Article ID Journal Published Year Pages File Type
5272295 Tetrahedron Letters 2012 4 Pages PDF
Abstract

An efficient one-step synthesis of a methotrexate fluorescein conjugate is described. Reaction of dried methotrexate with 5-aminofluorescein, mediated by HBTU, produced an isomerically pure methotrexate conjugate in good yield. Proof of structure was achieved by HPLC comparison of materials synthesized by development of a regiospecific pathway employing suitable protecting groups. Either strategy offers a general solution for the preparation of regiospecific methotrexate conjugates.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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