2H-1,4-Benzoxazin-3(4H)-one, 8-(1-piperazinyl)- synthesis

5synthesis methods

Product Name:2H-1,4-Benzoxazin-3(4H)-one, 8-(1-piperazinyl)-
CAS Number:105685-36-7
Molecular formula:C12H15N3O2
Molecular Weight:233.27

321126-82-3 Synthesis

321126-82-3
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821-48-7 Synthesis

821-48-7
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2H-1,4-Benzoxazin-3(4H)-one, 8-(1-piperazinyl)-

105685-36-7
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Yield:105685-36-7 64%

Reaction Conditions:

in chlorobenzene; for 100 h;Reflux;

Steps:

38

Intermediate 59:[0209] To a solution of intermediate 58 (164 mg, 1.0 mmol) in chlorobenzene (5 mL) was added bis(2-chloroethyl)amine hydrochloric acid (285 mg, 1.6 mmol) and the mixture was heated to reflux for 100 h. The reaction mixture was concentrated in vacuo and the residue was stirred in EtOAc for 2 h. The resulting brown solid was filtered and purified by silica gel chromatography to give 8-(piperazin-l-yl)-2H-benzo[b][l,4] oxazin-3(4H)-one (intermediate 59) (150 mg, 64%). HPLC: 99%, RT 1.344 min. MS(ESI) m/z 234.1 [M + H]⁺.

References:

WO2012/3418,2012,A2 Location in patent:Page/Page column 94

870064-73-6 Synthesis