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Communication | Special issue | Vol 52, No. 2, 2000, pp.511-514
Published online, 1st January, 1970
DOI: 10.3987/COM-99-S49
Synthesis of Water Soluble Derivatives of Milbemycin D

Rei Matsueda* and Susumu Higashida

*Exploratory Chemistry Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan

Abstract

Water Soluble 5-O-(S-glutathionylthio)cysteinylmilbemycin D was successfully synthesized by using 3-nitro-2-pyridinesulfenyl (Npys) reagent through esterification of a Boc-cysteine derivative to a hydroxyl group at the C-5 position of milbemycin D, activation of the conventional S-protecting group, and asymmetrical disulfide bond formation.