79710-87-5Relevant articles and documents
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator
Aicher, Thomas D.,Baer, Brian R.,Boyd, Steven A.,Chicarelli, Mark D.,Condroski, Kevin R.,DeWolf, Walter E.,Fischer, John,Frank, Michele,Hingorani, Gary P.,Hinklin, Ronald J.,Lee, Patrice A.,Neitzel, Nickolas A.,Pratt, Scott A.,Singh, Ajay,Sullivan, Francis X.,Turner, Timothy,Voegtli, Walter C.,Wallace, Eli M.,Williams, Lance
supporting information, (2019/12/24)
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.
Synthetic method of 3-aminomethyl tetrahydrofuran
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Paragraph 0035; 0047; 0054; 0061; 0068; 0075, (2017/07/20)
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%.