Canagliflozin Basic Product Information

Product Name	Canagliflozin	CAS	842133-18-0
Synonyms	(1S)-1,5-Anhydro-1-(3-{[5-(4-fluorophenyl)-2-thienyl]methyl}-4-methylphenyl)-D-glucitol;	Molecular Formula	C24H25FO5S
EINECS Number	695-192-1	Molecular Structure
Appearance	Light Yellow Powder
Purity
Supply Ability

Canagliflozin Quality documents

Canagliflozin Appearance/Package/Shipping/Storage

package

storage condition

Store in cool & dry place,Keep away from strong light and heat

Canagliflozin Application

Canagliflozin literature

Preparation method of SGLT-2 inhibitor and intermediate

-

, (2021/05/19)

The invention discloses a preparation method of an SGLT-2 inhibitor and an intermediate. The method comprises the following steps: (1) reacting a compound A with chlorosilane under the action of an acid-binding agent to generate a compound B; (2) mixing the compound B and a compound C to obtain a compound D; and (3) reacting the compound D with a reducing agent and a catalyst to obtain the SGLT-2 inhibitor compound.

Stereoselective Preparation of C-Aryl Glycosides via Visible-Light-Induced Nickel-Catalyzed Reductive Cross-Coupling of Glycosyl Chlorides and Aryl Bromides

Mou, Ze-Dong,Wang, Jia-Xi,Zhang, Xia,Niu, Dawen

supporting information, p. 3025 - 3029 (2021/05/27)

A nickel-catalyzed cross-coupling reaction of glycosyl chlorides with aryl bromides has been developed. The reaction proceeds smoothly under visible-light irradiation and features the use of bench-stable glycosyl chlorides, allowing the highly stereoselective synthesis of C-aryl glycosides. (Figure presented.).

METHOD FOR PRODUCING C-ARYL GLYCOSIDE DERIVATIVE

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Paragraph 0091-0097, (2021/06/25)

PROBLEM TO BE SOLVED: To provide a method that can produce a C-aryl glycoside derivative stably and inexpensively. SOLUTION: A method for producing a C-aryl glycoside derivative includes the step of mixing, for example, in an organic solvent, the following benzyl-protected C-aryl glycoside derivative (IaA), at least one silyl compound selected from trimethylsilyl chloride and trimethylsilyl bromide, and an alkali metal iodide, thereby producing the following C-aryl glycoside derivative (IIaA). SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

Preparation method of canagliflozin

-

, (2020/02/14)

The invention discloses a preparation method of canagliflozin. According to the method, the reaction of each step in a route is improved, so that the conversion rate of raw materials is increased, andintroduction of potential toxic compounds is avoided. In addition, reaction conditions are mild; operation is simple; purity of an obtained product is high; quality of drugs is improved; and the preparation method is suitable for industrial production.

Canagliflozin Upstream and downstream

842133-18-0 Upstream product

• 1132832-76-8

  1-[1-hydroxy-2,3,4,6-tetra-O-(trimethylsilyl)-β-D-glucopyranosyl]-4-methyl-3-[[5-(4-fluorophenyl)-2-thienyl]methyl]benzene 

• 866607-35-4

  (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate 

• 1030825-21-8

  methyl 1-C-(3-{[5-(4-fluorophenyl)-2-thienyl]methyl}-4-methyl-phenyl)-D-glucopyranoside 

• 1283129-18-9

  (2S,3S,4R,5R,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(pivaloyloxymethyl)tetrahydro-2H-pyran-3,4,5-triyl tris(2,2-dimethylpropanoate) 

• 898566-17-1

  (2-(4-fluorophenyl)-5-[(5-iodo-2-methylphenyl)methyl]thiophene) 

• 1283129-24-7

  C₃₆H₂₈F₂S₂Zn 

• 492-62-6

  alpha-D-glucopyranose 

• 81058-27-7

  2,3,4,6-tetra-O-pivaloyl-α-D-glucopyranosyl bromide 

842133-18-0 Downstream Products

• 928672-86-0

  (1S)-1,5-anhydro-1-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol hemihydrate 

• 866607-35-4

  (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate 

• 1409936-68-0

  L-proline-(2S,3R,4R,5S,6R)-2-{3-[5-(4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}-6-hydroxymethyl-tetrahydro-pyran-3,4,5-triol 

• 1409936-69-1

  (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol citric acid co-crystal 

• 1432187-89-7

  canagliflozin D-proline complex 

• 1432187-87-5

  canagliflozin L-phenylalanine complex 

• 928672-86-0

  1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hydrate 

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