反应详情

To a solution of the product of Step 4 (239 mg, 0.595 mmol) in ethyl acetate (5.4 mL)/acetic acid (0.54 mL) was added Pd/C (10 wt %, 60 mg, 0.056 mmol) and the reaction flask was purged with N2 and then H2. The reaction was stirred for 4 hr at room temperature under H2 (balloon; 25 mg of Pd/C were added after 2 h to complete the reaction) and then filtered through a microfilter (Glass Acrodisc 25 mm) and was washed with dichloromethane. The filtrate was concentrated, stripped with toluene (3×) and then dried under vacuum overnight to provide 221 mg (0.595 mmol, quant. yield) of {5-[3-amino-5-(morpholin-4-yl)phenyl]-1,3-thiazol-2-yl}(dicyclopropyl)methanol as a fluffy solid of sufficient purity to be used directly. MS APCI: [M+H]+ m/z 372.1.

1. customthe reaction flask was purged with N2
2. addition25 mg of Pd/C were added after 2 h
3. customthe reaction) and
4. filtrationthen filtered through a microfilter (Glass Acrodisc 25 mm)
5. washwas washed with dichloromethane
6. concentrationThe filtrate was concentrated
7. customdried under vacuum overnight