تفاعل #324433

معادلة التفاعل

3-(5-chloro-2-hydroxy-phenoxy)-azetidine-1-carboxylic acid tert-butyl ester

title compound

5-Bromomethyl-2-trifluoromethyl-furan-3-carboxylic acid ethyl ester

Cs2CO3

→

title compound

المردود 71.2%

3-[5-Chloro-2-(4-ethoxycarbonyl-5-trifluoromethyl-furan-2-ylmethoxy)-phenoxy]-azetidine-1-carboxylic acid tert-butyl ester

المردود 71.2%

المذيبات

DMF

ظروف التفاعل

المعالجة

1. 1
   أخرىThe title compound was prepared
2. 2
   أخرىThe crude material was purified by RP HPLC

الإجراء التجريبي

The title compound was prepared as described in Example 1 Step D using 3-(5-chloro-2-hydroxy-phenoxy)-azetidine-1-carboxylic acid tert-butyl ester (0.3 g, 1.0 mmol), the title compound of Example 75 Step A (0.75 g, 2.5 mmol), Cs2CO3 (0.80 g, 2.4 mmol) and KI (0.23 g, 1.4 mmol) in DMF (15 mL). The crude material was purified by RP HPLC to provide the title compound (0.37 g, 71%). 1H NMR (CDCl3): 7.20-6.92 (m, 1H), 6.91-6.80 (m, 2H), 6.77-6.69 (m, 1H), 6.53 (d, J=2.1 Hz, 1H), 4.87 (s, 2H), 4.79-4.69 (m, 1H), 4.27-4.12 (m, 2H), 4.00-3.88 (m, 2H), 1.38 (s, 9H).

المصدر