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Cas Database

75970-64-8

75970-64-8

Identification

  • Product Name:1H-Benzimidazol-2-amine,1-[(4-fluorophenyl)methyl]-N-4-piperidinyl-, hydrobromide (1:2)

  • CAS Number: 75970-64-8

  • EINECS:

  • Molecular Weight:486.225

  • Molecular Formula: C19H21 F N4 . 2 Br H

  • HS Code:

  • Mol File:75970-64-8.mol

Synonyms:1H-Benzimidazol-2-amine,1-[(4-fluorophenyl)methyl]-N-4-piperidinyl-, dihydrobromide (9CI);Norastemizole hydrobromide; R 41232

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Safety information and MSDS view more

  • Signal Word:no data available

  • Hazard Statement:no data available

  • First-aid measures: General adviceConsult a physician. Show this safety data sheet to the doctor in attendance.If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician. In case of skin contact Wash off with soap and plenty of water. Consult a physician. In case of eye contact Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.

  • Fire-fighting measures: Suitable extinguishing media Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Wear self-contained breathing apparatus for firefighting if necessary.

  • Accidental release measures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapours, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. For personal protection see section 8. Prevent further leakage or spillage if safe to do so. Do not let product enter drains. Discharge into the environment must be avoided. Pick up and arrange disposal. Sweep up and shovel. Keep in suitable, closed containers for disposal.

  • Handling and storage: Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Avoid exposure - obtain special instructions before use.Provide appropriate exhaust ventilation at places where dust is formed. For precautions see section 2.2. Store in cool place. Keep container tightly closed in a dry and well-ventilated place.

  • Exposure controls/personal protection:Occupational Exposure limit valuesBiological limit values Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. Eye/face protection Safety glasses with side-shields conforming to EN166. Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin protection Wear impervious clothing. The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique(without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. Respiratory protection Wear dust mask when handling large quantities. Thermal hazards

Supplier and reference price

  • Manufacture/Brand
  • Product Description
  • Packaging
  • Price
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  • Manufacture/Brand:TRC
  • Product Description:NorastemizoleHydrobromide
  • Packaging:500 mg
  • Price:$ 1455
  • Delivery:In stock
  • Buy Now
  • Manufacture/Brand:TRC
  • Product Description:NorastemizoleHydrobromide
  • Packaging:50 mg
  • Price:$ 185
  • Delivery:In stock
  • Buy Now

Relevant articles and documentsAll total 5 Articles be found

Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds

Tian, Junjun,Vandermosten, Leen,Peigneur, Steve,Moreels, Lien,Rozenski, Jef,Tytgat, Jan,Herdewijn, Piet,Van den Steen, Philippe E.,De Jonghe, Steven

, p. 6332 - 6344 (2017/10/23)

Astemizole is a H1-antagonist endowed with antimalarial activity, but has hERG liabilities. Systematic structural modifications of astemizole led to the discovery of analogues that display very potent activity as inhibitors of the growth of the Plasmodium parasite, but show a decreased hERG inhibition, when compared to astemizole. These compounds can be used as starting point for the development of a new class of antimalarials.

Synthesis and anti-Plasmodium activity of benzimidazole analogues structurally related to astemizole

Roman, Gheorghe,Crandall, Ian E.,Szarek, Walter A.

, p. 1795 - 1804 (2014/01/06)

A series of compounds structurally related to astemizole were designed and synthesized with the goal of determining their anti-Plasmodium activity. Several modifications of the astemizole structure, namely the removal of the 4-fluorobenzyl and/ or 4-methoxyphenethyl moieties, substitution of the benzene ring of the benzimidazole scaffold, replacement of the fluorine atom in the 4-fluorobenzyl group, and variation of the 4-aminopiperidine moiety, were explored. In vitro evaluation of the anti-Plasmodium activity of these compounds using the ItG strain showed that astemizole and some of its structurally similar derivatives have IC50 values in the nanomolar range and exhibit toxicity towards the parasite over Chinese ovarian hamster (CHO) cells with a selectivity as high as 200. The presence of a secondary cyclic amine at position 2 and substitution with chlorine at positions 4 and 5 in the benzimidazole moiety are two modifications that resulted in potent and selective antimalarials based on astemizole.

A short synthesis of astemizole

De Parrodi, Cecilia Anaya,Quintero-Cortes, Leticia,Sandoval-Ramirez, Jesus

, p. 3323 - 3329 (2007/10/03)

The synthesis of astemizole 6, a potent H1-antihistaminic agent, was achieved in 20% overall yield. Compound 6 was obtained in high purity and on a multigram scale starting from 2-hydroxybenzimidazole.

Anti-histaminic compositions containing n-heterocyclyl-4-piperidinamines

-

, (2008/06/13)

Anti-allergic compositions containing one or more pharmaceutical carriers and as active ingredient at least one compound which is a N-heterocyclyl-4-piperidinamine and methods of treating allergic diseases in warm-blooded animals. Novel N-heterocyclyl-4-piperidinamines.

New Antihistaminic N-Heterocyclic 4-Piperidinamines. 2. Synthesis and Antihistaminic Activity of 1--N-(4-piperidinyl)-1H-benzimidazol-2-amines

Janssens, Frans,Torremans, Joseph,Janssen, Marcel,Stokbroekx, Raymond A.,Luyckx, Marcel,Janssen, Paul A. J.

, p. 1934 - 1943 (2007/10/02)

The synthesis of a series of 1--N-(4-piperidinyl)-1H-benzimidazol-2-amines and the preliminary evaluation of their in vivo antihistamine activity are described.The title compounds were obtained starting from either 1, 4, 10, or 55 by different synthetic methods.Substitution on the phenyl nucleus of the benzimidazole ring (84-87) was achieved by two different approaches.The in vivo antihistamine activity was evaluated by the compound 48/80 induced lethality test in rats and the antihistamine-induced lethality test in guinea pigs after oral and/o r subcutaneous administration.The duration of action was studied in the guinea pig for three compounds (4, 51, and 55).Compound 51, "astemizole", was also studied in histamine- and serotonin-induced cutaneous reaction and for mydriatic activity in the rat and tested for peripheral and central effects not related to histamine antagonism in a variety of systems.Astemizole has been selected for clinical investigation.

Process route upstream and downstream products

Process route

ethyl 4-[[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]amino]-1-piperidinecarboxylate
84501-68-8

ethyl 4-[[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]amino]-1-piperidinecarboxylate

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
With hydrogen bromide; for 1h; Heating;
95%
With hydrogen bromide; for 1h; Heating;
82%
With hydrogen bromide; for 2h; Reflux;
66%
With hydrogen bromide;
3.3 parts (82%)
With hydrogen bromide; In water; for 2h; Reflux;
(1H-benzimidazol-2-yl)-(1-ethoxycarbonyl-piperidin-4-yl)amine
73734-07-3

(1H-benzimidazol-2-yl)-(1-ethoxycarbonyl-piperidin-4-yl)amine

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 2 steps
1: 40 percent / sodium carbonate, potassium iodide / dimethylformamide / 70 °C
2: 82 percent / 48 percent hydrobromic acid / 1 h / Heating
With hydrogen bromide; sodium carbonate; potassium iodide; In N,N-dimethyl-formamide;
Multi-step reaction with 2 steps
1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 20 h / 70 - 80 °C
2: hydrogen bromide / 2 h / Reflux
With hydrogen bromide; potassium carbonate; potassium iodide; In N,N-dimethyl-formamide;
1-chloromethyl-4-fluorobenzene
352-11-4

1-chloromethyl-4-fluorobenzene

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 2 steps
1: 40 percent / sodium carbonate, potassium iodide / dimethylformamide / 70 °C
2: 82 percent / 48 percent hydrobromic acid / 1 h / Heating
With hydrogen bromide; sodium carbonate; potassium iodide; In N,N-dimethyl-formamide;
2-chloro-1-(4-fluorobenzyl)-1H-benzimidazole
84946-20-3

2-chloro-1-(4-fluorobenzyl)-1H-benzimidazole

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 2 steps
1: 56 percent / 5 h / 125 °C
2: 95 percent / aq. HBr / 1 h / Heating
With hydrogen bromide;
Multi-step reaction with 2 steps
1: 1-methyl-pyrrolidin-2-one / 1 h / 180 °C / Microwave irradiation
2: hydrogen bromide / water / 2 h / Reflux
With hydrogen bromide; In 1-methyl-pyrrolidin-2-one; water;
ethyl 4-aminopiperidine-1-carboxylate
58859-46-4

ethyl 4-aminopiperidine-1-carboxylate

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 5 steps
1.1: sodium hydroxide / water / 1 h / 5 °C
1.2: 2 h / 60 - 70 °C
2.1: ethanol / 20 °C
3.1: mercury(II) oxide / ethanol / 2 h / Reflux
4.1: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 20 h / 70 - 80 °C
5.1: hydrogen bromide / 2 h / Reflux
With hydrogen bromide; potassium carbonate; potassium iodide; mercury(II) oxide; sodium hydroxide; In ethanol; water; N,N-dimethyl-formamide;
ethyl 4-isothiocyanato-1-piperidinecarboxylate
73733-70-7

ethyl 4-isothiocyanato-1-piperidinecarboxylate

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 4 steps
1: ethanol / 20 °C
2: mercury(II) oxide / ethanol / 2 h / Reflux
3: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 20 h / 70 - 80 °C
4: hydrogen bromide / 2 h / Reflux
With hydrogen bromide; potassium carbonate; potassium iodide; mercury(II) oxide; In ethanol; N,N-dimethyl-formamide;
ethyl 4-{[(2-aminophenyl)aminothioxomethyl]amino}-1-piperidinecarboxylate
73733-81-0

ethyl 4-{[(2-aminophenyl)aminothioxomethyl]amino}-1-piperidinecarboxylate

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 3 steps
1: mercury(II) oxide / ethanol / 2 h / Reflux
2: potassium carbonate; potassium iodide / N,N-dimethyl-formamide / 20 h / 70 - 80 °C
3: hydrogen bromide / 2 h / Reflux
With hydrogen bromide; potassium carbonate; potassium iodide; mercury(II) oxide; In ethanol; N,N-dimethyl-formamide;
4-Fluorobenzyl bromide
459-46-1

4-Fluorobenzyl bromide

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 4 steps
1: potassium carbonate / methanol / 20 °C
2: sodium hydride / N,N-dimethyl-formamide / 2 h / 60 °C
3: 1-methyl-pyrrolidin-2-one / 1 h / 180 °C / Microwave irradiation
4: hydrogen bromide / water / 2 h / Reflux
With hydrogen bromide; sodium hydride; potassium carbonate; In 1-methyl-pyrrolidin-2-one; methanol; water; N,N-dimethyl-formamide;
1,2-diamino-benzene
95-54-5

1,2-diamino-benzene

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 4 steps
1: potassium carbonate / methanol / 20 °C
2: sodium hydride / N,N-dimethyl-formamide / 2 h / 60 °C
3: 1-methyl-pyrrolidin-2-one / 1 h / 180 °C / Microwave irradiation
4: hydrogen bromide / water / 2 h / Reflux
With hydrogen bromide; sodium hydride; potassium carbonate; In 1-methyl-pyrrolidin-2-one; methanol; water; N,N-dimethyl-formamide;
N-(4''-fluorobenzyl)-1,2-phenylenediamine
7191-70-0

N-(4''-fluorobenzyl)-1,2-phenylenediamine

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide
75970-64-8

1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine dihydrobromide

Conditions
Conditions Yield
Multi-step reaction with 3 steps
1: sodium hydride / N,N-dimethyl-formamide / 2 h / 60 °C
2: 1-methyl-pyrrolidin-2-one / 1 h / 180 °C / Microwave irradiation
3: hydrogen bromide / water / 2 h / Reflux
With hydrogen bromide; sodium hydride; In 1-methyl-pyrrolidin-2-one; water; N,N-dimethyl-formamide;

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  • BOC Sciences
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