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A method for synthesizing geleg only Iraq (by machine translation)

The present invention provides a method for synthesizing geleg only Iraq, the prepared composite organic metal reagent with 2 – (5-bromo-2-fluorobenzyl) benzothiophene halogen exchange to obtain the aryl metal compound intermediate; aryl metal compound occurs with gluconic acid lactone intermediates for the coupling reaction, hydroxy protection by dehydration 1-C – [3 – (benzo [B] thiophene-2-yl methyl) – 4-fluoro phenyl]-ALPHA-D-pyran glucitol; 1-C – [3 – (benzo [B] thiophene-2-yl methyl) – 4-fluoro phenyl]-ALPHA-D-pyran anhydroglucitol crude product obtained after reduction of net iraqi Geleg ; iraqi Geleg net crude purified acylated, and net iraqi Geleg deacyl reaction to obtain pure product. The composite organic metal reagent, the reaction temperature is increased, the cost is saved, is suitable for industrial production; the protection of the dehydroxylated aqueous acid, the crude product is solid and non-oil material, it is convenient to process and shorten the reaction time. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Awesome Chemistry Experiments For 2-(5-Bromo-2-fluorobenzyl)benzo[b]thiophene

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The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extracurricular laboratory:new discovery of C15H10BrFS

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SGLT-2 this invention relates to a method for preparing the inhibitor compound, the protection of the hydroxy compound A, coupling reaction, hydroxy group deprotected, ketal reaction steps I to obtain intermediate, and then through the obtained intermediate I preparation SGLT-2 inhibitor compounds. (by machine translation)

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extended knowledge of C15H10BrFS

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STEREOSELECTIVE SYNTHESIS OF INTERMEDIATES IN THE PREPARATION OF ss-C-ARYLGLUCOSIDES

The invention belongs to the fields of pharmaceutical industry, and particularly to an improved stereoselective synthesis of intermediate compounds for the preparation of gliflozins, for example canagliflozin or structurally similar gliflozins. Gliflozins, such as canagliflozin, dapagliflozin, empagliflozin, or ipragliflozin, inhibit the sodium-dependent glucose cotransporter 2 (SGLT2) in the kidney and as such are useful in the treatment of type-2 diabetes.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Ni-Catalyzed Suzuki-Miyaura Cross-Coupling of alpha-Oxo-vinylsulfones to Prepare C-Aryl Glycals and Acyclic Vinyl Ethers

We demonstrate that readily available and bench-stable alpha-oxo-vinylsulfones are competent electrophiles in Ni-catalyzed Suzuki-Miyaura cross-coupling reactions. The C-sulfone bond in the alpha-oxo-vinylsulfone motif is cleaved chemoselectively in these reactions, furnishing C-aryl glycals or acyclic vinyl ethers in high yields. These reactions proceed under mild conditions and tolerate a remarkable scope of heterocycles and functional groups. Preliminary mechanistic studies revealed the importance of an alpha-heteroatom in facilitating these transformations.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Discovery of Ipragliflozin (ASP1941): A novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus

A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have potent inhibitory activity against SGLT2 and good selectivity versus SGLT1. Through further optimization of 14a, a novel benzothiophene derivative (14h; ipragliflozin, ASP1941) was discovered as a highly potent and selective SGLT2 inhibitor that reduced blood glucose levels in a dose-dependent manner in diabetic models KK-Ay mice and STZ rats.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

More research is needed about C15H10BrFS

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Iraqi geleg net intermediate preparation method (by machine translation)

The invention discloses the Iraqi gliclazide net intermediate preparation method, including 2 – (3 – benzo [B] thiophene – 2 – yl methyl – 4 – fluoro – phenyl) – 3, 4, 5 – c – trimethyl siloxy – 6 – trimethyl siloxy methyl – tetrahydro – pyran – 2 – ol (compound 3) and (1 S) – 2, 3, 4, 6 – four-acetoxy – 1, 5 – dehydration – 1 – [3 – (1 – benzothiophene – 2 – yl methyl) – 4 – fluorophenyl] – D – sorbitol (compound 6) specific preparation method; wherein the control of the reaction temperature not higher than – 60 C under the premise, as soon as possible should be adds by drops positively BuLi, n-butyl and the faster the dropping speed, compound 3 of ortho-substituted F of less by-products, to ensure that the resulting compound 3 of purity, and had a direct impact on the resulting compound 6 yield, the present invention is amplified without amplifying effect, it is suitable for industrial production. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Ni-Catalyzed Suzuki-Miyaura Cross-Coupling of alpha-Oxo-vinylsulfones to Prepare C-Aryl Glycals and Acyclic Vinyl Ethers

We demonstrate that readily available and bench-stable alpha-oxo-vinylsulfones are competent electrophiles in Ni-catalyzed Suzuki-Miyaura cross-coupling reactions. The C-sulfone bond in the alpha-oxo-vinylsulfone motif is cleaved chemoselectively in these reactions, furnishing C-aryl glycals or acyclic vinyl ethers in high yields. These reactions proceed under mild conditions and tolerate a remarkable scope of heterocycles and functional groups. Preliminary mechanistic studies revealed the importance of an alpha-heteroatom in facilitating these transformations.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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A concise and practical stereoselective synthesis of ipragliflozin L-proline

A concise and practical stereoselective synthesis of ipragliflozin L-proline was presented starting from 2-[(5-iodo-2-fluorophenyl)methyl]-1-benzothiophene and 2,3,4,6-tetra-O-pivaloyl-alpha-D-glucopyranosyl bromide without catalyst via iodine?lithium?zinc exchange. The overall yield was 52% in three steps and the product purity was excellent. Two key diastereomers were prepared with efficient and direct access to the alpha-C-arylglucoside.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 2-(5-Bromo-2-fluorobenzyl)benzo[b]thiophene, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 1034305-17-3

Discovery of Ipragliflozin (ASP1941): A novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus

A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have potent inhibitory activity against SGLT2 and good selectivity versus SGLT1. Through further optimization of 14a, a novel benzothiophene derivative (14h; ipragliflozin, ASP1941) was discovered as a highly potent and selective SGLT2 inhibitor that reduced blood glucose levels in a dose-dependent manner in diabetic models KK-Ay mice and STZ rats.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem