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ChemicalBook CAS DataBase List 4-(5-BROMOTHIAZOL-2-YL)MORPHOLINE
933728-73-5

4-(5-BROMOTHIAZOL-2-YL)MORPHOLINE synthesis

2synthesis methods
-

Yield:-

Reaction Conditions:

with triethylamine in ethanol at 150; for 2 h;

Steps:

198.1
Step 1:
A solution of 2,5-dibromothiazole (1.0 equiv.), morpholine (1.5 equiv.) and triethylamine (4 equiv.) were heated to 150° C. for 2 h in the microwave.
After concentration, the mixture was partitioned between water and EtOAc.
The organic phase was washed with brine and dried over sodium sulfate.
The solution was concentrated and dried under vacuo to give crude N-(4-methyl-3-(2-morpholinothiazol-5-yl)phenyl)-3-(trifluoromethyl)benzamide and was used in the next step without further purification. LCMS (m/z) (M+H)=448.2, Rt=0.83 min.

References:

NOVARTIS AG;Barsanti, Paul A.;Burger, Matthew;Lou, Yan;Nishiguchi, Gisele;Polyakov, Valery;Ramurthy, Savithri;Rico, Alice;Setti, Lina;Smith, Aaron;Taft, Benjamin;Tanner, Huw;DiPesa, Alan;Yusuff, Naeem US2014/275003, 2014, A1 Location in patent:Paragraph 0708; 0709