Synthesis of new vitamin K derivatives with a ketone group at the C-1' position of the side chain and their conversion to menaquinone-4

合成侧链C-1'位带有酮基的新型维生素K衍生物及其转化为甲萘醌-4

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Abstract

Prior to being utilized in the body, dietary vitamin K homologues are converted to menaquinone-4 (MK-4) by cleavage of the side chain part followed by prenylation. We predicted that the prenylation would occur due to the electron deficiency at the C-1' position of the allyl moiety. Therefore, as an alternative method to make the C-1' position electron-deficient, a new vitamin K derivative was synthesized by introducing a ketone group, and its conversion to MK-4 was investigated. Introduction of a ketone group at the C-1' position of the side chain of 2',3'-dihydrophylloquinone, which is known to resist conversion to MK-4, induced conversion to the MK-4 analog to a degree similar to that of natural phylloquinone. Thus, the electron deficiency at the C-1' position is important for the conversion to MK-4.

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