2-(5-BroMo-2-Methylbenzyl)-5-(4-fluorophenyl)thiophene NEW

CAS:	1030825-20-7
MF:	C18H14BrFS
MW:	361.27
EINECS:	807-103-7
Product Categories:	Pharmaceutical intermediates;1030825-20-7
Mol File:	1030825-20-7.mol

Uses

2-[(5-Bromo-2-methylphenyl)methyl]-5-(4-fluorophenyl)thiophene is an antidiabetic agent that can be used to prepare Canagliflozin (C175190), a sodium-dependent glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus.

Synthesis

prepares 2-(4-fluorophenyl) thiophene III: Prepared by Grignard reagent: N 2under protection; magnesium chips (11.7g is added in the 500mL there-necked flask that thermometer, reflux condensing tube, constant pressure funnel be housed; 480mmol), THF (15.0mL), drips 2 p-Fluoro bromo benzenes; add the initiation reaction of 2 iodine post-heating; p-Fluoro bromo benzene (70.0g, 400mmol) is dissolved in THF (250mL), after under reflux, drip the THF solution of p-Fluoro bromo benzene; drip Bi Baowen backflow 2h, GC detection feedstock conversion complete. Linked reaction: N 2under protection; in the 1000mL there-necked flask that thermometer, reflux condensing tube, constant pressure funnel be housed, add 2-bromothiophene (52.2g, 320mmol), under stirring, add two (methyl ethyl diketone) palladium (23.4mg; 0.0320mmol); THF (200mL), is heated to 50 DEG C, the above-mentioned Grignard reagent prepared of rear dropping; drip to finish and be warming up to 60 DEG C; insulation 1h, GC detect to raw material reaction complete, terminate reaction.System is cooled to 30 DEG C, drips dilute hydrochloric acid (2M, 150mL) under ice-water bath, drips complete vigorous stirring 0.5h, removes ice-water bath and make system naturally rise to room temperature, stratification, water layer CH 2cl 2(100mL × 3) extract, merge organic phase saturated sodium-chloride 200mL to wash, rear drying, concentrating under reduced pressure obtain light tan solid, vacuum-drying to constant weight obtains 2-(4-fluorophenyl) thiophene III (57.4g, 312mmol), it is 98.5% that GC detects purity, and yield is 99.1%. 1H NMR(500MHz,CDCl 3)δ7.65～7.54(m,2H),7.33～7.22(m,2H),7.14～7.03(m,3H).Gc-Ms:178.1.

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Company information
Hebei Mojin Biotechnology Co., Ltd, Our company is a professional in 4'-Methylacetophenone,Levamisole hydrochloride ,N-Methylformamide and other chemical reagents research and development production enterprises. Our business covers more than 30 countries, most of the big customers come from Europe, America and other countries in the world, we can guarantee the quality and price. In recent decades, with the efforts of all employees, we have established many cooperative companies in shandong, henan, guangdong and other places. Our corporate purpose is based on the market, enhance the strength, take the road of scientific and environmental sustainable development, relying on the country. Technology r & d center, increase the investment in r & d, based on the domestic market, expand the international market, manufacturing quality products, sincere service to the society, into a modern, ecological, scientific and technological enterprise world.

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