135700-53-7

Upstream product

• 78942-85-5 2,3,4,6-tetra-O-acetyl-1-O-trifluoroacetyl-β-D-glucopyranose 
• 108-90-7 chlorobenzene 
• 604-69-3 β-D-glucose pentaacetate 
• 3947-62-4 2,3,4,6-tetra-O-acetyl-β-D-glucopyranose 
• 492-61-5 β-D-glucose 
• 90-80-2 D-Glucono-1,5-lactone 
• 32469-28-6 (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one 
• 873-77-8 (4-chlorphenyl)magnesium bromide 
• 4451-35-8 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosyl chloride 

Downstream Products

• 914922-79-5 (1S)-2,3,4,6-tetra-O-acetyl-1,5-anhydro-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-D-glucitol 
• 864070-44-0 empagliflozin 
• 2125472-55-9 (2-chloro-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)phenyl) (4-(((S)-tetrahydrofuran-3-yl)oxy)phenyl)methanone 
• 915095-99-7 (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)tetrahydro-2H-pyran-3,4,5-trityl triacetate 

Relevant academic research and scientific papers

Synthetic method of empagliflozin

The invention belongs to the technical field of raw material medicine preparation, and relates to a synthetic method of an SGLT-2 inhibitor empagliflozin, which comprises the following steps: 1) taking glucose as an initial raw material, and preparing an active intermediate 3 through full acylation, selective hydrolysis and esterification; 2) reacting the intermediate 3 with chlorobenzene under the catalysis of boron trifluoride/diethyl ether to generate an intermediate 4, and reacting the intermediate 4 with paraformaldehyde and phenoxy tetrahydrofuran to generate an intermediate 5; and 3) removing the protecting group under the action of alkali to obtain the final product empagliflozin. The method is simple to operate, low-temperature reaction in the prior art is avoided, and the purity of the obtained product is higher.

Processes for the Preparation of SGLT-2 Inhibitors, Intermediates Thereof

The present invention relates to novel, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and novel intermediates thereof. More particularly, the present invention relates to a novel, improved process for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline, or in the form of amorphous/crystalline solid dispersions/solutions with pharmaceutically acceptable polymers and preparation process thereof. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

Process For Production Of 4-Biphenylyazetidin-2-Ones

The present invention relates to processes for the production of 4-biphenylylazetidin-2-one derivatives of formula

Remarkable β-selectivity in the synthesis of β-1-C- arylglucosides: Stereoselective reduction of acetyl-protected methyl 1-C-arylglucosides without acetoxy-group participation

(Chemical Equation Presented) An efficient and practical process to generate β-C-arylglucoside derivatives was achieved. The process described involves Lewis acid mediated ionic reduction of a peracetylated 1-C-aryl methyl glucoside derived from the addit