Title:A Simple and Efficient Path for the Synthesis Antineoplastic Agent
(2R,3R,4S,5R)-5-(6-Amino-2-Chloropurin-9-yl)-4-Fluoro-2-(Hydroxymethyl)
oxolan-3-ol (Clofarabine)
Volume: 21
Issue: 10
Author(s): Laxmi Kumari Nagarapu, Chithaluri Sudhakar*Suresh Babu Namana
Affiliation:
- Department of Chemistry, School of Science, GITAM Deemed to be University, Hyderabad, Telangana-502329, India
Keywords:
Phenol substrate, clofarabine (1), leukemia treatment, furanose moiety, non-toxic reagents, Eco friendly.
Abstract: Clofarabine (1) is an anticancer agent used to treat acute leukemia. This work discloses the
efforts to develop a convenient, environmentally benign, and high-yielding synthetic protocol leading
to Clofarabine (1). The synthesis includes bromination of 2-deoxy-2-β-fluoro-1,3,5-tri-O-benzoyl-1-
α-D-ribofuranose (6), followed by C-N coupling with a 2,6-dichloro purine (4) and selective amination
consecutively. The proposed total synthesis comprises five steps to afford an overall yield of 65-
70% with 99.85% purity. The present process provides preparation of Clofarabine (1) using a simple
purification process with lesser reaction time, better yield, and purity without using toxic and pyrophoric
chemicals.
