953071-73-3

Basic information

• Product Name: tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate
• Synonyms: tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate;Bilastine Impurity 1;tert-Butyl 4-(1H-benzimidazol-2-yl)piperidine-1-carboxylate;2-Methyl-2-propanyl 4-(1H-benzimidazol-2-yl)-1-piperidinecarboxylate
• CAS NO: 953071-73-3
• Molecular Formula: C₁₇H₂₃N₃O₂
• Molecular Weight: 301.38342
• Product Categories: API;Piperidine, heterocyclic
• Mol File: 953071-73-3.mol

Chemical Properties

• Boiling Point: 497.1±38.0 °C(Predicted)
• Appearance: /
• Density: 1.184±0.06 g/cm3(Predicted)
• PKA: 11.83±0.10(Predicted)
• CAS DataBase Reference: tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate(953071-73-3)
• EPA Substance Registry System: tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate(953071-73-3)

Safety Data

• Hazardous Substances Data: 953071-73-3(Hazardous Substances Data)

Usage

Uses

Used in Medicinal Chemistry:
Tert-butyl 4-(1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate is utilized as a key building block for the synthesis of potential therapeutic agents. Its incorporation into various chemical frameworks allows for the exploration of new drug candidates with improved pharmacological profiles.
Used in Research and Development:
In the realm of pharmaceutical research, tert-butyl 4-(1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate serves as an invaluable research tool. It is employed to investigate the biological activity and pharmacological properties of its derivatives, providing insights into their potential applications in treating specific medical conditions.
Used in Drug Development:
tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate is also used in the development of new drugs targeting a range of medical conditions. Its unique structure and functional groups enable the design of molecules with enhanced efficacy, selectivity, and safety profiles, contributing to the advancement of novel therapeutic options for patients.

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 38385-95-4 2-(4-piperidinyl)-1H-benzimidazole 
• 95-54-5 1,2-diamino-benzene 
• 88-74-4 2-nitro-aniline 
• 137076-22-3 tert butyl 4-formylpiperidine-1-carboxylate 
• 498-94-2 isonipecotic acid 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 

Downstream Products

• 1181267-36-6 tert-butyl 4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate 
• 38385-95-4 2-(4-piperidinyl)-1H-benzimidazole 
• 1381841-42-4 C₁₉H₂₀ClN₃ 

Relevant articles and documents

TITLE: PROCESS FOR THE PREPARATION OF BILASTINE

The present invention relates to a process for the preparation of bilastine, a compound of formula I. The present invention relates to p-xylene solvate of bilastine and process for its preparation. The present invention relates to a process for the prepar

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Photochemical Homologation for the Preparation of Aliphatic Aldehydes in Flow

Cheap and readily available aqueous formaldehyde was used as a formylating reagent in a homologation reaction with nonstabilized diazo compounds, enabled by UV photolysis of bench-stable oxadiazolines in a flow photoreactor. Various aliphatic aldehydes were synthesized along with the corresponding derivatized alcohols and benzimidazoles. No transition-metal catalyst or additive was required to affect the reaction, which proceeded at room temperature in 80 min.

SMALL MOLECULE ANTAGONISTS OF SUMO RELATED MODIFICATION OF CRMP2 AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a piperidinyl-benzoimidazole structure which function as antagonists of small ubiquitin like modifier (SUMO) related modification (SUMOylation) of collapsin response mediator protein 2 (CRMP2), and their use as therapeutics for the treatment of voltage gated sodium channel 1.7 (Nav1.7) related itch, anosmia, migraine event, and/or pain (e.g., neuropathic pain).

Bilastine preparation method

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Discovery of Novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole Derivatives as Potential Anti-Inflammatory Agents

A novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 5 with good anti-inflammatory activity was identified from our in-house library. Based on hit compound 5, two series of 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivative 6a-g and 7a-h were designed and synthesized as novel anti-inflammatory agents. Most of synthesized compounds exhibited good inhibitory activity on NO and TNF-α production in LPS-stimulated RAW 264.7 macrophages, in which the compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μm) and TNF-α (IC50 = 1.87 μm) production. Further evaluation revealed that compound 6e displayed more potent in vivo anti-inflammatory activity than ibuprofen did on xylene-induced ear oedema in mice. Additionally, Western blot analysis revealed that compound 6e could restore phosphorylation level of IκBα and protein expression of p65 NF-κB in LPS-stimulated RAW 264.7 macrophages.

NOVEL PROCESS FOR THE PREPARATION OF 2-[4-(2-{4-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL]-1-PIPERIDINYL}ETHYL) PHENYL]-2-METHYLPROPANOIC ACID

The present invention relates to novel process for the preparation of 2-[4-(2-{4-[l-(2- ethoxyethyl)-lH-benzimidazol-2-yl]-l-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid represented by the following structural formula- 1. Formula- 1 The present invention also provides novel intermediate compounds useful for the preparation of compound of formula- 1.

PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS

The present invention relates to a process for preparing 2-methyl-2′-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present inv

Alternative synthesis of bilastine

A new and efficient synthesis of the non-sedating histamine H1 receptor antagonist Bilastine is reported. The new route employs a convergent strategy, with a longest linear sequence of five steps, giving slightly improved yields over the previous routes.

A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties

We have been exploring the potential of 5-HT2B antagonists as a therapy for chronic heart failure. To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes: (a) potent and selective antagonis