Efficient synthesis of A 1,4-dihydro-2H-3,1-benzoxazin-2-one

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters

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C07C27128

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061145696

ABSTRACT:
An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.

REFERENCES:
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Uchida M., et al., Chem. & Pharm. Bull., vol. 38(6), pp. 1575-1586, 1990.
Gouilleux, L., et al., Tetrahedron Letters, vol. 39(37), pp. 7031-7034, 1996.
Radesca, L.A., et al., Synthetic Communications, vol. 27(24), pp. 4373-4384, 1997.

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