Related Products of 1978-39-8,Some common heterocyclic compound, 1978-39-8, name is 5-Fluoro-2-methoxyaniline, molecular formula is C7H8FNO, 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 compound Al (400 rng, 0.53 mrnoi) and 5-fluoro-2-rnethoxyaniline (150,7mg, 1.07 mmoi) intoluene (10 rnL) was added Ti(O-i] r)4 (151.6 mg, 0.53 mmoi). Themixture was stirred at 120 C over night under N2. The mixture was quenched with [120 (50 rnL) and extracted with DCM (20 mL x 3). The combined organic layer was dried over potassium carbonate, filtered and concentrated. The residue was purified by silica gel column chromatography (DCMMeOH = 15/i) to afford the crude products 29-1 and 29-2 (320 mg) as a yellow solid. LC-MS: m/z 89.4 [M+I-[. To a solution of compounds 29-1 and 292 (310 ing, 0.35 rnrnol) in DCM (5 mL) was added DAST (56.2mg, 0.35 mmoi) at -78 C underN2. After stirred at -78 C for 2 h, the mixture was quenched with aqueous NaHCO3 and 1-120 and then extracted with DCM (30 rnL x 3. The combined organic layer was dried over potassium carbonate, filtered and concentrated. The residue was purified by prep-HPLC to afford compound 29 (53 rng, yield17.5%) as white solid. Partial ?HNMR (CDC13, 400 MHz): 6.756.7I (m, 2H). 6.64-6.59 (rn, 2H), 4.89 (s, IH), 4.76-4.72 (rn. 1H), 4.43 (d, J= 8.0 Hz, IH), 4.34-4.30 (rn, TH), 3.87 (s. 3H). 2.59-2.50 (m, 21-1), LG-MS: m/z 871.4 [M¡ÀH.
The synthetic route of 1978-39-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; AGRIMETIS, LLC; CALABRESE, Andrew; (110 pag.)WO2018/132288; (2018); A1;,
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