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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Research Article

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)

Author(s): Laxmi Kumari Nagarapu, Chithaluri Sudhakar* and Suresh Babu Namana

Volume 21, Issue 10, 2024

Published on: 21 February, 2024

Page: [859 - 866] Pages: 8

DOI: 10.2174/0115701786287468240209105224

Price: $65

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.

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