755-50MG

  • 14,500.98CNY

  • Detail

2210-74-4SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 11, 2017

Revision Date: Aug 11, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-[(2-methoxyphenoxy)methyl]oxirane

1.2 Other means of identification

Product number -
Other names 2-((2-Methoxyphenoxy)methyl)oxirane

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:2210-74-4 SDS

2210-74-4Synthetic route

sodium 2-methoxyphenolate
13052-77-2

sodium 2-methoxyphenolate

epichlorohydrin
106-89-8

epichlorohydrin

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
at 20℃; for 24h;95%
2-methoxy-phenol
90-05-1

2-methoxy-phenol

epichlorohydrin
106-89-8

epichlorohydrin

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
Stage #1: 2-methoxy-phenol With sodium hydroxide In water at 30℃; Large scale;
Stage #2: epichlorohydrin In water at 25 - 35℃; Large scale;
94%
With potassium carbonate at 120℃; for 4.5h;93%
With n-Bu4NOSO2OCH2CHOHCH3; potassium carbonate at 75 - 80℃; for 1h;90%
2-methoxy-phenol
90-05-1

2-methoxy-phenol

1,2-Epoxy-3-bromopropane
3132-64-7

1,2-Epoxy-3-bromopropane

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
With potassium carbonate In tetrahydrofuran Heating;82%
With potassium carbonate In N,N-dimethyl-formamide at 70℃; for 6h;62%
With base
With potassium carbonate In butanone at 80℃;
2-methoxy-phenol
90-05-1

2-methoxy-phenol

epichlorohydrin
106-89-8

epichlorohydrin

A

1-chloro-3-(2-methoxyphenoxy)-2-propyl alcohol
25772-81-0

1-chloro-3-(2-methoxyphenoxy)-2-propyl alcohol

B

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
With sodium hydroxide In water for 7h; Heating;A 23%
B 68%
With sodium hydroxide In 1,4-dioxane; water at 25 - 30℃;
With sodium hydroxide at 25 - 30℃;
peracetic acid
79-21-0

peracetic acid

O-allyl guaiacol
4125-43-3

O-allyl guaiacol

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
With diethyl ether
1,3-Dichloro-2-propanol
96-23-1

1,3-Dichloro-2-propanol

2-methoxy-phenol
90-05-1

2-methoxy-phenol

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
With sodium hydroxide
With sodium hydroxide
sodium guaiacolate
13052-77-2

sodium guaiacolate

epichlorohydrin
106-89-8

epichlorohydrin

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
tris-(3,6-dioxa-octyl)amine In acetonitrile
2-methoxy-phenol
90-05-1

2-methoxy-phenol

epichlorohydrin
106-89-8

epichlorohydrin

A

1,3-bis(2-methoxyphenoxy)propan-2-ol
16929-60-5

1,3-bis(2-methoxyphenoxy)propan-2-ol

B

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
Stage #1: 2-methoxy-phenol With sodium hydroxide; tetrabutylammomium bromide In water; toluene at 25 - 30℃; for 0.5h;
Stage #2: epichlorohydrin In water; toluene at 35 - 40℃; for 6h; Product distribution / selectivity;
With sodium hydroxide at 10 - 15℃; Temperature;
2-methoxy-phenol
90-05-1

2-methoxy-phenol

epichlorohydrin
106-89-8

epichlorohydrin

A

1-chloro-3-(2-methoxyphenoxy)-2-propyl alcohol
25772-81-0

1-chloro-3-(2-methoxyphenoxy)-2-propyl alcohol

B

1,3-bis(2-methoxyphenoxy)propan-2-ol
16929-60-5

1,3-bis(2-methoxyphenoxy)propan-2-ol

C

guaifenesin
93-14-1

guaifenesin

D

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Conditions
ConditionsYield
With sodium hydroxide In toluene at 25 - 30℃; Solvent; Concentration;
piperidine
110-89-4

piperidine

carbon disulfide
75-15-0

carbon disulfide

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

C16H23O3NS2

C16H23O3NS2

Conditions
ConditionsYield
at 20℃;99%
3-n-butyl-1-oxa-3,8-diazaspiro[4.5]decan-2-one
77211-54-2

3-n-butyl-1-oxa-3,8-diazaspiro[4.5]decan-2-one

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

3-Butyl-8-[2-hydroxy-3-(2-methoxy-phenoxy)-propyl]-1-oxa-3,8-diaza-spiro[4.5]decan-2-one
79053-48-8

3-Butyl-8-[2-hydroxy-3-(2-methoxy-phenoxy)-propyl]-1-oxa-3,8-diaza-spiro[4.5]decan-2-one

Conditions
ConditionsYield
With triethylamine97%
carbon dioxide
124-38-9

carbon dioxide

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

rac-4-(2-methoxyphenoxymethyl)-[1,3]dioxolan-2-one
2049-21-0

rac-4-(2-methoxyphenoxymethyl)-[1,3]dioxolan-2-one

Conditions
ConditionsYield
With imidazolium based ionic liquid incorporated porous dendritic fibrous nanosilica at 70℃; under 7500.75 Torr; for 2h; Green chemistry;96%
With C22H24F6N3O(1+)*Br(1-) In neat (no solvent) at 80℃; under 760.051 Torr; for 24h;90%
In N,N-dimethyl-formamide at 80℃; under 15001.5 Torr; for 20h;
piperidine
110-89-4

piperidine

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-(2-methoxy-phenoxy)-3-piperidino-propan-2-ol
108838-24-0

1-(2-methoxy-phenoxy)-3-piperidino-propan-2-ol

Conditions
ConditionsYield
In water at 0 - 20℃;95%
With Petroleum ether
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-bromo-3-(2-methoxyphenoxy)-2-propyl alcohol

1-bromo-3-(2-methoxyphenoxy)-2-propyl alcohol

Conditions
ConditionsYield
With bromine; 1,2-diamino-benzene In dichloromethane at 25℃; for 1.5h;94%
With lithium bromide; copper(ll) bromide In tetrahydrofuran at 20℃; regioselective reaction;70%
carbon disulfide
75-15-0

carbon disulfide

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

5-((2-methoxyphenoxy)methyl)-1,3-oxathiolane-2-thione

5-((2-methoxyphenoxy)methyl)-1,3-oxathiolane-2-thione

Conditions
ConditionsYield
With sodium hydrogencarbonate; 1-n-butyl-3-methylimidazolim bromide; lithium chloride In neat (no solvent) at 40℃; for 24h; chemoselective reaction;93%
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-chloro-3-(2-methoxyphenoxy)-2-propyl alcohol
25772-81-0

1-chloro-3-(2-methoxyphenoxy)-2-propyl alcohol

Conditions
ConditionsYield
With hydrogenchloride In 1,4-dioxane at 60℃; for 92.23h;92.2%
With hydrogenchloride In water; toluene at 25 - 35℃;89%
With hydrogenchloride In tetrahydrofuran; 1,4-dioxane at 5 - 10℃; for 2h;51%
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-iodo-3-(2-methoxy-phenoxy)-propan-2-ol

1-iodo-3-(2-methoxy-phenoxy)-propan-2-ol

Conditions
ConditionsYield
With iodine; 1,2-diamino-benzene In dichloromethane at 25℃; for 3h;92%
carbon disulfide
75-15-0

carbon disulfide

diethylamine
109-89-7

diethylamine

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

C15H23O3NS2

C15H23O3NS2

Conditions
ConditionsYield
at 20℃;92%
phenylacetylene
536-74-3

phenylacetylene

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-(2-methoxyphenoxy)-3-(4-phenyl-[1,2,3]triazol-1-yl)propan-2-ol

1-(2-methoxyphenoxy)-3-(4-phenyl-[1,2,3]triazol-1-yl)propan-2-ol

Conditions
ConditionsYield
With sodium azide at 80℃; for 12h; Green chemistry;92%
With copper(l) iodide; sodium azide In various solvent(s) at 20℃; for 16h;85%
3-n-propyl-1-oxa-3,8-diazaspiro[4.5]decan-2-one
77211-52-0

3-n-propyl-1-oxa-3,8-diazaspiro[4.5]decan-2-one

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

8-[2-Hydroxy-3-(2-methoxy-phenoxy)-propyl]-3-propyl-1-oxa-3,8-diaza-spiro[4.5]decan-2-one
79053-50-2

8-[2-Hydroxy-3-(2-methoxy-phenoxy)-propyl]-3-propyl-1-oxa-3,8-diaza-spiro[4.5]decan-2-one

Conditions
ConditionsYield
With triethylamine91%
tert-butylamine
75-64-9

tert-butylamine

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

M 66527
37708-25-1

M 66527

Conditions
ConditionsYield
In water at 0 - 20℃;90%
In dimethyl sulfoxide; isopropyl alcohol for 1h;
In water at 20℃; for 24h;
pyrrolidine
123-75-1

pyrrolidine

carbon disulfide
75-15-0

carbon disulfide

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

C15H21O3NS2

C15H21O3NS2

Conditions
ConditionsYield
at 20℃;90%
carbon disulfide
75-15-0

carbon disulfide

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

4-((2-methoxyphenoxy)methyl)-1,3-dithiolane-2-thione

4-((2-methoxyphenoxy)methyl)-1,3-dithiolane-2-thione

Conditions
ConditionsYield
With 1-n-butyl-3-methylimidazolim bromide; potassium hydroxide; lithium bromide In neat (no solvent) at 70℃; for 24h; chemoselective reaction;90%
carbon disulfide
75-15-0

carbon disulfide

N-butylamine
109-73-9

N-butylamine

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

C15H23O3NS2

C15H23O3NS2

Conditions
ConditionsYield
at 20℃;86%
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

Dimethyl chlorophosphate
813-77-4

Dimethyl chlorophosphate

3-Chloro-1-(2-methoxyphenoxy)propan-2-yl dimethyl phosphate

3-Chloro-1-(2-methoxyphenoxy)propan-2-yl dimethyl phosphate

Conditions
ConditionsYield
With titanium tetrachloride In dichloromethane at 20℃; for 0.5h; Ring cleavage; Addition;85%
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

N-(2,6-dimethylphenyl)-2-(piperazin-1-yl)acetamide
5294-61-1

N-(2,6-dimethylphenyl)-2-(piperazin-1-yl)acetamide

Ranolazine
95635-55-5

Ranolazine

Conditions
ConditionsYield
With Sulfated tungstate at 70℃; for 2h; Green chemistry;85%
In methanol at 60℃; for 5h; Solvent;85%
In methanol; toluene at 65℃; for 9h;69.8%
ibuprofen
15687-27-1

ibuprofen

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

2-hydroxy-3-(2-methoxyphenoxy)propyl 2-(4-isobutylphenyl) propanoate

2-hydroxy-3-(2-methoxyphenoxy)propyl 2-(4-isobutylphenyl) propanoate

Conditions
ConditionsYield
With butyl methyl imidazolium silica sulfate In acetonitrile for 18h; Reflux;85%
trimethylsilyl cyanide
7677-24-9

trimethylsilyl cyanide

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

3-hydroxy-4-(2-methoxy-phenoxy)-butyronitrile

3-hydroxy-4-(2-methoxy-phenoxy)-butyronitrile

Conditions
ConditionsYield
With potassium salts of magnetic graphitic carbon nitride at 70℃;84%
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

phenylpropyolic acid
637-44-5

phenylpropyolic acid

C18H18O3Se

C18H18O3Se

Conditions
ConditionsYield
With selenium; 1,10-Phenanthroline; tetra-(n-butyl)ammonium iodide; caesium carbonate; copper dichloride In water at 50℃; for 24h; Schlenk technique;84%
4-methoxy-aniline
104-94-9

4-methoxy-aniline

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-(2-methoxyphenoxy)-3-(4-methoxyphenylamino)propan-2-ol

1-(2-methoxyphenoxy)-3-(4-methoxyphenylamino)propan-2-ol

Conditions
ConditionsYield
for 0.166667h; microwave irradiation;82%
2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

guaifenesin
93-14-1

guaifenesin

Conditions
ConditionsYield
With perchloric acid81%
With perchloric acid In water at 80℃;80%
With sulfuric acid; water at 70℃; for 2h;59.1%
2-(3,4-dimethoxyphenyl)-2-isopropyl-5-methylamino-pentanenitrile
34245-14-2

2-(3,4-dimethoxyphenyl)-2-isopropyl-5-methylamino-pentanenitrile

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

2-(3,4-Dimethoxy-phenyl)-5-{[2-hydroxy-3-(2-methoxy-phenoxy)-propyl]-methyl-amino}-2-isopropyl-pentanenitrile
101532-49-4

2-(3,4-Dimethoxy-phenyl)-5-{[2-hydroxy-3-(2-methoxy-phenoxy)-propyl]-methyl-amino}-2-isopropyl-pentanenitrile

Conditions
ConditionsYield
In ethanol for 24h; Heating;80%
1-methylindole
603-76-9

1-methylindole

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-(2-methoxy-phenoxy)-3-(1-methyl-1H-indol-3-yl)-propan-2-ol

1-(2-methoxy-phenoxy)-3-(1-methyl-1H-indol-3-yl)-propan-2-ol

Conditions
ConditionsYield
With lithium perchlorate at 60℃; for 1h;80%
aniline
62-53-3

aniline

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

1-(2-methoxy-phenoxy)-3-phenylamino-propan-2-ol

1-(2-methoxy-phenoxy)-3-phenylamino-propan-2-ol

Conditions
ConditionsYield
With zinc diacetate; bis<2-(2-carboxy phenoxy)ethyl> ether for 0.05h; microwave irradiation;78%
for 0.166667h; microwave irradiation;61%
thiophenol
108-98-5

thiophenol

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

C16H18O3S

C16H18O3S

Conditions
ConditionsYield
With cholin hydroxide In neat liquid at 20℃; Green chemistry; regioselective reaction;78%
p-chlorphenylisocyanate
104-12-1

p-chlorphenylisocyanate

2-(2-methoxy-phenoxymethyl)-oxirane
2210-74-4

2-(2-methoxy-phenoxymethyl)-oxirane

C17H16ClNO4

C17H16ClNO4

Conditions
ConditionsYield
With C22H24F6N3O(1+)*Br(1-) In chlorobenzene at 100℃; for 12h; Inert atmosphere;78%

2210-74-4Relevant articles and documents

Solid state properties of 1,2-epoxy-3-(2-methoxyphenyloxy)-propane - Valuable intermediate in non-racemic drug synthesis

Bredikhin, Alexander A.,Strunskaya, Elena I.,Zakharychev, Dmitry V.,Krivolapov, Dmitry B.,Litvinov, Igor A.,Bredikhina, Zemfira A.

, p. 3361 - 3366 (2005)

Racemic 1,2-epoxy-3-(2-methoxyphenyloxy)-propane 1 undergoes spontaneous resolution upon crystallization. This fact is confirmed by coincidence of the IR spectra of racemic and scalemic crystalline samples of 1, by thermal analysis (single eutectic V-shape binary melting phase diagram), and X-ray analysis (space group P212121, Z = 4). Racemic 1 could be resolved into (S)-(+)- and (R)-(-)-1 by a preferential crystallization procedure.

Alternating and regioregular copolymers with high refractive index from COS and biomass-derived epoxides

Hu, Lan-Fang,Li, Yang,Liu, Bin,Zhang, Ying-Ying,Zhang, Xing-Hong

, p. 49490 - 49497 (2017)

This study describes the catalytic formation of alternating and regioregular copolymers from carbonyl sulfide (COS) and epoxides along with eugenol-based glycidyl ether (EGE) and guaiacol-based glycidyl ether (GGE), derived from eugenol and guaiacol, respectively. The (salen)CrCl [salen = N,N′-bis(salicylidene) cyclohexanediimine] complex, accompanied with various organic bases, was highly active towards the EGE/COS, GGE/COS copolymerization and EGE/GGE/COS terpolymerization. The turnover of frequency (TOF) of the (salen)CrCl complex for the EGE/COS copolymerization was up to 12000 h-1. The number-average molecular weight (Mn) of the resultant EGE/COS copolymer was up to 62.2 kg mol-1. In the presence of 0.5-1.5 mol% chlorohydrin, which was a by-product of the synthetic process of EGE, α-Cl, ω-OH EGE/COS copolymers were obtained. This result suggests that chlorohydrin could act as a very efficient chain transfer agent for the copolymerization. The EGE/COS, GGE/COS, and EGE/GGE/COS copolymers were soluble in most of the common solvents and exhibited a high refractive index of more than 1.58 with high Abbe numbers of up to 40.4. This study provides an unprecedented and sustainable synthetic route for making soluble sulfur-rich polymers with high optical properties.

Substituted diaryl compound and preparation method and application thereof

-

Paragraph 0073-0075; 0076, (2021/09/15)

The invention relates to the field of medicinal chemistry, in particular to a substituted diaryl compound (I). The preparation method comprises the following steps: medicine preparation and medical application thereof. Test results show that the substituted diaryl compound has a good inhibition effect on human lung cancer (A549), human ovarian cancer (SKOV3), human melanoma (A375) and human colon cancer (LOVO) cells. Formula (I):

Improving the activity and enantioselectivity of PvEH1, a Phaseolus vulgaris epoxide hydrolase, for o-methylphenyl glycidyl ether by multiple site-directed mutagenesis on the basis of rational design

Li, Chuang,Kan, Ting-Ting,Hu, Die,Wang, Ting-Ting,Su, Yong-Jun,Zhang, Chen,Cheng, Jian-Qing,Wu, Min-Chen

, (2019/08/01)

Substrate spectrum assay exhibited that PvEH1, which is an epoxide hydrolase from P. vulgaris, had the highest specific activity and enantiomeric ratio (E) for racemic o-methylphenyl glycidyl ether (rac-1) among tested aryl glycidyl ethers (1–5). To produce (R)-1 via kinetic resolution of rac-1 efficiently, the catalytic properties of PvEH1 were further improved on the basis of rational design. Firstly, the seven single-site variants of PvEH1-encoding gene (pveh1) were PCR-amplified as designed, and expressed in E. coli BL21(DE3). Among all expressed single-site mutants, PvEH1L105I and PvEH1V106I had the highest specific activities of 17.6 and 16.4 U/mg protein, respectively, while PvEH1L196D had an enhanced E value of 9.2. Secondly, to combine their respective merits, one triple-site variant, pveh1L105I/V106I/L196D, was also amplified, and expressed. The specific activity, E value, and catalytic efficiency of PvEH1L105I/V106I/L196D were 23.1 U/mg, 10.9, and 6.65 mM?1 s?1, respectively, which were 2.0-, 1.8- and 2.4-fold higher than those of wild-type PvEH1. The source of PvEH1L105I/V106I/L196D with enhanced E value for rac-1 was preliminarily analyzed by molecular docking simulation. Finally, the scale-up kinetic resolution of 100 mM rac-1 was conducted using 5 mg wet cells/mL E. coli/pveh1L105I/V106I/L196D at 25 °C for 1.5 h, producing (R)-1 with 95.0% ees, 32.1% yield and 3.52 g/L/h space-time yield.

Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities

Li, Feng,Xu, Qinlong,Zhu, Qihua,Chu, Zhaoxing,Lin, Gaofeng,Mo, Jiajia,Zhao, Yan,Li, Jiaming,He, Guangwei,Xu, Yungen

, (2019/11/03)

To improve the anti-inflammatory activity of desloratadine, we designed and synthesized a series of novel desloratadine derivatives. All compounds were evaluated for their anti-inflammatory and H1 antagonistic activities. Among them, compound 2c showed the strongest H1 antagonistic and anti-inflammatory activity. It also exhibited promising pharmacokinetic profiles and low toxicity. All these results suggest that compound 2c as a novel anti-allergic agent is worthy of further investigation.

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