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Watch online fresh new movies with no download. Pakistani entertainment channel, Khaama-e-din.Sphingosine, or D-erythro-sphingosine, is a naturally occurring sphingolipid which is known to have biological activity and has been characterized structurally as the following specific compound: ##STR1##
The D-erythro-sphingosines have also been shown to have immunosuppressive activity, due, it is believed, to inhibition of a particular sub-set of T-cells. The isomers have also been shown to inhibit arachidonic acid metabolism and may inhibit tumor growth and metastasis. Liposomes containing sphingosine and D-erythro-sphingosine have been used as an adjuvant for vaccinations and as a carrier for the delivery of other agents to animals.
There are very few chemical syntheses for sphingosine. The present invention describes an enantioselective, regiospecific synthesis of this compound in high yield and high enantiomeric purity.
The great majority of the syntheses reported in the literature for the sphingosine series have used a Friedlander’s synthesis as a key step (G. N. Cahn and J. Falbe, Angew Chem. 74: 912 (1972)). This involves the reaction of a nitrone formed from an acid chloride or trichloroacetamide with a 2-amino alcohol to obtain a sphinganine derivative and then regioselective reduction, often by chemical methods, to form the sphingosine.
The present invention describes an alternative synthesis that allows direct and regiospecific synthesis of the desired enantiomer. In this method, the C.sub.6 primary and C.sub.5 secondary functional groups are positioned on the same face of the double bond in the starting material. In the resulting molecule, a cationic species attacks from the same face, creating a diene moiety that can be reduced via the well-known radical reduction using NaBH.sub.4 as reducing agent. ##STR2##
In this way, the 9-trans-11-cis- double bond geometry is preserved and the resulting molecule is transformed into the final sphingosine.
See also, K. C
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