- Synthesis process of Raltitrexed key intermediate
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The invention relates to the technical field of medicine preparation, in particular to a synthesis process of a Raltitrexed key intermediate. According to the synthesis process of the Raltitrexed keyintermediate, forming an active intermediate (isocyanate) through glutamate diethyl ester, the active intermediate and N-methyl-(2-thienyl) tert-butyl carbamate are directly reacted, and a target product N-[5-[N-(t-butyloxycarboryl)-N-methyl amino]-2-thenoyl]-L-glutamate diethyl ester is prepared by two steps. The synthesis process avoids difficulties of potential risks of part of racemization ofa chiral center caused by amidation reaction, low yield, complicated operation and purification and the like. The synthesis process of the Raltitrexed key intermediate is simple to operate, short in line, environmentally friendly and high in yield.
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Paragraph 0047-0051
(2019/05/22)
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