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阿瑞匹坦与焦磷酸四苄酯缩合得[3-[[(2R,3S)-2-[(1R)-1-[3,5-二(三氟甲基)苯基]乙氧基]-3-(4-氟苯基)-4-吗啉基]甲基]-5-氧代-4,5-二氢-1H-1,2,4-三唑-1-基]磷酸二苄酯,在甲醇中脱除一个苄基得[3-[[(2R,3S)-2-[(1R)-1-[3,5-二(三氟甲基)苯基]乙氧基]-3-(4-氟苯基)-4-吗啉基]甲基]-5-氧代-4,5-二氢-1H-1,2,4-三唑-1-基]-磷酸单苄酯,经催化氢化脱苄并与葡甲胺成盐得神经激肽-1受体拮抗药福沙匹坦二甲葡胺,总收率63%(以阿瑞匹坦计)。
Aprepitant was condensed with tetrabenzyl pyrophosphate to give [3 - [[(2R, 3S) -2 - [(1R) -1- [3,5-bistrifluoromethylphenyl] ethoxy ] -4- (4-fluorophenyl) -4-morpholinyl] methyl] -5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl] Dibenzyl ester and a benzyl group was removed in methanol to give [3 - [[(2R, 3S) -2 - [(1R) -1- [3,5-bistrifluoromethylphenyl] ethoxy (4-fluorophenyl) -4-morpholinyl] methyl] -5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl] - Monobenzyl Phosphate, Benzylaminated Benzylamin-1 Receptor Antagonist Oxidized by Benzoyl Hydrogenated Benzylamine Hydrochloride and Thalidomide Formosafostin Dimedulamide, with a total yield of 63% (with aprepitant) .