These common heterocyclic compound, 1484-26-0, name is 3-Benzyloxyaniline, 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. Safety of 3-Benzyloxyaniline
General procedure: [0158]7?c?3). Compound Ta or Tv (0.02 minol) dissolved in 0.5 ml.. of DMF was added to a solution of corresponding amines (0.04 mmol), HOB?I? (3.06 rng, 0.02 rnmol), [II3TU (7.5 mg, 0.02 inmol), and D1PEA (5.16 1±L, 0.04 mmol) in I mE of DMF. The mixture was stirred under room temperature for 4 hours. This crude product was purified by Pre-HPLC to give Ta?I to 7?a-3 and 7?c?l to 7?c?3.[0159] 2-(-ft3-(benzyloxy)phenyl)amino)-4-oxobntyfl-6-hydroxy-3-iodo-l-methyl-lH-indole-5-carboxylic acid (Ta-i, L89M52). White solid (5.4 tug,46percent): H NMR (500 MHz, DM80): iS 13.68 (s, IN), 11.27(s, 111), 9.91 (s, 111), 7.70(5, 1 H ), 7.45?7.3 1 (m, 611), 7. 18 (m, 1K), 7.10 (in, I H), 6.96 (s, 1 K), 6.69 (in, 111).5.05 (s. 211), 3.73 (a, 3K), 2.65 (nt 2H), 2.39 (in, 2H), 1.87 (in, 2H); LC-MS (ESI):607.0 (M±Na, 582.8 (M-H)?; Purity: >95percent WV, A 254 urn).
The synthetic route of 3-Benzyloxyaniline has been constantly updated, and we look forward to future research findings.
Reference:
Patent; INDIANA UNIVERSITY RESEARCH & TECHNOLOGY CORPORATION; ZHANG, Zhong-Yin; ZENG, Li-Fan; WO2014/176488; (2014); A1;,
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