A linear synthesis of gemcitabine

作者：Brown Kylie; Weymouth Wilson Alex; Linclau Bruno^*

来源：Carbohydrate Research, 2015, 406: 71-75.

DOI：10.1016/j.carres.2015.01.001

• Gemcitabine
• Glycosyl urea
• Fluorinated nucleoside
• Linear nucleoside introduction

Gemcitabine, 2'-deoxy-2',2'-difluorocytidine, is currently prescribed against a number of cancers. Here we report a linear synthesis of gemcitabine with a high-yielding direct conversion of 3,5-di-O-benzoyl-2-deoxy-2,2-difluororibose into the corresponding glycosyl urea as the key step, followed by conventional conversion to the cytosine base via the uracil derivative. The process proceeded with modest anomeric selectivity.

• 出版日期2015-4-10