79710-87-5

Upstream product

• 79710-86-4 tetrahydrofuran-3-carboxaldehyde 

Downstream Products

• 165253-31-6 (tetrahydro-3-furanyl)methylamine 

Relevant academic research and scientific papers

Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator

Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an inadequacy or defect in one or both of these processes, identifying compounds that can activate GK could provide a therapeutic benefit. Herein we report the further structure activity studies of a novel series of glucokinase activators (GKA). These studies led to the identification of pyridine 72 as a potent GKA that lowered post-prandial glucose in normal C57BL/6J mice, and after 14d dosing in ob/ob mice.

A versatile strategy for the synthesis of 4,5-dihydroxy-2,3-pentanedione (DPD) and related compounds as potential modulators of bacterial quorum sensing

Resistance to antibiotics is an increasingly serious threat to global public health and its management translates to significant health care costs. The validation of new Gram-negative antibacterial targets as sources for potential new antibiotics remains a challenge for all the scientists working in this field. The interference with bacterial Quorum Sensing (QS) mechanisms represents a potentially interesting approach to control bacterial growth and pursue the next generation of antimicrobials. In this context, our research is focused on the discovery of novel compounds structurally related to (S)-4,5-dihydroxy-2,3-pentanedione, commonly known as (S)-DPD, a small signaling molecule able to modulate bacterial QS in both Gram-negative and Gram-positive bacteria. In this study, a practical and versatile synthesis of racemic DPD is presented. Compared to previously reported syntheses, the proposed strategy is short and robust: it requires only one purification step and avoids the use of expensive or hazardous starting materials as well as the use of specific equipment. It is therefore well suited to the synthesis of derivatives for pharmaceutical research, as demonstrated by four series of novel DPD-related compounds described herein.

Synthetic method of 3-aminomethyl tetrahydrofuran

The invention discloses a synthetic method of 3-aminomethyl tetrahydrofuran. The synthetic method comprises the following steps: (1) carrying out cyclization reaction on 1,4-butylene glycol under the action of a fixed acid catalyst, so as to generate 2,5-dihydrofuran; (2) carrying out hydroformylation reaction on 2,5-dihydrofuran under the action of a homogeneous catalyst HRhCO[P(PhX)3]3, so as to obtain 3-formaldehyde tetrahydrofuran; (3) reacting by virtue of 3-formaldehyde tetrahydrofuran and hydroxylamine compounds, so as to obtain 3-formoxime tetrahydrofuran; and (4) carrying out hydrogenation on 3-formoxime tetrahydrofuran, so as to obtain 3-aminomethyl tetrahydrofuran. The synthetic method disclosed by the invention is environmentally friendly and has the beneficial effects that the process is simple, the steps are short, the total yield is very high, the cost is low, the yield of products in each step is higher than 90%, and the total yield of the finally prepared 3-aminomethyl tetrahydrofuran is higher than 80%.

NEW POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTOR

The present invention relates to indole derivatives useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said com- pounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.