Synthstic Of Direct Thrombin Inhibitor Dabigatran Etexilate And Progesterone Receptor Modulator Telapristone Acetate

This paper consists of two parts: the synthstic of Direct thrombin inhibitor Dabigatran etexilate and the synthstic of progesterone receptor modulator Telapristone acetate.Part Ⅰ: the synthstic of Dabigatran Etexilate. Dabigatran etexilate was synthesized from 4-aminobenzonitrile by carboxylation, esterification,amidination and other two-step reaction to give 2-(4-(N’-(hexyloxy Carbonyl)carbamimidoyl)phenylamino)acetic acid, which was subjected to reduction by acylchlorination and cyclization in the presence of ethyl3-(3-amino-4-(methylamino)-N-(pyridin-2-yl)benzamido)propanoate.Part Ⅱ: the synthstic of Telapristone acetate. Telapristone acetate was synthesized from ulipristal acetate as the starting material, through protection of the 3-Carbonyl group, iodination, substitution, methylation,deprotection of 3-carbonyl and acetylation of 17-hydroxy group.