Efficient Syntheses of 2-Chloro-2‘-Deoxyadenosine (Cladribine) from 2-Chloroadenosine

Abstract:

We report efficient syntheses of the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo), which is the drug of choice against hairy-cell leukemia and other neoplasms, from 2-chloroadenosine. Treatment of 3´, 5´-O-triacetyl-2-chloroadenosine (4) with PTC-Cl and followed by HCO2Na and (Bu4N)2S2O8 gave high yields of the 2´-deoxy-3´,5´-O-triacetyl-2-chloroadenosine which can be converted into target product after convenient deprotection step. This method avoids of using toxic Sn regent which is good for the medical industry production.

• Periodical: Advanced Materials Research (Volumes 535-537)
• Pages: 2425-2428
• DOI: https://doi.org/10.4028/www.scientific.net/AMR.535-537.2425
• Online since: June 2012
• Authors: Shao Hong Xu
• Keywords: 2-Chloro-2‘-Deoxyadenosine, 2-Chloroadenosine, Cladribine

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