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:

Nagarapu Laxmi Kumari12,Sudhakar Chithaluri1ORCID,Namana Suresh Babu3

Affiliation:

1. Department of Chemistry, School of Science, GITAM Deemed to be University, Hyderabad, Telangana-502329, India

2. Biophore India Pharmaceuticals Pvt. Ltd., Phase-II, IDA Pashamylaram, Hyderabad, Telangana-502329, India

3. Department of Chemistry, National Institute of Technology, Warangal, Telangana-506004, India

Abstract

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.

Publisher

Bentham Science Publishers Ltd.

Cited by 1 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. A Novel Synthesis and Quantitation Route of Belinostat;Current Organocatalysis;2024-08-16

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