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Org Lett. 2010 Dec 3;12(23):5526-9. doi: 10.1021/ol102428m. Epub 2010 Nov 1.

A selective and convenient method for the synthesis of 2-phenylaminothiazolines.

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  • 1Array BioPharma, 3200 Walnut Street, Boulder, Colorado 80301, USA.


A series of 2-phenylaminothiazolines have been prepared from the corresponding N-(2-hydroxyethyl)-N'-phenylthioureas under mild reaction conditions using either thio-CDI (1,1'-thiocarbonyldiimidazole) or CDI (1,1'-carbonyldiimidazole) to promote the cyclization. This protocol provides the desired cyclization products in good yield with excellent selectivity. The scope and selectivity of this methodology are also described.

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