New method for continuously operating to synthesize capecitabine

Abstract

The invention relates to a new method for continuously operating to synthesize capecitabine, which is characterized in that 5-flucytosine is subjected to acylation, condensation and hydrolysis to synthesize the capecitabine. The invention has the advantages of reasonable reaction sequence, continuous operation of three steps, operation simplification, high yield, low cost and less pollution.

Description

technical field The invention belongs to the technical field of medicinal chemistry, and in particular relates to a new continuous operation method for synthesizing capecitabine. Background technique There are several synthetic methods for the important anticancer drug capecitabine, the most commonly used one is the method using 5-fluorocytosine as the starting material. According to the different reaction sequences, this method is divided into two types: method one: Reference: US 5742949 US 2005 137392 WO 2008 145403 US 2009 209754 Since the price of 1,2,3-triacetyl-5-deoxy-D-ribose is much higher than other raw materials, the first step of this method is to use 1,2,3-triacetyl-5-deoxy-D-ribose, Therefore, the consumption is higher and the cost is increased, which is the disadvantage of this method. Method Two: references WO 2005 080351 WO 2009 071726 In the second step of this method, 1,2,3-triacetyl-5-deoxy-D-ribose is used, and the dosage is reduced,...

AI Technical Summary

Problems solved by technology

However, in the literature, the three-step reaction is operated separately, and the separation of two intermediates is required. The loss is relatively large, the yield is low, the operation is cumbersome, the amount of solvent is large, the number of distillation recovery is large, and the cost is high.

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