Synthetic Route of 15963-46-9, These common heterocyclic compound, 15963-46-9, name is Methyl 3-chlorocyclobutanecarboxylate, 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.
To a solution of 8-chloro-N-(4-chloro-2-hydroxyphenyl)-4-oxo-chromene-2-carboxamide (190 mg, 543 m mol), methyl 3-chlorocyclobutane-l-carboxylate (105 mg, 75 m L, 543 mmol) in DMF (5 mL) was added CS2CO3 (260 mg, 782 miho) at room temperature and the resulting mixture was then stirred at 90 C for 12 hours. After the reaction was completed, the mixture was diluted with water (30 mL) and extracted with EtOAc (50 mL) three times. The combined organic layer was washed with brine, dried over anhydrous Na2S04 and concentrated in vacuo to give methyl 3-(5-chloro-2-(8-chloro-4-oxo-chromene-2-carboxamido)phenoxy)cyclobutane- 1- carboxylate (200 mg, 79.8 %) as a yellow foam, which was used in next step directly without further purification. MS obsd. (ESL) [(M+H)+]: 462.1.
The synthetic route of 15963-46-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; FENG, Song; LIANG, Chungen; LIU, Yongfu; TAN, Xuefei; WU, Jun; WANG, Jianping; (134 pag.)WO2020/79106; (2020); A1;,
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