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An efficient biocatalytic process has been developed to obtain optically pure (1S,4R)-N-(benzylcarbamoyl)- 4-aminocyclopent-2-en-1-ol which can be used as the key intermediate of ticagrelor. In this research, several N-(benzylcarbamoyl)-4-aminocyclopent-2-en-1-ol derivatives have been investigated in which Candida antarctica lipase B (CALB) was used to catalyze the asymmetric hydrolysis reaction. As expected, some of these substrates successfully gave (1S,4R)-N-(benzylcarbamoyl)-4-aminocyclopent- 2-en-1-ol in >98% enantiomeric excess (ee) with conversion yields up to 45%. 相似文献
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以2-丙硫基-4,6-二氢-5-氨基嘧啶和2-{[(3aR,4S,6R,6aS)-6-氨基-2,2-二甲基四氢-3aH-环戊基[d][1,3]二氧-4-基]氧}-1-乙醇L-酒石酸盐为原料,经C-N偶联,亲核取代和环合反应制得2-{[(3aR,4S,6R,6aS)-6-(7-氯-5-丙硫基-3H-[1,2,3]三唑[4,5-d]嘧啶-3-基)-2,2-二甲基四氢-3aH-环戊基[d][1,3]二氧-4-基]氧}-1-乙醇(4); 4与(1R,2S)-2-(3,4-二氟苯基)环丙胺D-扁桃酸盐经亲核取代反应后酸解脱除丙酮叉保护基合成替格瑞洛,总收率58.7%,纯度99.2%,其结构经1H NMR, MS(ESI)和XRD确证。 相似文献
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《印度化学会志》2023,100(1):100800
Based on the foregoing gram-scale laboratory process, an efficient scale-up process for preparation of the diasteriomeric impurities of Ticagrelor is reported. The complete characterization of all impurities is presented to ensure stereo chemical structural integrity of the diastereomers.IPDO communication number: IPDO-IPM-00677. 相似文献
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