Application of 6298-96-0, A common heterocyclic compound, 6298-96-0, name is 1-(4-Methoxyphenyl)ethylamine, molecular formula is C9H13NO, 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.
EXAMPLE 2; Preparation of 2-chloro-N-[(lS)-1-(4-methoxyphenyl) ethyl] -6-methyl-4-propoxy-3-pyridine- carboxamide (Compound 103); To 2-chloro-6-methyl-4-propoxy-3-pyridinecarboxylic acid (i. e. product of Example 1, Step A) (100 mg) was added thionyl chloride (2 mL), and the reaction mixture was stirred at room temperature for 2 hours. The excess thionyl chloride was evaporated in vacuo, and dichloromethane was added and evaporated in vacuo. The residual oil was dissolved in dichloromethane (approximately 2 mL) and added to a solution of (aS)-4-methoxy- a-methylbenzenemethanamine (79.2 mg) in dichloromethane (3 mL). A molar excess of PS-DMAP was added, and the reaction mixture was shaken at room temperature overnight. The reaction mixture was then filtered, and the solvent was evaporated in vacuo. The residual oil was triturated with 1-chlorobutane-hexanes (approximately 1: 1) to provide the title product, a compound of the present invention, as a white solid (92.3 mg) melting at 110-111 C. 1H NMR (CDC13,300 MHz) 8 7.33 (d, 2H), 6. 87 (d, 2H), 6.61 (s, 1H), 5.88 (br d, 1H), 5.29-5. 39 (m, 1H), 3.96 (t, 2H), 3.80 (s, 3H), 2.48 (s, 3H), 1.73-1. 84 (m, 2H), 1.59 (d, 3H), 0.98 (t, 3H)
The synthetic route of 6298-96-0 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; E.I. DUPONT DE NEMOURS AND COMPANY; WO2005/70889; (2005); A1;,
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