1094071-11-0Relevant articles and documents
Raltitrexed synthesis of intermediates method (by machine translation)
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Paragraph 0030; 0031; 0058; 0059, (2018/05/16)
The invention belongs to the field of medical technology, in particular to a method for synthesizing intermediate raltitrexed. The method adopts the 2, 5 - thiophene dicarboxylic acid compound (1) by the Curtius rearrangement as a raw material to obtain compound (2); compound (2) in the phase transfer reagent, catalyst, the presence of a base with the N - methylation reagent by the reaction of the compound (3); compound (3) in the alkali aqueous solution or organic solvent mixed solution prepared by the hydrolysis of compound (4); the compound (4) and L - glutamic acid diester hydrochloride in the condensing agent and condensation activator role in the presence of a solvent condensation to make the compound (5); the compound (5) removing the amino protecting reagent in the reaction under the effect of the compound (6). The method overcomes the technical materials are not obtained easily, the price is expensive, the cost is high, the synthetic route is complicated and lengthy, the product does not easy to be purified and the like, to obtain the high purity of the intermediate. (by machine translation)
(R)-3-(N,N-DIMETHYLAMINO)PYRROLIDINE DERIVATIVES
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Page/Page column 77, (2010/04/27)
(R)-3-(N,N-Dimethyiamino)pyrrolidine derivatives of formula (I), wherein the meaning for Cy1 is as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors