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Journal of Pharmaceutical Research

Article

Derivatization of Steroids for Obtaining Conjugates: Use as Vectors for Drug Delivery
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Journal of Pharmaceutical Research

Year: 2010, Volume: 9, Issue: 1, Pages: 5-10

Original Article

Derivatization of Steroids for Obtaining Conjugates: Use as Vectors for Drug Delivery

Abstract

Mono-mode microwave assisted additions of ?-aminoacids (glycine/valine/phenylalanine) in the presence of K2CO3 to 16? , 17?-epoxy-3?-hydroxypregnenolone (20) afford corresponding 17?-hydroxy-16-N-carboxyalkylaminosteroids (21a-c) in good yield. Similar conjugate addition of aminoacids to 16-dehydropregnenolone-3b -acetate (15), under identical conditions, affords 16-N-carboxyalkylamino steroidal derivatives (22a-c). All the products have been purified chromatographically and characterized spectroscopically. The obtained molecules can be conjugated with molecules/moieties for use as steroidal vectors.

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