Welcome to LookChem.com Sign In|Join Free

CAS

  • or
4-Bromophthalic anhydride is an organic compound with the chemical formula C8H4BrO3 and a molecular weight of 229.02 g/mol. It is a white crystalline solid that is derived from phthalic anhydride by the substitution of one hydrogen atom with a bromine atom at the 4-position. 4-Bromophthalic anhydride is an important intermediate in the synthesis of various pharmaceuticals, dyes, and other organic compounds. It is also used as a reagent in organic synthesis and as a building block for the preparation of other brominated aromatic compounds. 4-Bromophthalic anhydride is known for its reactivity and can undergo various chemical reactions, such as nucleophilic substitution, electrophilic substitution, and condensation reactions. It is typically synthesized through the bromination of phthalic anhydride using bromine or other brominating agents. Due to its reactivity and potential applications, 4-bromophthalic anhydride is a valuable chemical in the field of organic chemistry and pharmaceutical industry.

86-90-8

Post Buying Request

86-90-8 Suppliers

Recommended suppliersmore

  • Product
  • FOB Price
  • Min.Order
  • Supply Ability
  • Supplier
  • Contact Supplier
  • 4-Bromophthalic anhydride CAS 86-90-8 4-Bromophthalicanhydride CAS no 86-90-8 5-Bromo-1,3-isobenzofurandione 4-Bromo Phthalic anhydride

    Cas No: 86-90-8

  • USD $ 3.5-5.0 / Kiloliter

  • 5 Kiloliter

  • 3000 Metric Ton/Month

  • Chemwill Asia Co., Ltd.
  • Contact Supplier

86-90-8 Usage

Check Digit Verification of cas no

The CAS Registry Mumber 86-90-8 includes 5 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 2 digits, 8 and 6 respectively; the second part has 2 digits, 9 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 86-90:
(4*8)+(3*6)+(2*9)+(1*0)=68
68 % 10 = 8
So 86-90-8 is a valid CAS Registry Number.
InChI:InChI=1/C8H3BrO3/c9-4-1-2-5-6(3-4)8(11)12-7(5)10/h1-3H

86-90-8SDS

SAFETY DATA SHEETS

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

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name 4-Bromophthalic anhydride

1.2 Other means of identification

Product number -
Other names 4-bromophthalic acid anhydride

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:86-90-8 SDS

86-90-8Synthetic route

4-bromophthalic acid
6968-28-1

4-bromophthalic acid

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
With acetic anhydride for 2h; Heating;97%
With acetic anhydride at 140℃; for 2h;84%
With acetic anhydride at 140℃; for 2h;84%
5-Bromoisoindoline-1,3-dione
6941-75-9

5-Bromoisoindoline-1,3-dione

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
With urea at 140℃; for 0.333333h;87%
phthalic anhydride
85-44-9

phthalic anhydride

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
With N-benzyl-N,N,N-triethylammonium chloride; bromine; sodium hydroxide In water at 45 - 80℃; for 11.7h; Catalytic behavior; Reagent/catalyst; Temperature;85.4%
Stage #1: phthalic anhydride With bromine; sodium hydroxide In water at 90℃; for 6h;
Stage #2: With thionyl chloride In water at 0℃; Reflux;
79%
Stage #1: phthalic anhydride With bromine; sodium hydroxide In water at 90℃; for 12h; Inert atmosphere;
Stage #2: With thionyl chloride for 5h; Reflux; Inert atmosphere;
71%
5-brom-7-oxa-bicyclo<2.2.1>hept-5-en-2-exo,3-cis-dicarbonsaeureanhydrid
118728-51-1, 145551-79-7

5-brom-7-oxa-bicyclo<2.2.1>hept-5-en-2-exo,3-cis-dicarbonsaeureanhydrid

hydrogen bromide
10035-10-6, 12258-64-9

hydrogen bromide

acetic acid
64-19-7

acetic acid

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-bromo-o-xylene
583-71-1

4-bromo-o-xylene

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: aq. KMnO4; Na2CO3; aliquat 336 / 0.75 h / Heating
2: Ac2O / 4 h / Heating
View Scheme
Multi-step reaction with 2 steps
1: 67 percent / potassium hydroxide, potassium permanganate / H2O / 7 h
2: Ac2O / 4 h / Heating
View Scheme
Stage #1: 4-bromo-o-xylene With pyridine; potassium permanganate In water for 24h; Reflux;
Stage #2: With acetic anhydride for 22h; Reflux;
4-bromo-2-methylbenzoic acid
68837-59-2

4-bromo-2-methylbenzoic acid

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: alkaline potassium permanganate
2: durch Destillation
View Scheme
4-bromo-2-methylbenzonitrile
67832-11-5

4-bromo-2-methylbenzonitrile

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: alcoholic NaOH-solution
2: alkaline potassium permanganate
3: durch Destillation
View Scheme
4-Bromo-2-methylaniline
583-75-5

4-Bromo-2-methylaniline

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: durch Austausch von NH2 gegen CN
2: alcoholic NaOH-solution
3: alkaline potassium permanganate
4: durch Destillation
View Scheme
4-chlorophthalic anhydride
118-45-6

4-chlorophthalic anhydride

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

Conditions
ConditionsYield
With bromine In chlorobenzene
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

6-bromo-2,3-dihydrophthalazine-1,4-dione
76240-49-8

6-bromo-2,3-dihydrophthalazine-1,4-dione

Conditions
ConditionsYield
Stage #1: 4-bromophthalic anhydride With acetic acid at 125℃; for 1h;
Stage #2: With hydrazine hydrate at 125℃; for 0.5h;
100%
Stage #1: 4-bromophthalic anhydride With acetic acid at 125℃; for 1h;
Stage #2: With hydrazine hydrate at 125℃; for 0.583333h;
100%
Stage #1: 4-bromophthalic anhydride With hydrazine hydrate Inert atmosphere;
Stage #2: With hydrogenchloride In water for 24h; Reflux; Inert atmosphere;
96%
3-methoxy-4-(2-(pyrrolidin-1-yl)ethoxy)aniline
394248-90-9

3-methoxy-4-(2-(pyrrolidin-1-yl)ethoxy)aniline

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

5-bromo-2-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-isoindole-1,3-dione
515877-85-7

5-bromo-2-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-isoindole-1,3-dione

Conditions
ConditionsYield
With EDC resin In dichloromethane for 12h;100%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-bromo-2-(hydroxymethyl)benzyl alcohol
171011-37-3

4-bromo-2-(hydroxymethyl)benzyl alcohol

Conditions
ConditionsYield
With lithium aluminium tetrahydride; zinc(II) chloride In tetrahydrofuran at 0 - 20℃; Inert atmosphere;100%
With borane-THF In tetrahydrofuran at 0 - 20℃; for 17.5h;94%
Stage #1: 4-bromophthalic anhydride With diisobutylaluminium hydride In toluene at 20℃; under 760.051 Torr; for 1.5h; Cooling with ice;
Stage #2: With hydrogenchloride In water; toluene at 0 - 20℃; for 1h;
91%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

5-aminoisophthalic acid
99-31-0

5-aminoisophthalic acid

C16H8BrNO6

C16H8BrNO6

Conditions
ConditionsYield
Stage #1: 4-bromophthalic anhydride; 5-aminoisophthalic acid In N,N-dimethyl acetamide at 60 - 100℃; for 1h;
Stage #2: With pyridine; acetic anhydride In N,N-dimethyl acetamide for 2h;
100%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

5-Bromoisoindoline-1,3-dione
6941-75-9

5-Bromoisoindoline-1,3-dione

Conditions
ConditionsYield
With formamide at 200℃; for 2h;99%
With choline chloride; urea at 140℃; for 1h; Green chemistry;99%
With formamide for 4h; Reflux;94%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

hexan-1-amine
111-26-2

hexan-1-amine

5-bromo-2-hexylisoindoline-1,3-dione
299963-46-5

5-bromo-2-hexylisoindoline-1,3-dione

Conditions
ConditionsYield
In toluene for 18h; Reflux;99%
With propionic acid at 130℃; for 72h;96%
With acetic acid for 4h;
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

sulfanilamide
63-74-1

sulfanilamide

C14H9BrN2O4S

C14H9BrN2O4S

Conditions
ConditionsYield
With acetic acid for 19h; Reflux;97%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-amino-n-butyric acid
56-12-2

4-amino-n-butyric acid

4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butanoic acid
299964-12-8

4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butanoic acid

Conditions
ConditionsYield
With acetic acid at 100℃; for 3h;96.7%
With triethylamine In toluene for 24h; Reflux;68%
With triethylamine In toluene for 24h; Reflux;
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

methylamine
74-89-5

methylamine

5-bromo-2-methyl-2,3-dihydro-1H-isoindole-1,3-dione
90224-73-0

5-bromo-2-methyl-2,3-dihydro-1H-isoindole-1,3-dione

Conditions
ConditionsYield
With sodium acetate; acetic acid In water for 6h; Inert atmosphere; Reflux;96%
In water; toluene at 130℃; for 12h; Dean-Stark; Inert atmosphere;90%
In water; toluene for 9h; Reflux;88%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-hydroxyphthalic acid
610-35-5

4-hydroxyphthalic acid

Conditions
ConditionsYield
Stage #1: 4-bromophthalic anhydride With copper(l) chloride; potassium hydroxide In water; dimethyl sulfoxide at 25℃; for 0.166667h; Inert atmosphere;
Stage #2: In water; dimethyl sulfoxide at 130℃; for 24h; Inert atmosphere;
Stage #3: With hydrogenchloride In water; dimethyl sulfoxide pH=1 - 2; Reagent/catalyst; Temperature;
95.3%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

benzylamine
100-46-9

benzylamine

2-benzyl-5-bromoisoindoline-1,3-dione
82104-06-1

2-benzyl-5-bromoisoindoline-1,3-dione

Conditions
ConditionsYield
95%
With acetic acid at 130℃; for 4h; Inert atmosphere;89%
With acetic acid at 130℃; for 4h; Inert atmosphere;89%
56%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

2-amino-5-styryl-1,3,4-thiadiazole
28004-54-8

2-amino-5-styryl-1,3,4-thiadiazole

C18H10BrN3O2S

C18H10BrN3O2S

Conditions
ConditionsYield
With acetic acid at 120℃; Molecular sieve;95%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

N,N-diethylaniline
93-05-0

N,N-diethylaniline

5-bromo-2-(4-(diethylamino)phenyl)isoindoline-1,3-dione

5-bromo-2-(4-(diethylamino)phenyl)isoindoline-1,3-dione

Conditions
ConditionsYield
In acetic acid at 118℃;95%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

rac-α-aminoglutarimide hydrochloride
24666-56-6

rac-α-aminoglutarimide hydrochloride

5-bromo-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione
26166-92-7

5-bromo-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione

Conditions
ConditionsYield
With sodium acetate; acetic acid Heating / reflux;93%
With sodium acetate In acetic acid at 20 - 80℃; for 16h;92%
With sodium acetate; acetic acid at 115℃; for 16h;91.6%
With potassium acetate; acetic acid at 90℃; for 12h;60%
With sodium acetate; acetic acid at 120℃; for 5h;
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

aniline
62-53-3

aniline

5-bromo-2-phenylisoindoline-1,3-dione
82104-66-3

5-bromo-2-phenylisoindoline-1,3-dione

Conditions
ConditionsYield
With acetic acid at 120℃; Molecular sieve;92%
With acetic acid at 120℃; for 1h; Molecular sieve; Microwave irradiation;86%
75%
With acetic acid Reflux;73%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

bis(pinacol)diborane
73183-34-3

bis(pinacol)diborane

C14H15BO5
849677-21-0

C14H15BO5

Conditions
ConditionsYield
With potassium acetate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2 In dimethyl sulfoxide at 80℃; for 10h;92%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

acetylene
74-86-2

acetylene

5,5'-(ethyne-1,2-diyl)bis(isobenzofuran-1,3-dione)
129808-00-0

5,5'-(ethyne-1,2-diyl)bis(isobenzofuran-1,3-dione)

Conditions
ConditionsYield
With copper(l) iodide; bis(triphenylylphosphine)palladium(II) dichloride; triethylamine; triphenylphosphine In toluene at 80℃; Temperature; Pressure; Solvent; Time; Neutral conditions;92%
With bis-triphenylphosphine-palladium(II) chloride; copper(l) iodide; triethylamine; triphenylphosphine In toluene at 80℃; Concentration; Inert atmosphere; Large scale;80%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-bromo-aniline
106-40-1

4-bromo-aniline

5-bromo-2-(4-bromophenyl)isoindoline-1,3-dione

5-bromo-2-(4-bromophenyl)isoindoline-1,3-dione

Conditions
ConditionsYield
In N,N-dimethyl-formamide at 100℃; for 30h;92%
With acetic acid Reflux;82%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-methoxy-aniline
104-94-9

4-methoxy-aniline

5-bromo-2-(4-methoxyphenyl)isoindoline-1,3-dione
82104-71-0

5-bromo-2-(4-methoxyphenyl)isoindoline-1,3-dione

Conditions
ConditionsYield
With acetic acid at 120℃; Molecular sieve;91%
With acetic acid at 120℃; for 1h; Molecular sieve; Microwave irradiation;80%
67%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

isopropylamine
75-31-0

isopropylamine

5-bromo-2-isopropylisoindoline-1,3-dione
351996-68-4

5-bromo-2-isopropylisoindoline-1,3-dione

Conditions
ConditionsYield
With isoquinoline In 3-methyl-phenol at 20 - 200℃; for 10h; Inert atmosphere;91%
With acetic acid for 1.5h; Inert atmosphere; Reflux;80%
methanol
67-56-1

methanol

4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-bromophthalic Acid Dimethyl Ester
87639-57-4

4-bromophthalic Acid Dimethyl Ester

Conditions
ConditionsYield
With sulfuric acid at 80℃; for 16h;90%
With sulfuric acid
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

3-aminopentane
616-24-0

3-aminopentane

4-bromo-2-(1-ethylpropyl)phthalimide

4-bromo-2-(1-ethylpropyl)phthalimide

Conditions
ConditionsYield
In acetic acid at 120 - 180℃; for 0.333333h; Microwave irradiation; Sealed tube;90%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

sodium methylate
124-41-4

sodium methylate

4-methoxyphthalic acid
1885-13-8

4-methoxyphthalic acid

Conditions
ConditionsYield
With Methyl formate; copper(l) chloride In methanol at 150℃; for 16h; Inert atmosphere;90%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

diphenyl acetylene
501-65-5

diphenyl acetylene

3-bromo-5,6,7,8-tetraphenyl-1-naphthoic acid

3-bromo-5,6,7,8-tetraphenyl-1-naphthoic acid

Conditions
ConditionsYield
With [ruthenium(II)(η6-1-methyl-4-isopropyl-benzene)(chloride)(μ-chloride)]2; tetrabutylammomium bromide In N,N-dimethyl-formamide at 100℃; for 12h; Sealed tube;90%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

(+/-)-α-aminoglutarimide
2353-44-8

(+/-)-α-aminoglutarimide

5-bromo-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione
26166-92-7

5-bromo-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione

Conditions
ConditionsYield
With sodium acetate; acetic acid at 120℃; for 5h;90%
With sodium acetate; acetic acid at 120℃; for 5h;90%
With sodium acetate; acetic acid Reflux; Inert atmosphere;82%
With sodium acetate; acetic acid at 75℃; for 12h; Inert atmosphere;82%
With triethylamine In acetonitrile at 80℃; for 12h;81%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

4-trifluoromethylphenylamine
455-14-1

4-trifluoromethylphenylamine

5-bromo-2-(4-(trifluoromethyl)phenyl)isoindoline-1,3-dione

5-bromo-2-(4-(trifluoromethyl)phenyl)isoindoline-1,3-dione

Conditions
ConditionsYield
With acetic acid Reflux;88%
In N,N-dimethyl-formamide at 150℃; for 24h; Inert atmosphere;80%
In N,N-dimethyl-formamide for 24h; Inert atmosphere; Reflux;70%
In N,N-dimethyl-formamide for 24h; Inert atmosphere; Reflux;68%
4-bromophthalic anhydride
86-90-8

4-bromophthalic anhydride

n-butylguanidine hydrochloride
19341-56-1

n-butylguanidine hydrochloride

2,2'-((butylimino)methylene)bis(5-bromoisoindoline-1,3-dione)

2,2'-((butylimino)methylene)bis(5-bromoisoindoline-1,3-dione)

Conditions
ConditionsYield
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 50℃; for 5h; Reagent/catalyst; Inert atmosphere;86%

86-90-8Relevant articles and documents

An Isosteric and Fluorescent DNA Base Pair Consisting of 4-aminophthalimide and 2,4-diaminopyrimidine as C-Nucleosides

Merkel, Marcus,Dehmel, Lars,Ernsting, Nikolaus P.,Wagenknecht, Hans-Achim

, p. 384 - 388 (2017)

A 13mer DNA duplex containing the artificial 4-aminophthalimide:2,4-diaminopyrimidine (4AP:DAP) base pair in the central position was characterized by optical and NMR spectroscopy. The fluorescence of 4AP in the duplex has a large Stokes shift of Δλ=124 nm and a quantum yield of ΦF=24 %. The NMR structure shows that two interstrand hydrogen bonds are formed and confirms the artificial base pairing. In contrast, the 4-N,N-dimethylaminophthalimide moiety prefers the syn conformation in DNA. The fluorescence intensity of this chromophore in DNA is very low and the NMR structure shows no significant interaction with DAP. Primer-extension experiments with DNA polymerases showed that not only is the 4AP C nucleotide incorporated at the desired position opposite DAP in the template, but also that the polymerase is able to progress past this position to give the full-length product. The observed selectivity supports the NMR results.

COMPOUNDS AND USES THEREOF

-

Page/Page column 316, (2021/08/06)

The present disclosure features compounds and methods useful for the treatment of BAF complex-related disorders.

In pursuit of a selective hepatocellular carcinoma therapeutic agent: Novel thalidomide derivatives with antiproliferative, antimigratory and STAT3 inhibitory properties

Nutt, Michael J.,Yee, Yeung Sing,Buyan, Amanda,Andrewartha, Neil,Corry, Ben,Yeoh, George C.T.,Stewart, Scott G.

, (2021/03/30)

Advanced stage liver cancer is predominantly treated with the multi-kinase inhibitor sorafenib; however, this therapeutic agent lacks selectivity in its cytotoxic actions and is associated with poor survival outcomes. Herein we report the design and preparation of several thalidomide derivatives, including a variety of novel thioether-containing forms that are especially rare in the literature. Importantly, two of the derivatives described are potent antiproliferative agents with dose-dependent selectivity for tumorigenic liver progenitor cells (LPC) growth inhibition (up to 36% increase in doubling time at 10 μM) over non-tumorigenic cells (no effect at 10 μM). Furthermore, these putative anti-liver cancer agents were also found to be potent inhibitors of tumorigenic LPC migration. This report also describes these derivatives’ effects on several key signalling pathways in our novel liver cell lines by immunofluorescence and AlphaLISA assays. Aryl thioether derivative 7f significantly reduced STAT3 phosphorylation (23%) and its nuclear localisation (16%) at 10 μM in tumorigenic LPCs, implicating the IL-6/JAK/STAT3 axis is central in the mode of action of our derivatives.

Synthesis method of 4-halogenated phthalic anhydride and derivative thereof

-

Paragraph 0024-0027; 0029-0032; 0034-0037; 0039-0042; 0044-0, (2020/12/30)

The invention relates to a synthetic method of 4-halogenated phthalic anhydride and a derivative of the 4-halogenated phthalic anhydride, and solves the technical problems of low product purity, poorproduct performance, complex synthetic process and low utilization ratio of monohalide isomers and polyhalides in the existing production process. The method specifically comprises the following steps: dissolving phthalic anhydride in an organic solvent, and introducing a halogenating reagent under the action of iron powder and a Lewis acid catalyst to prepare a halogenated phthalic anhydride mixture; rectifying and purifying the polyhalogenated phthalic anhydride mixture to obtain a 4-halogenated phthalic anhydride pure product; and continuing subjecting residual halogenated phthalic anhydride mixture to halogenation reaction under the action of fuming sulfuric acid and the catalyst to prepare tetrahalogenated phthalic anhydride, and to realize comprehensive utilization of the raw materials. The method is widely applied to the technical field of flame retardant synthesis.

Dihydroxyphenyl Sulfonylisoindoline Derivatives

-

Paragraph 058; 060; 0116, (2018/06/12)

Provided are compounds that are inhibitors of pyruvate dehydrogenase kinase (PDK), and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.

Industrial preparation method of 5-bromophthalide

-

Paragraph 0017; 0018, (2017/09/01)

The invention relates to a preparation method of 5-bromophthalide and mainly solves such production technical problems of an existing preparation method as expensive raw material, dangerous and complex operation, relatively low yield, high quantity of generated three wastes and etc. The technical scheme of the invention is as follows: an industrial preparation method of 5-bromophthalide is characterized in that 5-bromophthalide is obtained through three step reactions of bromination, ammoniation and reduction by taking a conventional and easily available ammoniation as a raw material. The chemical reaction formula is as shown in the description. The method provided by the invention is mainly used for industrial preparation of 5-bromophthalide.

PROCESS FOR THE PREPARATION OF ORGANIC BROMIDES

-

Paragraph 00139; 00141; 00162, (2017/07/28)

The present invention provides a process for the preparation of organic bromides, by a radical bromodecarboxylation of carboxylic acids with a bromoisocyanurate.

Development of Dihydroxyphenyl Sulfonylisoindoline Derivatives as Liver-Targeting Pyruvate Dehydrogenase Kinase Inhibitors

Tso, Shih-Chia,Lou, Mingliang,Wu, Cheng-Yang,Gui, Wen-Jun,Chuang, Jacinta L.,Morlock, Lorraine K.,Williams, Noelle S.,Wynn, R. Max,Qi, Xiangbing,Chuang, David T.

supporting information, p. 1142 - 1150 (2017/02/19)

Pyruvate dehydrogenase kinases 1-4 (PDK1-4) negatively control activity of the pyruvate dehydrogenase complex (PDC) and are up-regulated in obesity, diabetes, heart failure, and cancer. We reported earlier two novel pan-PDK inhibitors PS8 [4-((5-hydroxyisoindolin-2-yl)sulfonyl)benzene-1,3-diol] (1) and PS10 [2-((2,4-dihydroxyphenyl)sulfonyl)isoindoline-4,6-diol] (2) that targeted the ATP-binding pocket in PDKs. Here, we developed a new generation of PDK inhibitors by extending the dihydroxyphenyl sulfonylisoindoline scaffold in 1 and 2 to the entrance region of the ATP-binding pocket in PDK2. The lead inhibitor (S)-3-amino-4-(4-((2-((2,4-dihydroxyphenyl)sulfonyl)isoindolin-5-yl)amino)piperidin-1-yl)-4-oxobutanamide (17) shows a ~8-fold lower IC50 (58 nM) than 2 (456 nM). In the crystal structure, the asparagine moiety in 17 provides additional interactions with Glu-262 from PDK2. Treatment of diet-induced obese mice with 17 resulted in significant liver-specific augmentation of PDC activity, accompanied by improved glucose tolerance and drastically reduced hepatic steatosis. These findings support 17 as a potential glucose-lowering therapeutic targeting liver for obesity and type 2 diabetes.

Preparation method of 4-bromo phthalic anhydride

-

Paragraph 0025, (2016/12/01)

The invention belongs to the field of chemical engineering, and relates to a preparation method of 4-bromo phthalic anhydride. The preparation method includes the following steps that sodium hydroxide is dissolved in water, phthalic anhydride and a phase transfer catalyst are added and evenly mixed, a reaction is performed in the mode that programmed temperature control is performed in three stages and reactants are added in three times, 20% fuming sulphuric acid is added for acidification, a sodium bisulfite aqueous solution is added after cooling for removing excessive bromine, an organic solvent is added for extraction, the organic solvent is removed through distillation, then temperature is increased to obtain a crude 4-bromo phthalic anhydride product, rectification dehydration is performed under the vacuum condition, fraction is collected, and the finished 4-bromo phthalic anhydride product is obtained. Compared with a multi-step reaction in the prior art, the process steps are simplified, the product yield is high, the production energy consumption is reduced, the three-waste emission is greatly reduced, the energy consumption and wastewater treatment cost for extraction of 4-bromophthalic acid crystals are reduced, production cost is reduced, and environmental protection pressure is relieved.

Synthesis and biological evaluation of novel aromatic imide-polyamine conjugates

Li, Ming,Wang, Yuxia,Zhang, Jianying,Xie, Songqiang,Wang, Chaojie,Wu, Yingliang

, (2016/12/16)

Three types of conjugates in which aromatic imide scaffolds were coupled to diverse amine/polyamine motifs were synthesized, and their antitumor activities were evaluated in vitro and in vivo. Results showed that the conjugate 11e of 1,8-naphthilimide with spermine had pronounced effects on inhibiting tumor cell proliferation and inducing tumor cell apoptosis via ROS-mediated mitochondrial pathway. The in vivo assays on three H22 tumor transplant models revealed that compound 11e exerted potent ability in preventing lung cancer metastasis and extending lifespan. Furthermore, the efficacy of 11e in inhibiting tumor growth and improving body weight index were better than that of positive control, amonafide. Our study demonstrates that compound 11e is a valuable lead compound for further investigation.

Post a RFQ

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

1

What can I do for you?
Get Best Price

Get Best Price for 86-90-8