These common heterocyclic compound, 1159010-96-4, name is 3-Bromo-5,6,7,8-tetrahydro-1,6-naphthyridine hydrochloride, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Product Details of 1159010-96-4
To a solution of 3-bromo-5,6,7,8-tetrahydro-1 ,6-naphthyridine hydrochloride (CAS:1159010-96-4, Vendor: PhamaBlock, 300 mg, 1.20 mmol), sodium carbonate (382 mg, 3.61 mmol) in THF (3 mL) and water (3 mL) was added N-[2- (trimethylsilyl)ethoxycarbonyloxyl succinimide (624 mg, 2.40 mmol). After being stirred at 25 C for 5 hrs, the reaction was quenched by addition of saturated NH4C1 (aq. 20 mL), diluted with 50 mL water, extracted with EA (30 mL) three times. The combined organic layer waswashed with water (30 mL) twice and brine (20 mL) once, dried over Na2SO4 and concentrated to give crude product which was purified by flash column (PE/EA = 10/1) to give compound 47a (400 mg) as a white solid. MS calc?d 357 (MHj, measured 357 (MHj.
The synthetic route of 3-Bromo-5,6,7,8-tetrahydro-1,6-naphthyridine hydrochloride has been constantly updated, and we look forward to future research findings.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; DEY, Fabian; KOU, Buyu; LIU, Haixia; SHEN, Hong; WANG, Xiaoqing; ZHANG, Weixing; ZHANG, Zhisen; ZHANG, Zhiwei; ZHU, Wei; (203 pag.)WO2019/238616; (2019); A1;,
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