360775-96-8

Upstream product

• 83-87-4 D-glucose pentaacetate 
• 37155-50-3 2-(4-methoxybenzyl)phenol 
• 85604-67-7 2-(tetrahydropyran-2-yloxy)benzaldehyde 
• 90-02-8 salicylaldehyde 
• 108-95-2 phenol 
• 18733-07-8 (2-hydroxyphenyl)(4-methoxyphenyl)methanone 
• 92052-29-4 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl trichloroacetimidate 
• 100-66-3 methoxybenzene 
• 21615-34-9 2-Methoxybenzoyl chloride 
• 3947-62-4 2,3,4,5-tetra-O-acetyl-D-glucopyranose 
• 604-69-3 β-D-glucose pentaacetate 
• 824-94-2 p-methoxybenzyl chloride 
• 572-09-8 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosyl bromide 
• 7234-29-9 2-iodophenyl β-D-glucopyranoside 

Downstream Products

• 408504-26-7 Sergliflozin etabonate 
• 408504-27-8 2-{[4-(methyloxy)phenyl]methyl}phenyl-6-O-[(methyloxy)carbonyl]-β-D-glucopyranoside 
• 866476-37-1 2-[(4-methoxyphenyl)methyl]phenyl 6-O-(1,1-dimethylethyl)-β-D-glucopyranoside 

Relevant academic research and scientific papers

Discovery of Salidroside-Derivated Glycoside Analogues as Novel Angiogenesis Agents to Treat Diabetic Hind Limb Ischemia

Therapeutic angiogenesis is a potential therapeutic strategy for hind limb ischemia (HLI); however, currently, there are no small-molecule drugs capable of inducing it at the clinical level. Activating the hypoxia-inducible factor-1 (HIF-1) pathway in skeletal muscle induces the secretion of angiogenic factors and thus is an attractive therapeutic angiogenesis strategy. Using salidroside, a natural glycosidic compound as a lead, we performed a structure-activity relationship (SAR) study for developing a more effective and druggable angiogenesis agent. We found a novel glycoside scaffold compound (C-30) with better efficacy than salidroside in enhancing the accumulation of the HIF-1α protein and stimulating the paracrine functions of skeletal muscle cells. This in turn significantly increased the angiogenic potential of vascular endothelial and smooth muscle cells and, subsequently, induced the formation of mature, functional blood vessels in diabetic and nondiabetic HLI mice. Together, this study offers a novel, promising small-molecule-based therapeutic strategy for treating HLI.

An efficient and practical preparation of a potent low-affinity na+-dependent glucose cotransporter (SGLT2) inhibitor, sergliflozin etabonate

The development of an efficient and practical process for the preparation of Sergliflozin etabonate (1), a prodrug of a novel selective low-affinity Na+-dependent glucose cotransporter (SGLT2) inhibitor, Sergliflozin (2), is described. Its development required a suitable process for large-scale manufacturing. We established a chromatography-free approach for 2-[(4-methoxyphenyl)methyl]phenol (5), the efficient O-glycosylation of 5 with penta-O-acetyl-β-D-glucopyranose (7) without using a trichloroacetimidate intermediate (9), and efficient reaction conditions to introduce an ethoxycarbonyl group onto the primary alcohol of 2 with high selectivity. This process provided 1 with a 45% overall yield from anisole (10).

Modification on the O-glucoside of Sergliflozin-A: A new strategy for SGLT2 inhibitor design

Poor pharmacokinetic stability is one of the issues of O-glucoside SGLT2 inhibitors in clinical trials, hence C-glucoside inhibitors have been developed and extensively applied. Herein, we provided an alternative approach to improve the pharmacokinetic st

LiCl-mediated preparation of functionalized benzylic indium(III) halides and highly chemoselective palladium-catalyzed cross-coupling in a protic cosolvent

(Chemical Equation Presented) Sensitive functional groups such as COR, CHO, or CH2OH can be present in benzylic indium reagents prepared by the direct insertion of indium in the presence of LiCl. These reagents undergo palladium-catalyzed cross

Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a group forming a prodrug; and R represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower al

GLUCOPYRANOSYLOXY BENZYLBENZENE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES FOR THE PREPARATION OF THE DERIVATIVES

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy( lower alkyl) group; and R2 represents a lower alkyl group, a lower al

GLUCOPYRANOSYLOXYBENZYLBENZENE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a group forming a prodrug; and R represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower al