NOVEL PROCESSES FOR PREPARING TRIAZOLO[4, 5-d]PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
申请人:Nair Vignesh
公开号:US20130317220A1
公开(公告)日:2013-11-28
Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.
本文提供了一种新型的三唑并[4,5-d]嘧啶衍生物制备方法。特别提供了一种新型、商业可行和工业上优劣势明显的制备高纯度替卡格雷洛或其药学可接受盐的方法。此外,本文还提供了一种制备取代环戊胺衍生物的新方法,这些衍生物在制备三唑并[4,5-d]嘧啶化合物中是有用的中间体。特别提供了一种新型、商业可行和工业上优劣势明显的制备替卡格雷洛中间体2-[[(3aR,4S,6R,6aS)-6-氨基-2,2-二甲基四氢-3aH-环戊[d][1,3]-二氧杂环-4-基]氧基]-1-乙醇的方法。