1-(1,3-thiazol-2-yl)-1,4-diazepane synthesis

Yield:868065-15-0 76%

Reaction Conditions:

at 140; for 0.166667 h;

Steps:

3.a

Synthesis of Exemplary Compound 3: 1-Thiazol-2-yl-4-(3-phenylpropioloyl)-1,4-diazepane; a) Synthesis of 2-(1,4-diazepan-1-yl)thiazole; 11.0 g (110 mmol) of homopiperazine and 980 μl (11 mmol) of 2-bromothiazole were heated together to 140° C. for 10 min. The reaction solution was poured into water and this solution was saturated with NaCl and extracted with EA. The organic phase was washed with water and sat. aq. NaCl soln., dried over MgSO₄ and evaporated under a vacuum. 1.54 (8.4 mmol, 76%) of 2-(1,4-diazepan-1-yl)thiazole were obtained by crystallising the residue from ether.

References:

US2009/176756,2009,A1 Location in patent:Page/Page column 49