Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 136117-74-3, name is Imidazo[1,2-a]pyridine-8-carbaldehyde. A new synthetic method of this compound is introduced below., Recommanded Product: 136117-74-3
Intermediate 5 : ci&3-( Imidazol” 1.2-al pyridin-8-ylmethyl)amino”|cyclobuta nolTo an emulsion of s-3-aminocyclobutanol hydrochloride (1.254g, 10.15mmol) in DCM (15mL) was added MeOH (60mL), imidazo[l,2-a]pyridine-8-carbaldehyde (1.5g, 10.26mmol) and DIPEA (2mL, 11.45mmol) and the reaction mixture stirred at room temperature under nitrogen for 10 minutes. Sodium triacetoxyborohydride (5.4g, 25.5mmol) was then added and the reaction mixture stirred under nitrogen for 18 hours and then concentrated in vacuo. The residue was dissolved in DCM (200mL), aqueous sodium hydroxide (2M, 200mL) was added and the mixture was stirred at room temperature for 1 hour. The layers were separated and to the aqueous phase was added sodium hydroxide pellets (ca. 5g) which was then extracted with 3:1chloroform sopropanol (2 x 500mL). The combined organic extracts were dried using a hydrophobic frit, evaporated in vacuo and the residue was dissolved in DCM and purified on a silica cartridge (lOOg) using a 0-25% methanol-DCM gradient over 60 min. The product containing fractions were combined and evaporated in vacuoto give the title compound as an orange oil (2.3g).LCMS (System B): tier = 1.33 min; MH+ 218
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Reference:
Patent; GLAXO GROUP LIMITED; BIGGADIKE, Keith; BRAVI, Gianpaolo; CHAMPIGNY, Aurelie Cecile; COE, Diane Mary; NEEDHAM, Deborah; TAPE, Daniel Terence; WO2012/139963; (2012); A1;,
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