Some tips on 676273-39-5

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676273-39-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.676273-39-5,3-Iodo-1-tosyl-1H-indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

Compound 15 (0.682 g), [2-(trifluoromethyl)-3-thienyl] boronic acid (0.38 g) and 2N solution of Na2CO3 (0.514 g, 2.4ml) were taken in n-Butanol (5ml) in a RB flask. Resulting mixture was de- gassed for 10 min. To this, was added PdCl2(PPh3)2 (0.057 g) and again degassed for 5 min. Resulting reaction mixture was stirred and heated at 110C for 2 hrs under nitrogen atmos- phere. Reaction completion was monitored by TLC. After completion of reaction it was cooled to RT. Filtered the reaction through celite bed and washed with ethyl acetate. Filtrate was washed with water and brine. Organic layer was dried over Na2SO4 and evaporated completely. Crude compound was purified by flash column chromatography. Pure compound was eluted with 10- 25% ethyl acetate in heptane. Evaporated solvent under vacuum. It was concentrated under vacuum to afford 0.25 g (34.70%) of the desired product 18. 1H NMR (300 MHz, DMSO-d6) delta 8.20 (d, J = 8.7 Hz, 1H), 8.11 (d, J = 4.9 Hz, 2H), 8.05- 7.95 (m, 3H), 7.84 (dd, J = 8.7, 1.4 Hz, 1H), 7.51 (dd, J = 5.1, 1.4 Hz, 1H), 7.44 (d, J = 8.2 Hz, 2H), 2.34 (s, 3H).

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Reference:
Patent; BASF SE; POONOTH, Manojkumar; RHEINHEIMER, Joachim; RATH, Rakesh; ROSENBAUM, Claudia; WIEBE, Christine; BRAHM, Lutz; RUDOLF, Georg Christoph; KHANNA, Smriti; HADEN, Egon; ROEHL, Franz; SIEPE, Isabella; KREMZOW-GRAW, Doris; SCHIFFER, Helmut; (199 pag.)WO2018/210659; (2018); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles