162607-27-4

Usage

Uses

Used in Pharmaceutical Industry:
(5‐ethylfuran‐2‐yl)boronic acid is used as a reactant/reagent for the preparation of pyrazolopyrimidine compounds. These compounds serve as histone demethylase inhibitors, which are useful in treating cancer. By targeting specific enzymes involved in gene regulation, these inhibitors can potentially halt the progression of cancer cells and provide a novel therapeutic approach to cancer treatment.

Upstream product

• 3208-16-0 2-ethylfuran 
• 121-43-7 Trimethyl borate 
• 7732-18-5 water 

Downstream Products

• 62596-42-3 2-Ethyl-5-(4-methoxy-phenyl)-furan 
• 57044-49-2 2-ethyl-5-phenylfuran 
• 55854-89-2 8-methyl-7-propionylindolizino[1,2-b]quinoline-9(11H)-one 

Relevant academic research and scientific papers

Stereoselective Synthesis of cis-2-Ene-1,4-diones via Aerobic Oxidation of Substituted Furans Catalyzed by ABNO/HNO3

We report a highly efficient and selective catalytic system, ABNO (9-azabicyclo-[3.3.1]nonane N-oxyl)/HNO3, for the aerobic oxidation of substituted furans to cis-2-ene-1,4-diones under mild reaction conditions using oxygen as the oxidant. The catalyst system is amenable to various substituted (mon-, di-, and tri-) furans and tolerates diverse functional groups, including cyano, nitro, naphthyl, ketone, ester, heterocycle, and even formyl groups. Based on the control and 18O-labeling experiments, the possible mechanism of the oxidation is proposed.

Beta-carbolines V-type phosphodiesterase inhibitor and preparation method and usage thereof

The invention provides a Beta-carbolines V-type phosphodiesterase inhibitor and a preparation method and a usage thereof. The Beta-carbolines V-type phosphodiesterase inhibitor has a structure as shown in a formula (X): the formula is as shown in the desc

Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors

Based on perlolyrine (1), a natural alkaloid with weak PDE5 potency from the traditional Chinese aphrodisiac plant Tribulus terrestris L., a series α-substituted tetrahydro-β-carboline (THβC) derivatives were synthesized via T+BF4--mediated oxidative C–H functionalization of N-aryl THβCs with diverse potassium trifluoroborates. Following Winterfeldt oxidation afforded the corresponding furyl/thienyl pyrroloquinolones, of which 5-ethylthiophene/ethylfuran derivatives 20a–b were identified as the most potent and selective PDE5 inhibitors. Among the enantiomers, (S)-20a and (S)-20b (IC50 = 0.52 and 0.39 nM) were found to be more effective than their (R)-antipode, display favorable pharmacokinetic profiles, exert in vitro vasorelaxant effects on the isolated thoracic aorta, and exhibit in vivo efficacy in the anesthetized rabbit erectile model.

Phosphodiesterase inhibitor type 5 (PDE 5), and preparation method and application thereof

The invention discloses a PDE 5 and a preparation method thereof, and application of the PDE 5 to preparation of drugs used for treating, alleviating or preventing PDE 5-related diseases or disease states of mammals. The structural formula of the PDE 5 is as described in the specification. The preparation method for the PDE 5 is simple in process and mild in reaction conditions and utilizes cheap and easily available raw materials; and the prepared PDE 5 has the advantages of a definite target, high security and outstanding active effect and shows good application prospects in preparation of drugs used for treating PDE 5-related diseases, especially male erectile dysfunction (MED) or pulmonary arterial hypertension (PAH).

2-Pyridones from cyanoacetamides and enecarbonyl compounds: Application to the synthesis of nothapodytine B

The condensation of an enone or enal with cyanoacetamide derivatives and t-BuOK furnishes either 3-cyano-2-pyridones or 3-unsubstituted-2-pyridones, depending on whether the reaction is carried out in the presence or in the absence of O2. In the first case, in situ oxidation of Michael-type intermediates takes place; in the second case, the products result from "decyanidative aromatization" of such intermediates. A one-step synthesis of 3-alkyl-2-pyridones has been devised on the basis of decyanative union of an enone/enal and a 2-alkylcyanoacetamide. The new reaction forms the centerpiece of an unusually concise synthesis of nothapodytine B (mappicine ketone).