cas 898566-17-1, 2-(4-Fluorophenyl)-5-[(5-iodo-2-methylphenyl)methyl]thiophene

Articles about 898566-17-1Total 11 be found

Preparation method of carbagliflozin intermediate and application of intermediate in preparation of glipizide
The invention provides a preparation method of a carbagliflozin intermediate and an application thereof in preparation of glipizide. To the preparation method, 5 - iodine -2 - methylbenzoic acid and a chlorination reagent are subjected to a Fourier acylation reaction, 5 - iodine -2 - methylbenzoyl chloride is obtained. The 5 -iod -2 -methylbenzoyl chloride and 2 - (4 - fluorophenyl) thiophene were subjected to a Fries alkylation reaction to give (5 -iod -2 -methylphenyl) (5 - (4 - fluorophenyl) thiophene -2 -yl) methyl ketone. (5 -iod -2 -methylphenyl) (5 - (4 - fluorophenyl) thiophene -2 -yl) methyl ketone was subjected to a carbonyl reduction reaction to give a crude product of. The intermediate crude product is subjected to purification treatment to obtain the glipizide intermediate. The preparation method has the advantages of mild reaction conditions, simple operation, environmental protection, safety, suitability for industrial mass production, and high product yield and purity.
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Paragraph 0043; 0067; 0070-0073; 0076-0079; 0082; ...

(2021/11/26)

METHOD FOR MANUFACTURING DIARYLMETHANE COMPOUND
An object is to provide a method for producing a compound which is useful as a synthetic intermediate for an active pharmaceutical ingredient of an antidiabetic drug or the like in an industrially inexpensive and efficient manner, and the present invention can achieve the object by reducing a compound (2) represented by the following formula (2): wherein R1, Ar, n and X are as mentioned herein in the presence of a titanium compound by using a reducing agent to produce a compound (1) represented by the following formula (1): wherein R1, Ar and n are the same as defined above.
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Paragraph 0192-0215

(2021/07/02)

SYNTHESIS, CRYSTAL STRUCTURE, ANTI-LUNG CANCER ACTIVITY OF 2-(4-FLUOROPHENYL)-5- (5-IODO-2-METHYLBENZYL)THIOPHENE
Abstract: New heterocycle compound 2-(4-fluorophenyl)-5-(5-iodo-2-methylbenzyl)thiophene (1), designed using5-iodo-2-methylbenzoic acid (2) as the starting material is successfully obtained via the multiple synthesis route and finally characterized by IR, 1H NMR, and single crystal X-ray crystallography. In addition, the in vitro anticancer activity of compound 1 on three human lung cancer cells (H20, H2227, and H69) is further determined, which suggests that compound 1 may be a potential anticancer agent.
Dong, Y. L.,Liu, J. P.,Qiu, F.,Wang, C. M.,Zhang, Z. F.,Zhou, L. P.
p. 1111 - 1116
(2020/09/09)

Synthesis method of canagliflozin intermediate
The invention relates to a synthesis method of a canagliflozin intermediate. Concretely, succinyl oxide and fluorobenzene are used as starting raw materials to be prepared into the canagliflozin crucial intermediate of 2-(4-fluorophenyl)-5-[(5-halogen-2-methyl phenyl)methyl]thiophene through the steps of Friedel-Crafts acylation ring opening, thiophene ring preparation, Friedel-Crafts acylation coupling, reduction and the like. The cheap succinyl oxide is used for preparing the thiophene ring, so that the Suzuki coupling reaction and Grignard reaction are avoided; the use of heavy metal reagents of palladium and the like is avoided; the production process is simplified; the product yield and the quality are improved; the environment pollution is reduced; the production cost is reduced.
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Paragraph 0054; 0055; 0056

(2018/03/26)

Synthesis and Optimization of Canagliflozin by Employing Quality by Design (QbD) Principles
Efforts toward a synthesis and process optimization of canagliflozin 1 are described. Canagliflozin synthesis was accomplished via purified open ring intermediate 12. The process was optimized by employing quality by design (QbD) methodologies, and a telescopic strategy was executed for the first three and last two steps in a total six-step sequence. Optimization of the Friedel-Craft acylation reaction followed by Lewis acid mediated reductive elimination, n-BuLi mediated C-arylation, and reductive demethoxylation was performed to develop a robust process. These steps were found to be critical; therefore, critical process parameters (CPPs) were identified by employing design of experiment (DoE) methodology. In addition, control strategies for dealing with impurities are described.
Metil, Dattatray S.,Sonawane, Swapnil P.,Pachore, Sharad S.,Mohammad, Aaseef,Dahanukar, Vilas H.,McCormack, Peter J.,Reddy, Ch. Venkatramana,Bandichhor, Rakeshwar
p. 27 - 39
(2018/01/28)

A antidiabetic drug synthesis of intermediates method
The invention discloses a synthetic method of an antidiabetic drug intermediate (I). According to the method, in the presence of a particular reducing agent, a compound shown in the formula II is converted into a compound shown in the formula I.
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Paragraph 0028-0031

(2017/10/06)

A hypoglycemic compound and its preparation method and application
The invention discloses an efficient blood glucose reducing compound as well as a preparation and an application thereof. The structure of the compound disclosed by the invention is shown in a formula I, in the formula, R1, R2, R3 and R4 are defined in specification and claims. The invention further discloses the preparation method of the compound shown in the formula I. The compound shown in the formula I has an inhibiting activity to SGLT (Sodium-Glucose-Linked Transporter), and can be effectively used for preventing or treating diseased related to hyperglycemia.
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Paragraph 0137; 0138; 0139

(2017/01/31)

TABLETS CONTAINING A 1-(?-D-GLUCOPYRANOSYL)-3-(PHENYLTHIENYLMETHYL)BENZENE COMPOUND
The present invention is directed to a tablet containing a 1-(β-D-glucopyranosyl)-3-(phenylthienylmethyl)benzene compound in high drug loading, in particular, containing the compound ranging from 30 to 95% by weight of tablet and pharmaceutically acceptable additives.
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Paragraph 0097; 0098

(2016/09/12)

Process for synthesizing card Geleg only (by machine translation)
The invention discloses a process for synthesizing card Geleg only, in order to 2?Methyl benzoic acid as starting material, use of improvised catalyst, reaction to produce the iodine iodate a in the middle, or in 2?Methyl benzoic acid as starting material, the metal reagent and under the action of catalyst, by adding liquid bromine, synthetic intermediates b; optionally intermediate one or intermediate two acylation reaction with thionyl chloride, to Friedel-crafts reaction produce intermediate three; in order to ALPHA?D?Glucose as raw material, with the reaction protection of all hydroxyl after pivalyl chloride, and then with zinc bromide, trimethyl silane reaction produce intermediate four; three intermediate the intermediate body, connecting delivery into intermediate five; finally under acidic conditions to remove the acyl special fifth heavenly stem, produce the target compound. card Geleg only of the present invention new process for the synthesis of high yield, mild condition, safety and reliability, is suitable for industrial production, raw material is cheap and easy to obtain, it is beneficial to control the production cost. (by machine translation)
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(2016/12/01)

PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT
The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
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Page/Page column 43

(2010/05/13)

PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT
The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
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Page/Page column 77

(2009/04/25)